405 results match your criteria Current Opinion in Drug Discovery & Development [Journal]


Developing animal models of Zika virus infection for novel drug discovery.

Expert Opin Drug Discov 2019 Apr 16:1-13. Epub 2019 Apr 16.

a Department of Microbiology, Institute of Biomedical Sciences , University of São Paulo , São Paulo , Brazil.

Introduction: Just before the Brazilian outbreak, Zika virus was related to a mild infection, causing fever and skin rash. Congenital Zika Syndrome was first described in Brazil, causing microcephaly and malformations in newborns. Three years after the outbreak, the mechanisms of Zika pathogenesis are still not completely elucidated. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1597050DOI Listing
April 2019
2 Reads

Drugs that target aging: how do we discover them?

Authors:
A Myers G J Lithgow

Expert Opin Drug Discov 2019 Apr 11:1-8. Epub 2019 Apr 11.

a Buck Institute for Research on Aging , Novato , CA , USA.

Introduction: Biology of aging is focused on elucidating the biochemical and genetic pathways that contribute to cellular damage accumulation over time. Thirty years of research are beginning to bear fruit as the first pharmacological interventions based on biology of aging go through clinical trials. Evolutionary theories of aging suggest that naturally selected traits believed to impart fitness in young organisms may be damaging in later life. Read More

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http://dx.doi.org/10.1080/17460441.2019.1597049DOI Listing
April 2019
2 Reads

Molecular insights into cancer drug resistance from a proteomics perspective.

Expert Rev Proteomics 2019 Mar 29:1-17. Epub 2019 Mar 29.

a West China School of Basic Medical Sciences & Forensic Medicine , Sichuan University , Chengdu , PR China.

Introduction: Resistance to chemotherapy and development of specific and effective molecular targeted therapies are major obstacles facing current cancer treatment. Comparative proteomic approaches have been employed for the discovery of putative biomarkers associated with cancer drug resistance and have yielded a number of candidate proteins, showing great promise for both novel drug target identification and personalized medicine for the treatment of drug-resistant cancer. Areas covered: Herein, we review the recent advances and challenges in proteomics studies on cancer drug resistance with an emphasis on biomarker discovery, as well as understanding the interconnectivity of proteins in disease-related signaling pathways. Read More

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http://dx.doi.org/10.1080/14789450.2019.1601561DOI Listing
March 2019
3 Reads

The discovery and development of inhaled therapeutics for migraine.

Expert Opin Drug Discov 2019 Mar 29:1-9. Epub 2019 Mar 29.

a Headache Group, Department of Basic and Clinical Neuroscience , King's College London , London , UK.

Introduction: Migraine is a disabling primary headache disorder that requires effective treatments. Inhalation is currently being explored for the delivery of drugs for migraine. Pulmonary-route delivery of drugs shows potential advantages for its use as a treatment, particularly compared the oral route. Read More

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http://dx.doi.org/10.1080/17460441.2019.1598373DOI Listing
March 2019
1 Read

Current opinion and mechanistic interpretation of combination therapy for castration-resistant prostate cancer.

Authors:
Jin Xu Yun Qiu

Asian J Androl 2019 Mar 22. Epub 2019 Mar 22.

Department of Pharmacology, University of Maryland School of Medicine, Baltimore, MD 21201, USA.

Recent advances in genomics technology have led to the massive discovery of new drug targets for prostate cancer; however, none of the currently available therapeutics is curative. One of the greatest challenges is drug resistance. Combinations of therapies with distinct mechanisms of action represent a promising strategy that has received renewed attention in recent years. Read More

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http://dx.doi.org/10.4103/aja.aja_10_19DOI Listing

How can we develop better antispasmodics for irritable bowel syndrome?

Expert Opin Drug Discov 2019 Mar 28:1-14. Epub 2019 Mar 28.

d Department of Toxicology and Pharmacology, Faculty of Pharmacy , Tehran University of Medical Sciences , Tehran , Iran.

Introduction: Irritable bowel syndrome (IBS) is a prevalent gastrointestinal (GI) disease. Antispasmodics are a heterogeneous group of drugs that tackle IBS-associated altered bowel habit and abdominal pain. However, some studies have shown their failure to exhibit benefit over placebo. Read More

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http://dx.doi.org/10.1080/17460441.2019.1593369DOI Listing
March 2019
2 Reads

The impact of decreasing biodiversity on novel drug discovery: is there a serious cause for concern?

Authors:
David J Newman

Expert Opin Drug Discov 2019 Mar 22:1-5. Epub 2019 Mar 22.

a Newman Consulting LLC , Wayne , PA , USA.

Introduction: The aim of this perspective is to discuss the current and potential situation concerning the loss of biodiversity and its current and potential effects upon the search for novel bioactive agents from natural sources, be they from marine, microbial or terrestrial environments. Areas covered: Herein, the author covers terrestrial plants, marine organisms (but not vertebrates), and unicellular microbes from both terrestrial and marine sources. The emphasis is on the unknown effects of biodiversity perturbation and/or loss of microbes that are now realized to underlie the production of a significant number of natural products, whether they were first found in plants or marine invertebrates. Read More

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http://dx.doi.org/10.1080/17460441.2019.1593370DOI Listing
March 2019
1 Read

A patent update on cannabinoid receptor 1 antagonists (2015-2018).

Expert Opin Ther Pat 2019 Apr 8;29(4):261-269. Epub 2019 Apr 8.

a Center for Drug Discovery , RTI International , RTP , NC , USA.

Introduction: The endocannabinoid system is an important regulator of various physiological processes. Preclinical and clinical studies indicate that attenuation of the endocannabinoid system via antagonism of the type 1 cannabinoid receptor (CB1) is an excellent strategy to treat obesity, metabolic syndrome and associated disorders. However, centrally acting antagonists of CB1 also produce adverse effects like depression and anxiety. Read More

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http://dx.doi.org/10.1080/13543776.2019.1597851DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6476312PMC
April 2019
2 Reads

Spectrum of candidate molecules against Chikungunya virus - an insight into the antiviral screening platforms.

Expert Rev Anti Infect Ther 2019 Apr 27;17(4):243-264. Epub 2019 Mar 27.

a Manipal Centre for Virus Research , Manipal Academy of Higher Education (Deemed to be University) , Manipal , Karnataka , India.

Introduction: Chikungunya disease has undergone a phenomenal transition in its status from being recognized as a sporadic infection to acquiring a global prominence over the last couple of decades. The causative agent behind the explosive epidemics worldwide is the re-emerging pathogen, Chikungunya virus (CHIKV). Areas covered: The current review discusses all the possible avenues of antiviral research towards combating CHIKV infection. Read More

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http://dx.doi.org/10.1080/14787210.2019.1595591DOI Listing

Pharmaceutical "New Prior Knowledge": Twenty-First Century Assurance of Therapeutic Equivalence.

AAPS PharmSciTech 2019 Mar 12;20(3):140. Epub 2019 Mar 12.

Arnold and Marie Schwartz College of Pharmacy and Health Sciences, 75 DeKalb Avenue, Room WL 313, Brooklyn, New York, 11201, USA.

Facilitating utility of prior knowledge to accelerate evidence-based new drug development is a focus of several communities of knowledge, such as clinical pharmacology. For example, progress has been made via modeling and simulation of pharmacokinetic and pharmacodynamic relationships in the more effective use of "End of Phase 2" regulatory meetings for a New Drug Application (NDA). Facilitating utility of prior "Chemistry, Manufacturing, and Controls" (CMC) knowledge to accelerate new drug development and regulatory review process is also a topic of significant interest. Read More

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http://dx.doi.org/10.1208/s12249-019-1347-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6439171PMC
March 2019
3 Reads

Structure-Based Macrocycle Design in Small-Molecule Drug Discovery and Simple Metrics To Identify Opportunities for Macrocyclization of Small-Molecule Ligands.

J Med Chem 2019 Mar 22. Epub 2019 Mar 22.

Cambridge Crystallographic Data Centre , 252 Nassau Street , Princeton , New Jersey 08542 , United States.

Interest is growing in the use of macrocycles in pharmaceutical discovery. Macrocylization may provide a gateway to an expanded chemical space for small-molecule drug discovery, and this could be beneficial in prosecuting difficult targets, e.g. Read More

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http://dx.doi.org/10.1021/acs.jmedchem.8b01985DOI Listing
March 2019
1 Read

Screening drugs for myocardial disease in vivo with zebrafish: an expert update.

Expert Opin Drug Discov 2019 Apr 6;14(4):343-353. Epub 2019 Mar 6.

c Cardiovascular Medicine , Brigham and Women's Hospital, Harvard Medical School , Boston , MA , USA.

Introduction: Our understanding of the complexity of cardiovascular disease pathophysiology remains very incomplete and has hampered cardiovascular drug development over recent decades. The prevalence of cardiovascular diseases and their increasing global burden call for novel strategies to address disease biology and drug discovery. Areas covered: This review describes the recent history of cardiovascular drug discovery using in vivo phenotype-based screening in zebrafish. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1577815DOI Listing
April 2019
6 Reads

Exciting advances in GPCR-based drugs discovery for treating metabolic disease and future perspectives.

Expert Opin Drug Discov 2019 May 1;14(5):421-431. Epub 2019 Mar 1.

d Neurotransmission et signalisation laboratoire , Inserm UMR-S 839 , Paris , France.

Introduction: Current pharmacological therapies that target single receptors have limited efficacy for the treatment of diabetes and obesity. Novel approaches with hybrid peptides that activate more than one receptor at once to generate beneficial effects through synergistic effects have shown promising results. Several unimolecular dual and tri-agonists, mainly associated with GPCR like GLP-1/GCG/GIP receptors, have shown exceptional efficacy in preclinical models, and are currently being evaluated in clinical trials to investigate their safety and beneficial effects in humans. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1583642DOI Listing
May 2019
8 Reads

Current strategies toward safer mu opioid receptor drugs for pain management.

Expert Opin Ther Targets 2019 Apr 15;23(4):315-326. Epub 2019 Mar 15.

a Department of Psychiatry , McGill University, Douglas Hospital Research Center , Montréal , QC , Canada.

Introduction: Pain relief remains a major public health challenge. The most efficient available painkillers are opioids targeting the mu opioid receptor (MOR). MORs are expressed in the areas of the brain [including pain and respiratory centers] that are important for processing reward and aversion. Read More

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http://dx.doi.org/10.1080/14728222.2019.1586882DOI Listing

Current Treatment Options for Breast Cancer Brain Metastases.

Curr Treat Options Oncol 2019 Feb 15;20(3):19. Epub 2019 Feb 15.

Department of Medicine, Burkhardt Brain Tumor and Neuro-Oncology Center, Neurological Institute, Cleveland Clinic, 9500 Euclid Ave, S73, Cleveland, OH, 44195, USA.

Opinion Statement: In the past, the standard of care for treatment of BM was whole brain radiation therapy (WBRT), stereotactic radiosurgery (SRS), and surgery. There has been a greater role for medical therapies in the last two decades due to the discovery of driver mutations and corresponding targeted therapies. These innovations have dramatically altered the approach to treating these patients. Read More

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http://dx.doi.org/10.1007/s11864-019-0618-5DOI Listing
February 2019
3 Reads

Animal models of ischemic stroke and their impact on drug discovery.

Expert Opin Drug Discov 2019 Mar 4;14(3):315-326. Epub 2019 Feb 4.

c Department of Neurology , University Medicine Göttingen , Göttingen , Germany.

Introduction: Representing the leading cause of long-term disability, ischemic stroke urgently needs further research and drug development. This review summarizes current animal models of ischemic stroke that can be used for drug discovery. Areas covered: Several reproducible models of permanent and transient focal cerebral ischemia have been established in a variety of animal species including rats and mice, in which a brain-supplying artery, often the middle cerebral artery, is occluded by mechanical devices including sutures, clips and hooks, pharmacological agents or delivery of blot clots. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1573984DOI Listing
March 2019
8 Reads

Anticancer drug discovery using multicellular tumor spheroid models.

Expert Opin Drug Discov 2019 Mar 28;14(3):289-301. Epub 2019 Jan 28.

a Biosciences Laboratory , Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (IRST) IRCCS , Meldola , Italy.

Introduction: Despite the increasing financial outlay on cancer research and drug discovery, many advanced cancers remain incurable. One possible strategy for increasing the approval rate of new anticancer drugs for use in clinical practice could be represented by three-dimensional (3D) tumor models on which to perform in vitro drug screening. There is a general consensus among the scientific community that 3D tumor models more closely recapitulate the complexity of tumor tissue architecture and biology than bi-dimensional cell cultures. Read More

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http://dx.doi.org/10.1080/17460441.2019.1570129DOI Listing
March 2019
6 Reads

Novel antiviral drug discovery strategies to tackle drug-resistant mutants of influenza virus strains.

Expert Opin Drug Discov 2019 Feb 26;14(2):153-168. Epub 2018 Dec 26.

b Department of Biotechnology , College of Life Science and Biotechnology, Yonsei University , Seoul , South Korea.

Introduction: The emergence of drug-resistant influenza virus strains highlights the need for new antiviral therapeutics to combat future pandemic outbreaks as well as continuing seasonal cycles of influenza. Areas covered: This review summarizes the mechanisms of current FDA-approved anti-influenza drugs and patterns of resistance to those drugs. It also discusses potential novel targets for broad-spectrum antiviral drugs and recent progress in novel drug design to overcome drug resistance in influenza. Read More

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http://dx.doi.org/10.1080/17460441.2019.1560261DOI Listing
February 2019
3 Reads

Brentuximab vedotin in T-cell lymphoma.

Expert Rev Hematol 2019 Jan 18;12(1):5-19. Epub 2018 Dec 18.

a Department of Haematology , Peter MacCallum Cancer Centre , Melbourne , Australia.

Introduction: Brentuximab vedotin is an antibody-drug conjugate, which combines a CD30 monoclonal antibody with the microtubule-disrupting agent monomethylauristatin E. The utility of brentuximab vedotin has been explored in a number of diseases, with a recent focus on T-cell lymphoma, particularly systemic anaplastic large-cell lymphoma (sALCL) and cutaneous T-cell lymphoma (CTCL), as well as other peripheral T-cell lymphoma (PTCL) histologies. Areas covered: This review surveys current data on the efficacy of brentuximab vedotin in T-cell lymphoma, as well as embedding it in a therapeutic context by reviewing potential competitor agents in the clinic. Read More

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https://www.tandfonline.com/doi/full/10.1080/17474086.2019.1
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http://dx.doi.org/10.1080/17474086.2019.1558399DOI Listing
January 2019
23 Reads

Current state on tryptophan 2,3-dioxygenase inhibitors: a patent review.

Expert Opin Ther Pat 2019 01 16;29(1):11-23. Epub 2019 Jan 16.

a Medicinal Chemistry Research Group (CMFA), Louvain Drug Research Institute (LDRI) , Université Catholique de Louvain (UCLouvain) , Brussels , Belgium.

Introduction: Tryptophan-2, 3-dioxygenase (TDO2) is a tryptophan-degrading enzyme constitutively expressed in the liver and to a lesser extend in the brain. Before its link to cancer immunotherapy was discovered in 2011, the search for TDO2 inhibitors was initially driven by depression therapy. In the recent years, TDO2 has drawn an increasing attention as a promising target in both cancer and neuropsychiatric diseases. Read More

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http://dx.doi.org/10.1080/13543776.2019.1556638DOI Listing
January 2019
1 Read

Current developments in lantibiotic discovery for treating Clostridium difficile infection.

Expert Opin Drug Discov 2019 Jan 27;14(1):71-79. Epub 2018 Nov 27.

a Alderley Park Macclesfield , Evotec , Cheshire , UK.

Introduction: Clostridium difficile is a major cause of healthcare-associated diarrhea linked to the misuse of antimicrobials and the corresponding deleterious impact they have on the protective microbiota of the gut. Resistance to agents used to treat C. difficile including metronizadole and vancomycin has been reported highlighting the need for novel agents. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2019.1
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http://dx.doi.org/10.1080/17460441.2019.1549032DOI Listing
January 2019
31 Reads

A patent review of the ubiquitin ligase system: 2015-2018.

Expert Opin Ther Pat 2018 Dec 23;28(12):919-937. Epub 2018 Nov 23.

c Barbara Ann Karmanos Cancer Institute, and Departments of Oncology, Pharmacology and Pathology, School of Medicine , Wayne State University , Detroit , MI , USA.

Introduction: Ubiquitin-proteasome system (UPS) has been validated as a novel anticancer drug target in the past 20 years. The UPS contains two distinct steps: ubiquitination of a substrate protein by ubiquitin activating enzyme (E1), ubiquitin conjugating enzyme (E2), and ubiquitin ligase (E3), and substrate degradation by the 26S proteasome complex. The E3 enzyme is the central player in the ubiquitination step and has a wide range of specific substrates in cancer cells, offering great opportunities for discovery and development of selective drugs. Read More

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https://www.tandfonline.com/doi/full/10.1080/13543776.2018.1
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http://dx.doi.org/10.1080/13543776.2018.1549229DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6398165PMC
December 2018
30 Reads

Disease-modifying drugs in osteoarthritis: current understanding and future therapeutics.

Expert Opin Emerg Drugs 2018 12 3;23(4):331-347. Epub 2018 Dec 3.

a Rheumatology Department, Royal North Shore Hospital, and, Institute of Bone and Joint Research, Kolling Institute , University of Sydney , Sydney , Australia.

Introduction: Osteoarthritis (OA) is a leading cause of pain and disability among adults with a current prevalence of around 15% and a predicted prevalence of 35% in 2030 for symptomatic OA. It is increasingly recognized as a heterogeneous multi-faceted joint disease with multi-tissue involvement of varying severity. Current therapeutic regimens for OA are only partially effective and often have significant associated toxicities. Read More

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https://www.tandfonline.com/doi/full/10.1080/14728214.2018.1
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http://dx.doi.org/10.1080/14728214.2018.1547706DOI Listing
December 2018
307 Reads
3.058 Impact Factor

High-throughput drug screens for amyotrophic lateral sclerosis drug discovery.

Expert Opin Drug Discov 2018 11 13;13(11):1015-1025. Epub 2018 Oct 13.

a Sheffield Institute for Translational Neuroscience (SITraN) , University of Sheffield , Sheffield , United Kingdom.

Introduction: Amyotrophic lateral sclerosis (ALS) is a rapid adult-onset neurodegenerative disorder characterised by the progressive loss of upper and lower motor neurons. Current treatment options are limited for ALS, with very modest effects on survival. Therefore, there is a unmet need for novel therapeutics to treat ALS. Read More

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http://dx.doi.org/10.1080/17460441.2018.1533953DOI Listing
November 2018
4 Reads

Managing urinary incontinence in women - a review of new and emerging pharmacotherapy.

Expert Opin Pharmacother 2018 12 10;19(18):1989-1997. Epub 2018 Oct 10.

a Urology Department, Agostino Gemelli Academic Hospital Foundation IRCCS , Catholic University School of Medicine of Rome , Rome , Italy.

Introduction: The pharmacological treatment of urinary incontinence and overactive bladder (OAB) has been, for a longer time, based on antimuscarinic agents. In recent years, two other pharmacological principles have been introduced for the treatment of OAB and urgency urinary incontinence: the β3-adrenergic agent mirabegron and botulinum neurotoxin. Meanwhile, there is lack of effective drugs for the treatment of stress incontinence. Read More

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https://www.tandfonline.com/doi/full/10.1080/14656566.2018.1
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http://dx.doi.org/10.1080/14656566.2018.1532502DOI Listing
December 2018
3 Reads

RNAi-based therapeutics for lung cancer: biomarkers, microRNAs, and nanocarriers.

Expert Opin Drug Deliv 2018 10 21;15(10):965-982. Epub 2018 Sep 21.

a Department of Pharmaceutical Technology, Faculty of Pharmacy , University of Coimbra , Coimbra , Portugal.

Introduction: Despite the current advances in the discovery of the lung cancer biomarkers and, consequently, in the diagnosis, this pathology continues to be the primary cause of cancer-related death worldwide. In most cases, the illness is diagnosed in an advanced stage, which limits the current treatment options available and reduces the survival rate. Therefore, RNAi-based therapy arises as a promising option to treat lung cancer. Read More

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http://dx.doi.org/10.1080/17425247.2018.1517744DOI Listing
October 2018
2 Reads

The use of biomarkers as a tool for novel psoriatic disease drug discovery.

Expert Opin Drug Discov 2018 09 20;13(9):875-887. Epub 2018 Aug 20.

d Department of Rheumatology , Hammersmith Hospital , London , UK.

Introduction: Psoriatic disease is a relatively new term which encompasses psoriatic arthritis, psoriasis, and associated comorbidities. In this heterogeneous condition, the study of biomarkers is necessary to direct best therapy. Resulting in significant disability and socioeconomic burden, recent recommendations stress the need for tight control in psoriatic disease. Read More

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http://dx.doi.org/10.1080/17460441.2018.1508206DOI Listing
September 2018
19 Reads

Developments in lncRNA drug discovery: where are we heading?

Expert Opin Drug Discov 2018 09 6;13(9):837-849. Epub 2018 Aug 6.

a Center for Therapeutic Innovation and Department of Psychiatry and Behavioral Sciences , University of Miami Miller School of Medicine , Miami , FL , USA.

Introduction: The central dogma of molecular biology, which states that the only role of long RNA transcripts is to convey information from gene to protein, was brought into question in recent years due to discovery of the extensive presence and complex roles of long noncoding RNAs (lncRNAs). Furthermore, lncRNAs were found to be involved in pathogenesis of multiple diseases and thus represent a new class of therapeutic targets. Translational efforts in the lncRNA field have been augmented by progress in optimizing the chemistry and delivery platforms of lncRNA-targeting modalities, including oligonucleotide-based drugs and CRISPR-Cas9. Read More

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http://dx.doi.org/10.1080/17460441.2018.1501024DOI Listing
September 2018
4 Reads

Structure-kinetic relationships that control the residence time of drug-target complexes: insights from molecular structure and dynamics.

Curr Opin Chem Biol 2018 06 6;44:101-109. Epub 2018 Jul 6.

Department of Chemistry, Institute for Chemical Biology & Drug Discovery, Stony Brook University, Stony Brook, New York, USA; Department of Radiology, Stony Brook University School of Medicine, Stony Brook, New York, USA.

Time-dependent target occupancy is a function of both the thermodynamics and kinetics of drug-target interactions. However, while the optimization of thermodynamic affinity through approaches such as structure-based drug design is now relatively straight forward, less is understood about the molecular interactions that control the kinetics of drug complex formation and breakdown since this depends on both the ground and transition state energies on the binding reaction coordinate. In this opinion we highlight several recent examples that shed light on current approaches that are elucidating the factors that control the life-time of the drug-target complex. Read More

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http://dx.doi.org/10.1016/j.cbpa.2018.06.002DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6066427PMC
June 2018
3 Reads

Proteomic approaches for novel systemic lupus erythematosus (SLE) drug discovery.

Authors:
Yaxi Li Tianfu Wu

Expert Opin Drug Discov 2018 08 4;13(8):765-777. Epub 2018 Jun 4.

a Department of Biomedical Engineering , University of Houston , Houston , TX , USA.

Introduction: Systemic lupus erythematosus (SLE) is a complex autoimmune disease with a high risk of morbidity and mortality; however, there is no cure and the current medications are far from optimal in addressing efficacy and safety concerns. Over the past decade, various emerging technologies have been used in the search for novel drug targets of SLE which have resulted in numerous promising data. However, the systematic review and careful digestion of this information have been lacking. Read More

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http://dx.doi.org/10.1080/17460441.2018.1480718DOI Listing
August 2018
2 Reads

Management of Resistance to First-Line Anaplastic Lymphoma Kinase Tyrosine Kinase Inhibitor Therapy.

Curr Treat Options Oncol 2018 May 28;19(7):37. Epub 2018 May 28.

Oncology Department, Centre Hospitalier Universitaire Vaudois, BH09/725, Rue du Bugnon 46, 1000, Lausanne, Switzerland.

Opinion Statement: A decade after the discovery of echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (EML4-ALK) rearrangements in non-small cell lung cancer (NSCLC), several inhibitors have gained regulatory approval, and their sequential use has deferred platinum-based chemotherapy to later lines of therapy. Nevertheless, although most ALK-driven tumors dramatically respond to ALK TKIs , all patients ultimately develop drug-resistant disease. Analysis of post-progression biopsy samples has provided invaluable insight into the mechanisms of resistance, now informing on subsequent therapeutic strategies. Read More

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http://dx.doi.org/10.1007/s11864-018-0553-xDOI Listing
May 2018
2 Reads

Comparative efficacy and acceptability of antidiabetic agents for Alzheimer's disease and mild cognitive impairment: A systematic review and network meta-analysis.

Diabetes Obes Metab 2018 10 19;20(10):2467-2471. Epub 2018 Jun 19.

Mood Disorders Psychopharmacology Unit, Toronto Western Hospital, University Health Network, Toronto, Canada.

This study (registered with PROSPERO, CRD42018085967) compares the efficacy (i.e. pro-cognitive effects) and acceptability of antidiabetic agents for Alzheimer's disease (AD) and mild cognitive impairment (MCI). Read More

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http://dx.doi.org/10.1111/dom.13373DOI Listing
October 2018
8 Reads
1 Citation
6.360 Impact Factor

Mitochondrial disease patient motivations and barriers to participate in clinical trials.

PLoS One 2018 17;13(5):e0197513. Epub 2018 May 17.

Mitochondrial Medicine Frontier Program, The Children's Hospital of Philadelphia, Philadelphia, Pennsylvania, United States of America.

Background: Clinical treatment trials are increasingly being designed in primary mitochondrial disease (PMD), a phenotypically and genetically heterogeneous collection of inherited multi- system energy deficiency disorders that lack effective therapy. We sought to identify motivating factors and barriers to clinical trial participation in PMD.

Methods: A survey study was conducted in two independent mitochondrial disease subject cohorts. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0197513PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5957366PMC
December 2018
4 Reads

A systems biology approach to antimalarial drug discovery.

Expert Opin Drug Discov 2018 07 8;13(7):617-626. Epub 2018 May 8.

c Laboratório de Malária , Instituto René Rachou, Fundação Oswaldo Cruz , Belo Horizonte , Brazil.

Introduction: In spite of significant efforts to reduce malaria deaths, this disease still kills around 445,000 people every year. Overcoming drug resistance is one of the main goals of current malaria research programs. This is challenging, since the biology of Plasmodium is not fully understood, requiring the development of advanced models for data analysis in the search for new antimalarials. Read More

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https://www.tandfonline.com/doi/full/10.1080/17460441.2018.1
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http://dx.doi.org/10.1080/17460441.2018.1471056DOI Listing
July 2018
15 Reads

Emerging therapeutic targets for treatment of leishmaniasis.

Expert Opin Ther Targets 2018 06 9;22(6):467-486. Epub 2018 May 9.

a Department of Medicine , Institute of Medical Sciences, Banaras Hindu University , Varanasi , UP , India.

Introduction: Parasitic diseases that pose a threat to human life include leishmaniasis - caused by protozoan parasite Leishmania species. Existing drugs have limitations due to deleterious side effects like teratogenicity, high cost and drug resistance. This calls for the need to have an insight into therapeutic aspects of disease. Read More

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http://dx.doi.org/10.1080/14728222.2018.1472241DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6047532PMC
June 2018
5 Reads

Discovery and development of varenicline for smoking cessation.

Expert Opin Drug Discov 2018 07 28;13(7):671-683. Epub 2018 Mar 28.

a Molecular Targets and Medications Discovery Branch, Intramural Research Program , National Institute on Drug Abuse, National Institutes of Health , Baltimore , MD , USA.

Introduction: Tobacco use causes one premature death every six seconds. Current smoking cessation aids include nicotine replacement therapies, bupropion, and varenicline. Although more than 70% of smokers express a desire to quit, fewer than 3% remain abstinent for more than one year, highlighting a critical need for more efficacious smoking cessation treatments. Read More

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http://dx.doi.org/10.1080/17460441.2018.1458090DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6179352PMC
July 2018
23 Reads

Recent developments with tau-based drug discovery.

Expert Opin Drug Discov 2018 05 1;13(5):399-410. Epub 2018 Mar 1.

a Department of Neurochemistry, Inge Grundke-Iqbal Research Floor , New York State Institute for Basic Research in Developmental Disabilities , Staten Island , NY , USA.

Introduction: Alzheimer's disease (AD), which accounts for three fourth of all cases of dementia, is a major public health problem in modern society and, yet, there is no effective treatment available that can prevent or inhibit this chronic progressive neurodegenerative disease. A major current drug target is intraneuronal abnormally hyperphosphorylated microtubule-associated protein tau which is a histopathological hallmark of this disease and of a family of neurodegenerative diseases called tauopathies. Areas covered: In this review, the authors discuss a growing number of studies that describe the nature and mechanism of tau pathology and various drug discovery options and most recent developments in tau-based therapeutics. Read More

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http://dx.doi.org/10.1080/17460441.2018.1445084DOI Listing
May 2018
11 Reads

Evaluation of cAMS for C microtracer ADME studies: opportunities to change the current drug development paradigm.

Bioanalysis 2018 Mar 16;10(5):321-339. Epub 2018 Feb 16.

Novartis Pharma AG, Novartis Institutes for Biomedical Research, PK Sciences, Fabrikstrasse 14, CH-4002 Basel, Switzerland.

Aim: Although regulatory guidances require human metabolism information of drug candidates early in the development process, the human mass balance study (or hADME study), is performed relatively late. hADME studies typically involve the administration of a C-radiolabelled drug where biological samples are measured by conventional scintillation counting analysis. Another approach is the administration of therapeutic doses containing a C-microtracer followed by accelerator mass spectrometry (AMS) analysis, enabling hADME studies completion much earlier. Read More

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https://www.future-science.com/doi/10.4155/bio-2017-0216
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http://dx.doi.org/10.4155/bio-2017-0216DOI Listing
March 2018
24 Reads

Optogenetics in cancer drug discovery.

Expert Opin Drug Discov 2018 05 15;13(5):459-472. Epub 2018 Feb 15.

a Department of Biochemistry and Molecular Biology , Medical University of Lublin , Lublin , Poland.

Introduction: The discovery and domestication of biomolecules that respond to light has taken a light of its own, providing new molecular tools with incredible spatio-temporal resolution to manipulate cellular behavior. Areas covered: The authors herein analyze the current optogenetic tools in light of their current, and potential, uses in cancer drug discovery, biosafety and cancer biology. Expert opinion: The pipeline from drug discovery to the clinic is plagued with drawbacks, where most drugs fail in either efficacy or safety. Read More

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http://dx.doi.org/10.1080/17460441.2018.1437138DOI Listing
May 2018
11 Reads

Current insights into anti-HIV drug discovery and development: a review of recent patent literature (2014-2017).

Expert Opin Ther Pat 2018 04 13;28(4):299-316. Epub 2018 Feb 13.

a Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences , Shandong University , Ji'nan , PR China.

Introduction: To deal with the rapid emergence of drug resistance challenges, together with the difficulty to eradicate the virus, off-target effects and significant cumulative drug toxicities, it is still imperative to develop next-generation anti-HIV agents with novel chemical classes or new mechanisms of action.

Areas Covered: We primarily focused on current strategies to discover novel anti-HIV agents. Moreover, examples of anti-HIV lead compounds were mainly selected from recently patented publications (reported between 2014 and 2017). Read More

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http://dx.doi.org/10.1080/13543776.2018.1438410DOI Listing
April 2018
5 Reads

Pharmacovigilance: pharmacists' perspective on spontaneous adverse drug reaction reporting.

Integr Pharm Res Pract 2017 22;6:91-98. Epub 2017 Mar 22.

Faculty of Pharmacy, Umm-Al-Qura University, Makkah, Saudi Arabia.

Globally, adverse drug reactions (ADRs), one of the leading causes of morbidity and mortality, will continue to pose a threat to public health as long as drugs are being used to treat various ailments. Prompt ADR reporting is crucial in ensuring drug safety. The aim of this narrative review was to highlight the role of pharmacists in pharmacovigilance and to identify barriers and facilitators toward ADR reporting documented in the literature. Read More

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http://dx.doi.org/10.2147/IPRP.S105881DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5774327PMC
March 2017
3 Reads

An update on the advancing high-throughput screening techniques for patch clamp-based ion channel screens: implications for drug discovery.

Expert Opin Drug Discov 2018 03 17;13(3):269-277. Epub 2018 Jan 17.

a Nanion Technologies GmbH , Munich , Germany.

Introduction: Automated patch clamp (APC) devices have become commonplace in many industrial and academic labs. Their ease-of-use and flexibility have ensured that users can perform routine screening experiments and complex kinetic experiments on the same device without the need for months of training and experience. APC devices are being developed to increase throughput and flexibility. Read More

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http://dx.doi.org/10.1080/17460441.2018.1428555DOI Listing
March 2018
14 Reads
3.470 Impact Factor

The latest animal models of ovarian cancer for novel drug discovery.

Expert Opin Drug Discov 2018 03 17;13(3):249-257. Epub 2018 Jan 17.

a Department of Cancer Immunology and Virology , Dana-Farber Cancer Institute , Boston , MA , USA.

Introduction: Epithelial ovarian cancer is a heterogeneous disease classified into five subtypes, each with a different molecular profile. Most cases of ovarian cancer are diagnosed after metastasis of the primary tumor and are resistant to traditional platinum-based chemotherapeutics. Mouse models of ovarian cancer have been utilized to discern ovarian cancer tumorigenesis and the tumor's response to therapeutics. Read More

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http://dx.doi.org/10.1080/17460441.2018.1426567DOI Listing
March 2018
6 Reads

Lipid nanoparticles for intranasal administration: application to nose-to-brain delivery.

Expert Opin Drug Deliv 2018 04 22;15(4):369-378. Epub 2018 Jan 22.

f Perrigo Company Minneapolis , Product Development , Minneapolis , MN , USA.

Introduction: The blood brain barrier is a functional barrier allowing the entry into the brain of only essential nutrients, excluding other molecules. Its structure, although essential to keep the harmful entities out, is also a major roadblock for pharmacological treatment of brain diseases. Several alternative invasive drug delivery approaches, such as transcranial drug delivery and disruption of blood brain barrier have been explored, with limited success and several challenges. Read More

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http://dx.doi.org/10.1080/17425247.2018.1429401DOI Listing
April 2018
7 Reads

Parents' attitude, awareness and behaviour towards influenza vaccination in Pakistan.

Hum Vaccin Immunother 2018 04 25;14(4):952-957. Epub 2018 Jan 25.

f School of Pharmacy, Monash University Malaysia, Bandar Sunway, Selangor Darul Ehsan , Malaysia.

National immunization program of Pakistan does not include Influenza vaccines. The low rate of immunization might be attributed to the poor knowledge of influenza vaccination in Pakistan. Current study was aimed to assess the knowledge and attitude of influenza vaccination among parents. Read More

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http://dx.doi.org/10.1080/21645515.2017.1415686DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5893193PMC
April 2018
9 Reads
2.131 Impact Factor

Lost in translation? A critical look at the role that animal models of obsessive compulsive disorder play in current drug discovery strategies.

Expert Opin Drug Discov 2018 03 23;13(3):211-220. Epub 2017 Dec 23.

a Centro de Investigación en Reproducción Animal , CINVESTAV-Universidad Autónoma de Tlaxcala , Tlaxcala , México.

Introduction: Obsessive-compulsive disorder (OCD) is a severe neuropsychiatric illness estimated to affect between 1-3% of the population. In today's literature, there are a number well-validated and convincing animal models of OCD described. Areas covered: Herein, the authors look at the role that animal models of OCD (including transgenic models, deer mouse stereotypy, quinpirole sensitization, post-training signal attenuation, and mouse marble burying) have played in determining the current directions of OCD drug discovery. Read More

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http://dx.doi.org/10.1080/17460441.2018.1417379DOI Listing
March 2018
16 Reads

Particle morphology: an important factor affecting drug delivery by nanocarriers into solid tumors.

Expert Opin Drug Deliv 2018 04 27;15(4):379-395. Epub 2017 Dec 27.

a Department of Pharmaceutics , China Pharmaceutical University , Nanjing , PR China.

Introduction: Efficient delivery of drugs by nanoparticles deep into solid tumors is the precondition of valid cancer therapy. Despite profound understanding of the delivery of spherical nanoparticles into solid tumor attained, insufficient attention was paid to anisotropic particles. Actually, owing to their structural asymmetry, some non-spherical particles exhibit significant advantages over their spherical counterparts. Read More

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http://dx.doi.org/10.1080/17425247.2018.1420051DOI Listing
April 2018
8 Reads

Urinary peptidomics in kidney disease and drug research.

Expert Opin Drug Discov 2018 03 19;13(3):259-268. Epub 2017 Dec 19.

b Mosaiques Diagnostics GmbH , Hannover , Germany.

Introduction: Due to its close connection with the renal system, urine is considered a valuable source of information in kidney disease research. Peptidomics methods focus on the discovery of endogenous peptides, given their wide range of biological functions and diagnostic and therapeutic potential. Representing a non-invasive and sensitive method, technological prospects of urinary peptidomics should be evaluated in the context of drug discovery and research. Read More

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http://dx.doi.org/10.1080/17460441.2018.1418320DOI Listing
March 2018
7 Reads

Phenotypic screening approaches for Chagas disease drug discovery.

Expert Opin Drug Discov 2018 02 20;13(2):141-153. Epub 2017 Dec 20.

a Drugs for Neglected Diseases initiative (DNDi), R&D Department , Geneva , Switzerland.

Introduction: Chagas disease, caused by the parasite Trypanosoma cruzi, is a global public health issue. Current treatments targeting the parasite are limited to two old nitroheterocyclic drugs with serious side effects. The need for new and safer drugs has prompted numerous drug discovery efforts to identify compounds suitable for parasitological cure in the last decade. Read More

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http://dx.doi.org/10.1080/17460441.2018.1417380DOI Listing
February 2018
6 Reads