174,210 results match your criteria medicinal


Polymyxin B-inspired non-hemolytic tyrocidine A analogues with significantly enhanced activity against gram-negative bacteria: How cationicity impacts cell specificity and antibacterial mechanism.

Eur J Med Chem 2021 May 1;221:113488. Epub 2021 May 1.

National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang, 330004, PR China; Laboratoire de Méthodologie, Synthèse et Molécules Thérapeutiques (ICMMO), UMR 8182, CNRS, Université Paris-Saclay, Bât 410, Facultédes Sciences D'Orsay, Orsay, 291405, France; State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Guangxi Normal University, 15 Yuchai Road, Guilin, 541004, PR China. Electronic address:

Naturally occurring cyclic antimicrobial peptides (AMPs) such as tyrocidine A (Tyrc A) and gramicidin S (GS) are appealing targets for the development of novel antibiotics. However, their therapeutic potentials are limited by undesired hemolytic activity and relatively poor activity against Gram-negative bacteria. Inspired by polycationic lipopeptide polymyxin B (PMB), the so called 'last-resort' antibiotic for the treatment of infections caused by multidrug-resistant Gram-negative bacteria, we synthesized and biologically evaluated a series of polycationic analogues derived from Tyrc A. Read More

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Hydrogel-based therapeutic angiogenesis: An alternative treatment strategy for critical limb ischemia.

Biomaterials 2021 May 7;274:120872. Epub 2021 May 7.

Key Laboratory for Biomechanics and Mechanobiology of Ministry of Education, Beijing Advanced Innovation Centre for Biomedical Engineering, School of Biological Science and Medical Engineering, Beihang University, Beijing, 100191, PR China. Electronic address:

Critical limb ischemia (CLI) is the most severe clinical manifestation of peripheral arterial disease (PAD), resulting in the total or partial loss of limb function. Although the conventional treatment strategy of CLI (e.g. Read More

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Nitrile-based peptoids as cysteine protease inhibitors.

Bioorg Med Chem 2021 May 10;41:116211. Epub 2021 May 10.

Medicinal and Biological Chemistry Group (NEQUIMED), Institute of Chemistry of São Carlos, University of São Paulo, São Carlos/SP, Brazil.

Peptidomimetics of the class of dipeptidyl nitrile analog peptoids were synthesized as inhibitors of mammalian cysteine proteases of the papain superfamily. The dipeptidyl nitrile side chains were attached to the peptide backbone's nitrogen atom, not to the α-carbons. Synthesized nitrile-based peptoid analogs that lack the hydrogen amide at P2-P3 are responsible for many of the secondary structure elements in peptides and proteins, making them resistant to proteolysis. Read More

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Anti-trypanosomal and anthelminthic properties of ethanol and aqueous extracts of Tetrapleura tetraptera Taub.

Vet Parasitol 2021 May 10;294:109449. Epub 2021 May 10.

Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana.

Trypanosomosis and helminthosis, considered as part of neglected tropical diseases, are parasitic infections of public health importance, especially in Africa. Medicinal plants have been used in most parts of Africa, to treat these parasitic infections. The study aims to determine the anti-trypanosomal and anthelminthic properties of Tetrapleura tetraptera (fruit and stembark). Read More

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Proteomic insights into protostane triterpene biosynthesis regulatory mechanism after MeJA treatment in Alisma orientale (Sam.) Juz.

Biochim Biophys Acta Proteins Proteom 2021 May 12:140671. Epub 2021 May 12.

School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China.

Protostane triterpenes in Alisma orientale (Sam.) Juz. have unique structural features with distinct pharmacological activities. Read More

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From forest to pharmacy: should we be depressed about a sustainable Griffonia simplicifolia (Fabaceae) seed supply chain?

J Ethnopharmacol 2021 May 12:114202. Epub 2021 May 12.

Bundesamt für Naturschutz (BfN), Konstantinstr. 110, Bonn 53179, Germany.

Ethnopharmacological Relevance: Griffonia simplicifolia D.C (Baill.) (Fabaceae) seeds are unusually high (6-20% wet weight) in 5-HTP (5-Hydroxytryptophan), a serotonin precursor widely used to treat depression. Read More

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Ni and Cr impurities profile in Valeriana officinalis L., radix-based herbal medicinal product available in Polish pharmacies due to ICH Q3D guideline.

Regul Toxicol Pharmacol 2021 May 12:104945. Epub 2021 May 12.

Department of Food Chemistry and Nutrition, Medical College, Jagiellonian University, Medyczna 9, 30-688, Kraków, Poland.

Elemental impurities (EIs) profiling in final pharmaceutical products is often not adequately treated, however it is crucial problem in pharmaceutical analysis by reason of the various regulatory authorities (like ICH Q3D guideline). EIs in pharmaceuticals may arise from numerous sources of which the herbal ingredients are not a frequent subject of pharmaceutical analyses. However, based on number of traditional use registrations per year for herbal medicinal products (HMPs) in the EU, it can be stated that monocomponent HMPs are still very popular for use. Read More

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Design, synthesis and antibacterial evaluation of novel C-11, C-9 or C-2'-substituted 3-O-descladinosyl-3-ketoclarithromycin derivatives.

Bioorg Med Chem Lett 2021 May 12:128110. Epub 2021 May 12.

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, China. Electronic address:

A novel series of 3-O-descladinosyl-3-keto-clarithromycin derivatives, including 11-O-carbamoyl-3-O-descladinosyl-3-keto-clarithromycin derivatives and 2',9(S)-diaryl-3-O-descladinosyl-3-keto-clarithromycin derivatives, were designed, synthesized and evaluated for their in vitro antibacterial activity. Among them, some derivatives were found to have activity against resistant bacteria strains. In particular, compound 9b showed not only the most significantly improved activity (16 µg/mL) against S. Read More

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Discovery of a new class of JMJD6 inhibitors and structure-activity relationship study.

Bioorg Med Chem Lett 2021 May 12:128109. Epub 2021 May 12.

Department of Medicinal Chemistry, School of Medicine, Nankai University, Tianjin 300071, PR China. Electronic address:

JmjC domain-containing protein 6 (JMJD6) has been thought as a potential target for various diseases particularly cancer. However, few selective JMJD6 inhibitors have been reported. In this investigation, molecular docking and biological activity evaluation were performed to retrieve new JMJD6 inhibitors, which led to the identification of a hit compound, J2. Read More

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Emerging strategies against tumor-associated fibroblast for improved the penetration of nanoparticle into desmoplastic tumor.

Eur J Pharm Biopharm 2021 May 12. Epub 2021 May 12.

College of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China; Anhui Province Key Laboratory of Chinese Medicinal Formula, Hefei, Anhui 230012, China. Electronic address:

The therapeutic effect of nanoparticles is limited in solid tumors, especially desmoplastic tumors, because the tumor matrix hinders the delivery of nanoparticles. As the most abundant cells in the tumor stroma, tumor-associated fibroblasts (TAFs) produce a dense extracellular matrix, which leads to higher tissue fluid pressure, thereby creating a physical barrier for nanoparticle delivery. Therefore, researchers focused on eliminating TAFs to combat desmoplastic tumors. Read More

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Dengratiols A-D, four new bibenzyl derivatives from Dendrobium gratiossimum.

Fitoterapia 2021 May 12:104926. Epub 2021 May 12.

State Key Laboratory of Bioactive Substance and Function of Natural Medicines, CAMS Key Laboratory of Enzyme and Biocatalysis of Natural Drugs, and NHC Key Laboratory of Biosynthesis of Natural Products, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, China. Electronic address:

Dengratiol A (1), an unprecedented bibenzyl derivative bearing a tropolone unit together with three pairs of bibenzyl enantiomers (±)-dengratiols B-D [(±)-2-(±)-4], were isolated from Dendrobium gratiossimum Rchb.f. The resolution of enantiomers was performed with chiral HPLC. Read More

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Immunoinformatics and Pepscan strategies on the path of a peptide-based serological diagnosis of COVID19.

J Immunol Methods 2021 May 12:113071. Epub 2021 May 12.

Unidad de Química Medicinal, Facultad de Farmacia, Universidad Central de Venezuela, Caracas 1051, Venezuela. Electronic address:

Several diagnostic tools have been developed for clinical and epidemiological assays. RT-PCR and antigen detection tests are more useful for diagnosis of acute disease, while antibody tests allow the estimation of exposure in the population. Currently, there is an urgent need for the development of diagnostic tests for COVID-19 that can be used for large-scale epidemiological sampling. Read More

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Investigation of therapeutic effect of Curcumin α and β Glucoside anomers against Alzheimer's disease by the nose to brain drug delivery.

Brain Res 2021 May 12:147517. Epub 2021 May 12.

Zanjan Applied Pharmacology Research Center, Zanjan University of Medical Sciences, Zanjan, Iran; Department of Pharmacology and toxicology, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.

Alzheimer's disease (AD) is one of the greatest geriatric medicinal challenges of our century and is the main disease leading to dementia. Despite extensive scientific research advances, available disease-modifying treatment strategies remained limited; thus, increasing demand for new drugs. In recent years, medicinal plants attracted attention due to their potential role in dementia. Read More

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Nano-selenium on reproduction and immunocompetence: an emerging progress and prospect in the productivity of poultry research.

Authors:
Tanmoy Rana

Trop Anim Health Prod 2021 May 15;53(2):324. Epub 2021 May 15.

Department of Veterinary Clinical Complex (V.M.E.J.), West Bengal University of Animal & Fishery Sciences, Kolkata, India.

Nanotechnology, an emerging and promising technology, has been implicated to revolutionize the poultry industry. The main aspect of nanotechnology was to modify or alter the particle size into nanometers and thereby alter the physical as well as chemical features of the particular molecules. Selenium (Se), an essential trace element, can play an immense role in the maintenance of diverse physiological functions, body metabolism and cellular homeostasis, and the performance of poultry. Read More

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In vitro effects of aqueous extract of fermented rooibos (Aspalathus linearis) on human sperm function.

Andrologia 2021 May 15:e14114. Epub 2021 May 15.

Department of Pre-Clinical Sciences, University of Limpopo, Polokwane, South Africa.

Aspalathus linearis (rooibos) is a herbal medicinal plant originally from South Africa's fynbos and well known for its medicinal effects in treating different medical conditions. Rooibos contains significant levels of antioxidants capable of inhibiting the production of reactive oxygen species, which may improve seminal parameters. This study focussed on investigating the direct effect of fermented rooibos on human sperm functions in vitro. Read More

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Comparative HPTLC fingerprinting profile and GC-MS analysis of raw and purified () by purification method.

J Complement Integr Med 2021 May 14. Epub 2021 May 14.

Department of Dravyaguna Vijnanam, Government Ayurveda College, Thiruvananthapuram, Kerala, India.

Background: is an oleo gum resin obtained from the plant (Arn.) Bhand., used in medicines for various ailments like anti-inflammatory conditions, hyperlipidemia, thyroid disorders etc. Read More

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Copper-mediated radioiodination reaction through aryl boronic acid or ester precursor and its application to direct radiolabeling of a cyclic peptide.

J Labelled Comp Radiopharm 2021 May 14. Epub 2021 May 14.

Department of Analytical and Bioinorganic Chemistry, Division of Analytical and Physical Chemistry, Kyoto Pharmaceutical University, Kyoto, Japan.

A copper-mediated radioiodination using aryl boronic precursors is attracting attention as a solution to oxidative iododestannylation and nickel-mediated radioiodination drawbacks. The copper-mediated radiolabeling method allows radioiodination at room temperature with stable aryl boronic precursors without preparing complex starting materials or reagents, and can be performed in a reaction vessel exposed to air. This method has good potential in radiochemistry; however, studies on the scope of copper-mediated radioiodination through boronic precursors are insufficient. Read More

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Blueberry-derived exosomes-like nanoparticles ameliorate nonalcoholic fatty liver disease by attenuating mitochondrial oxidative stress.

Acta Pharmacol Sin 2021 May 14. Epub 2021 May 14.

Chongqing Key Lab of Medicinal Chemistry & Molecular Pharmacology, Chongqing University of Technology, Chongqing, 400054, China.

Accumulating evidence indicates that mitochondrial dysfunction and oxidative stress play a pivotal role in the initiation and progression of nonalcoholic fatty liver disease (NAFLD). In this study, we found that blueberry-derived exosomes-like nanoparticles (BELNs) could ameliorate oxidative stress in rotenone-induced HepG2 cells and high-fat diet (HFD)-fed C57BL/6 mice. Preincubation with BELNs decreased the level of reactive oxygen species (ROS), increased the mitochondrial membrane potential, and prevented cell apoptosis by inducing the expression of Bcl-2 and heme oxygenase-1 (HO-1) and decreasing the content of Bax in rotenone-treated HepG2 cells. Read More

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Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity.

Nat Commun 2021 May 14;12(1):2792. Epub 2021 May 14.

Department of Pathology, University of Michigan, Ann Arbor, MI, USA.

ASH1L histone methyltransferase plays a crucial role in the pathogenesis of different diseases, including acute leukemia. While ASH1L represents an attractive drug target, developing ASH1L inhibitors is challenging, as the catalytic SET domain adapts an inactive conformation with autoinhibitory loop blocking the access to the active site. Here, by applying fragment-based screening followed by medicinal chemistry and a structure-based design, we developed first-in-class small molecule inhibitors of the ASH1L SET domain. Read More

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Effect of preoperative cannabis use on perioperative outcomes: a retrospective cohort study.

Reg Anesth Pain Med 2021 May 14. Epub 2021 May 14.

Department of Anesthesia, McMaster University, Hamilton, Ontario, Canada

Introduction: The reported use of cannabis within surgical population is increasing. Cannabis use is potentially associated with increased harms and varied effects on pain control. These have important implications to perioperative care. Read More

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Distinct synaptic mechanisms underlying the analgesic effects of GABA transporter subtypes 1 and 3 inhibitors in the spinal dorsal horn.

Pain 2021 May 10. Epub 2021 May 10.

Laboratory of Pharmacology, School of Pharmaceutical Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan Medicinal Research Laboratories, School of Pharmacy, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.

Abstract: Normalization of the excitatory and inhibitory balance by increasing the levels of endogenous inhibitory neurotransmitters by blocking their reuptake is a promising therapeutic strategy for relieving chronic pain. Pharmacological blockade of spinal GABA transporter subtypes 1 and 3 (GAT1 and GAT3) has been reported to generate analgesic effects in animal models of neuropathic pain. Here we explored the synaptic mechanisms underlying their analgesic effects in the spinal dorsal horn. Read More

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Elevated CO improves the nutritive value, antibacterial, anti-inflammatory, antioxidant and hypocholestecolemic activities of lemongrass sprouts.

Food Chem 2021 Mar 31;357:129730. Epub 2021 Mar 31.

Department of Medicinal and Aromatic Plants, Desert Research Centre, Cairo, Egypt. Electronic address:

Sprouts have been regarded as a big store for bioactive compounds with a wide range of biological activities. Elevated CO (eCO, 620 μmol mol)was employed to enhance the nutritive and health promoting values of sprouts of two species of lemongrass, i.e. Read More

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Efficacy of Berberine in Treatment of Rheumatoid Arthritis: from Multiple Targets to Therapeutic Potential.

Pharmacol Res 2021 May 11:105667. Epub 2021 May 11.

National Chinmedomics Research Center, National TCM Key Laboratory of Serum Pharmacochemistry, Heilongjiang University of Chinese Medicine, Heping Road 24, Harbin, China; National Engineering Laboratory for the Development of Southwestern Endangered Medicinal Materials, Guangxi Botanical Garden of Medicinal Plants, Nanning, Guangxi, China. Electronic address:

Rheumatoid arthritis is a systemic autoimmune disorder involved in persistent synovial inflammation. Berberine is a nature-derived alkaloid compound with multiple pharmacological activities in different pathologies, including RA. Recent experimental studies have clarified several determinant cellular and molecular targets of BBR in RA, and provided novel evidence supporting the promising therapeutic potential of BBR to combat RA. Read More

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Systematic review of Ethiopian medicinal plants used for their anti-inflammatory and wound healing activities.

J Ethnopharmacol 2021 May 11:114179. Epub 2021 May 11.

Centre for Global Health Research, Brighton and Sussex Medical School, University of Sussex, Brighton, BN1 9PX, United Kingdom; School of Public Health, Addis Ababa University, Addis Ababa, Ethiopia.

Ethnopharmacological Relevance: Plant materials are used worldwide as complementary and alternative therapeutics for the treatment of various illnesses. In Ethiopia, folk medicines are utilized across a wide range of cultures and settings. Ethiopia has numerous plant species of which around 12% are endemic, making it a rich source of medicinal plants that are potentially important for human wellbeing. Read More

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Nitrosamine contamination in pharmaceuticals: threat, impact, and control.

J Pharm Sci 2021 May 11. Epub 2021 May 11.

Department of Food and Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand. Electronic address:

Nitrosamine-contaminated medicinal products have raised safety concerns towards the use of various drugs, not only valsartan and all tetrazole-containing angiotensin II receptor blockers, but also ranitidine, metformin, and other medicines, many of which have been recalled and prone to shortage. At any stages, from drug substance synthesis throughout each product's lifetime, these impurities may evolve if an amine reacts with a nitrosating agent coexisting under appropriate conditions. Consequently, drug regulatory authorities worldwide have established stringent guidelines on nitrosamine contamination for all drug products in the market. Read More

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Increasing fatty acid oxidation elicits a sex-dependent response in failing mouse hearts.

J Mol Cell Cardiol 2021 May 11. Epub 2021 May 11.

Mitochondria and Metabolism Center, Department of Anesthesiology and Pain Medicine, University of Washington, Republican Street 850, 98109 Seattle, WA, USA. Electronic address:

Background: Reduced fatty acid oxidation (FAO) is a hallmark of metabolic remodeling in heart failure. Enhancing mitochondrial long-chain fatty acid uptake by Acetyl-CoA carboxylase 2 (ACC2) deletion increases FAO and prevents cardiac dysfunction during chronic stresses, but therapeutic efficacy of this approach has not been determined.

Methods: Male and female ACC2f/f-MCM (ACC2KO) and their respective littermate controls were subjected to chronic pressure overload by TAC surgery. Read More

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Molecular Docking and Dynamic Studies of a Potential Therapeutic Target Inhibiting Glyoxalase System: metabolic action of the 3, 3 '- [3- (5-chloro-2-hydroxyphenyl) -3-oxopropane-1, 1-diyl] - bis-4-hydroxycoumarin leads overexpression of the intracellular level of methylglyoxal and induction of a pro-apoptotic phenomenon in a hepatocellular carcinoma model.

Chem Biol Interact 2021 May 11:109511. Epub 2021 May 11.

QOPNA, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal. Electronic address:

Methylglyoxal is a dicarbonyl compound recruited as a potential cytotoxic marker, initially presents in cells and considered as a metabolite of the glycolytic pathway. Our aim is to demonstrate the inhibitory effect of 3, 3'-[3-(5-chloro-2-hydroxyphenyl)-3-oxopropane-1, 1-diyl] Bis (4-hydroxycoumarin) on the glyoxalase system, and indirectly its anticancer activity. The docking of OT-55 was conducted by using Flexible docking protocol, ChiFlex and libdock tools inside the active site of Glo-I indicated that both hydrogen bonding and hydrophobic interactions contributed significantly in establishing potent binding with the active site which is selected as a strong inhibitor with high scoring values and maximum Gibbs free energy. Read More

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Endogenous vitamin E metabolites mediate allosteric PPARγ activation with unprecedented co-regulatory interactions.

Cell Chem Biol 2021 May 12. Epub 2021 May 12.

Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Frankfurt 60438, Germany. Electronic address:

Vitamin E exhibits pharmacological effects beyond established antioxidant activity suggesting involvement of unidentified mechanisms. Here, we characterize endogenously formed tocopherol carboxylates and the vitamin E mimetic garcinoic acid (GA) as activators of the peroxisome proliferator-activated receptor gamma (PPARγ). Co-stimulation of PPARγ with GA and the orthosteric agonist pioglitazone resulted in additive transcriptional activity. Read More

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Infectious clone construction and pathogenicity confirmation of Cotton leaf curl Multan virus (CLCuMuV), Ramie mosaic virus (RamV) and Corchorus yellow vein Vietnam virus (CoYVV) by southern blot analysis.

PLoS One 2021 14;16(5):e0251232. Epub 2021 May 14.

Department of Plant Sciences, College of Agricultural and Marine sciences, Sultan Qaboos University, Alkhound, Oman.

Geminiviruses are insect-transmissible, economically vital group of plant viruses, which cause significant losses to crop production and ornamental plants across the world. During this study, infectious clones of three devastating begomoviruses, i.e. Read More

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Microbially Guided Discovery and Biosynthesis of Biologically Active Natural Products.

ACS Synth Biol 2021 May 14. Epub 2021 May 14.

Department of Chemical and Biological Engineering, University of Colorado Boulder, 3415 Colorado Avenue, Boulder, Colorado 80303, United States.

The design of small molecules that inhibit disease-relevant proteins represents a longstanding challenge of medicinal chemistry. Here, we describe an approach for encoding this challenge-the inhibition of a human drug target-into a microbial host and using it to guide the discovery and biosynthesis of targeted, biologically active natural products. This approach identified two previously unknown terpenoid inhibitors of protein tyrosine phosphatase 1B (PTP1B), an elusive therapeutic target for the treatment of diabetes and cancer. Read More

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