271,445 results match your criteria receptor antagonists


Quantification of kappa opioid receptor ligand potency, efficacy and desensitization using a real-time membrane potential assay.

Biomed Pharmacother 2021 Sep 15;143:112173. Epub 2021 Sep 15.

Department of Pharmacology and Neuroscience, School of Medicine, Creighton University, Omaha, NE, USA.

We explored the utility of the real-time FLIPR Membrane Potential (FMP) assay as a method to assess kappa opioid receptor (KOR)-induced hyperpolarization. The FMP Blue dye was used to measure fluorescent signals reflecting changes in membrane potential in KOR expressing CHO (CHO-KOR) cells. Treatment of CHO-KOR cells with kappa agonists U50,488 or dynorphin [Dyn (1-13)NH] produced rapid and concentration-dependent decreases in FMP Blue fluorescence reflecting membrane hyperpolarization. Read More

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September 2021

Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists.

Eur J Med Chem 2021 Sep 9;226:113812. Epub 2021 Sep 9.

Department of Chemistry, Tsinghua University, Beijing, 100084, PR China; State Key Laboratory of Chemical Oncogenomics, Key Laboratory of Chemical Biology, Tsinghua Shenzhen International Graduate School, Tsinghua University, Shenzhen, 518055, PR China; Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University, Beijing, 100084, PR China; National & Local United Engineering Lab for Personalized Anti-tumor Drugs, Shenzhen Kivita Innovative Drug Discovery Institute, Tsinghua Shenzhen International Graduate School, Shenzhen, 518055, PR China. Electronic address:

Chemokine receptor 2 (CXCR2) is the receptor of glutamic acid-leucine-arginine sequence-contained chemokines CXCs (ELR CXCs). In recent years, CXCR2-target treatment strategy has come a long way in cancer therapy. CXCR2 antagonists could block CXCLs/CXCR2 axis, and are widely used in regulating immune cell migration, tumor metastasis, apoptosis and angiogenesis. Read More

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September 2021

Vasomotor effects of noradrenaline, 5-hydroxytryptamine, angiotensin II, bradykinin, histamine, and acetylcholine on the bat (Rhinolophus ferrumequinum) basilar artery.

Comp Biochem Physiol C Toxicol Pharmacol 2021 Sep 15:109190. Epub 2021 Sep 15.

Department of Veterinary Pharmacology, Joint Faculty of Veterinary Medicine, Kagoshima University, 1-21-24 Korimoto, Kagoshima 890-0065, Japan. Electronic address:

The responsiveness of the basilar artery to intrinsic vasoactive substances is species-specific and can be a unique characteristic. We investigated the responsiveness of the bat (Rhinolophus ferrumequinum) basilar artery to noradrenaline (NA), 5-hydroxytryptamine (5-HT), angiotensin (Ang) II, bradykinin (BK), histamine (His), and acetylcholine (ACh). NA, 5-HT, Ang II, and BK induced contraction, whereas His and ACh induced relaxation, in a concentration-dependent manner. Read More

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September 2021

Development of a Triazolobenzodiazepine-Based PET Probe for Subtype-Selective Vasopressin 1A Receptor Imaging.

Pharmacol Res 2021 Sep 15:105886. Epub 2021 Sep 15.

Department of Radiology, Division of Nuclear Medicine and Molecular Imaging Massachusetts General Hospital and Harvard Medical School, 55 Fruit Street, Boston, Massachusetts 02114, United States. Electronic address:

Objectives: To enable non-invasive real-time quantification of vasopressin 1A (V1A) receptors in peripheral organs, we sought to develop a suitable PET probe that would allow specific and selective V1A receptor imaging in vitro and in vivo.

Methods: We synthesized a high-affinity and -selectivity ligand, designated compound 17. The target structure was labeled with carbon-11 and tested for its utility as a V1A-targeted PET tracer by cell uptake studies, autoradiography, in vivo PET imaging and ex vivo biodistribution experiments. Read More

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September 2021

Blockade of adenosine A receptors inhibits Tremulous Jaw Movements as well as expression of zif-268 and GAD65 mRNAs in brain motor structures.

Behav Brain Res 2021 Sep 15:113585. Epub 2021 Sep 15.

Department of Neuropsychopharmacology, Maj Institute of Pharmacology Polish Academy of Sciences, 12 Smętna Street, 31-343, Kraków, Poland. Electronic address:

Tremor is one of the motor symptoms of Parkinson's disease (PD), present also in neuroleptic-induced parkinsonism. Tremulous jaw movements (TJMs) are suggested to be a well-validated rodent model of PD resting tremor. TJMs can be induced by typical antipsychotics and are known to be reduced by different drugs, including adenosine A2A receptor antagonists. Read More

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September 2021

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J Pharmacol Exp Ther 2021 Sep 17. Epub 2021 Sep 17.

Pharmacology and Toxicology, University Hospital Halle, Germany

In an integrative approach, we studied cardiac effects of recently published novel H receptor agonists in the heart of mice that overexpress the human H receptor (H-TG), littermate wild type control mice (WT) and in isolated electrically driven muscle preparations from patients undergoing cardiac surgery. Under our experimental conditions, the H receptor agonists UR-Po563, UR-MB-158 and UR-MB-159 increased force of contraction in left atrium from H-TG with pEC values of 8.27, 9. Read More

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September 2021

Polyphenolic Natural Products Active In Silico against SARS-CoV-2 Spike Receptor Binding Domains and Non-Structural Proteins - A Review.

Comb Chem High Throughput Screen 2021 Sep 16. Epub 2021 Sep 16.

Laboratory for Organic Reactivity, Discovery and Synthesis (LORDS), Research Center for the Natural and Applied Sciences, University of Santo Tomas, Manila, Espana Blvd., Manila 1015, Philippines.

The ongoing Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) pandemic has been proven to be more severe than the previous coronavirus outbreaks due to the virus' high transmissibility. With the emergence of new variants, this global phenomenon took on a more dramatic turn with many countries recently experiencing higher surges of confirmed cases and deaths. On top of this, the inadequacy of effective treatment options for COVID-19 aggravated the problem. Read More

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September 2021

Integrative Network-Based Analysis Reveals Gene Networks and Novel Drug Repositioning Candidates for Alzheimer Disease.

Neurol Genet 2021 Oct 9;7(5):e622. Epub 2021 Sep 9.

Translational Neurogenomics Laboratory (Z.F.G., E.M.D.), QIMR Berghofer Medical Research Institute, Brisbane, Queensland, Australia; Division of Genetic Medicine (E.R.G.), Vanderbilt Genetics Institute, Vanderbilt University Medical Center, Nashville, TN; and Cellular and Molecular Neurodegeneration (A.W.), QIMR Berghofer Medical Research Institute, Brisbane, Queensland, Australia.

Background And Objectives: To integrate genome-wide association study data with tissue-specific gene expression information to identify coexpression networks, biological pathways, and drug repositioning candidates for Alzheimer disease.

Methods: We integrated genome-wide association summary statistics for Alzheimer disease with tissue-specific gene coexpression networks from brain tissue samples in the Genotype-Tissue Expression study. We identified gene coexpression networks enriched with genetic signals for Alzheimer disease and characterized the associated networks using biological pathway analysis. Read More

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October 2021

Comparison of proton pump inhibitors and histamine 2 receptor antagonists for stress ulcer prophylaxis in the intensive care unit.

Sci Rep 2021 Sep 16;11(1):18467. Epub 2021 Sep 16.

Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Seoul National University College of Medicine, Seoul National University Bundang Hospital, 82 Gumi-ro, 173 Beon-gil, Bundang-gu, Seongnam-si, Gyeonggi-do, 13620, Republic of Korea.

Proton pump inhibitors (PPIs), followed by histamine 2 receptor antagonists (H2RAs), are the most commonly used drugs to prevent gastrointestinal bleeding in critically ill patients through stress ulcer prophylaxis. The relative efficacy and drug-related adverse events of PPIs and H2RAs remain unclear. In this retrospective, observational, comparative cohort study, PPIs and H2RAs for stress ulcer prophylaxis in critically ill patients were compared using a common data model. Read More

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September 2021

Click-to-lead design of a picomolar ABA receptor antagonist with potent activity in vivo.

Proc Natl Acad Sci U S A 2021 Sep;118(38)

Institute for Integrative Genome Biology, University of California, Riverside, CA 92521;

Abscisic acid (ABA) is a key plant hormone that mediates both plant biotic and abiotic stress responses and many other developmental processes. ABA receptor antagonists are useful for dissecting and manipulating ABA's physiological roles in vivo. We set out to design antagonists that block receptor-PP2C interactions by modifying the agonist opabactin (OP), a synthetically accessible, high-affinity scaffold. Read More

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September 2021

Effect of gastric acid suppression on Clostridioides difficile-induced diarrhea and appropriateness of gastric acid suppressors in hospitalized patients: A matched case-control study.

Arab J Gastroenterol 2021 Sep 13. Epub 2021 Sep 13.

Hacettepe University, Faculty of Pharmacy, Department of Clinical Pharmacy, P.O. Box 06100, Sıhhiye, Ankara, Turkey.

Background And Study Aims: The effects of gastric acid suppressors (GASs) on Clostridioides difficile infection remain controversial. Moreover, studies have shown that GASs are overused. This study was designed to evaluate the effects of GAS use on the risk of C. Read More

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September 2021

The Role of Orexin in Alzheimer Disease: From Sleep-wake Disturbance to Therapeutic Target.

Neurosci Lett 2021 Sep 13:136247. Epub 2021 Sep 13.

Department of Neurology, the Affiliated Hospital of Qingdao University, Qingdao, China. Electronic address:

Accumulating evidence has shown that sleep disturbance is a common symptom in Alzheimer's disease (AD), which is regarded as a modifiable risk factor for AD. Orexin is a key modulator of the sleep-wake cycle and has been found to be dysregulated in AD patients. The increased orexin in cerebrospinal fluid (CSF) is associated with decreased sleep efficiency and REM sleep, as well as cognitive impairment in AD patients. Read More

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September 2021

Scaffold Hybridization Strategy Leads to the Discovery of Dopamine D Receptor-Selective or Multitarget Bitopic Ligands Potentially Useful for Central Nervous System Disorders.

ACS Chem Neurosci 2021 Sep 16. Epub 2021 Sep 16.

School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Via S. Agostino 1, Camerino 62032, Italy.

In the search for novel bitopic compounds targeting the dopamine D receptor (DR), the -(2,3-dichlorophenyl)piperazine nucleus (primary pharmacophore) has been linked to the 6,6- or 5,5-diphenyl-1,4-dioxane-2-carboxamide or the 1,4-benzodioxane-2-carboxamide scaffold (secondary pharmacophore) by an unsubstituted or 3-F-/3-OH-substituted butyl chain. This scaffold hybridization strategy led to the discovery of potent DR-selective or multitarget ligands potentially useful for central nervous system disorders. In particular, the 6,6-diphenyl-1,4-dioxane derivative showed a DR-preferential profile, while an interesting multitarget behavior has been highlighted for the 5,5-diphenyl-1,4-dioxane and 1,4-benzodioxane derivatives and , respectively, which displayed potent DR antagonism, 5-HTR and DR agonism, as well as potent DR partial agonism. Read More

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September 2021

Treatment of pulmonary arterial hypertension in children.

Cardiovasc Diagn Ther 2021 Aug;11(4):1144-1159

Department of Pediatric Cardiology and Congenital Heart Diseases, Centre of Child and Adolescent Health, University Hospital Heidelberg, Heidelberg, Germany.

Pulmonary arterial hypertension (PAH) is a devastating illness causing already significant morbidity in childhood. Currently approved treatment options for children comprise the endothelin receptor antagonist bosentan, as well as the phosphodiesterase-5 inhibitor sildenafil. But PAH treatment has advanced significantly over the past decade, and new classes of targeted drug therapies, such as stimulators of the soluble guanylate cyclase (riociguat) or prostacyclin receptor agonists (selexipag), are currently evaluated regarding their efficacy and safety in children, in order to limit off-label use. Read More

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Losartan and Eprosartan Induce a Similar Effect on the Acute Rise in Serum Uric Acid Concentration after an Oral Fructose Load in Patients with Metabolic Syndrome.

J Renin Angiotensin Aldosterone Syst 2021 25;2021:2214978. Epub 2021 Aug 25.

Department of Nephrology, Hypertension and Kidney Transplantation, Medical University of Lodz, Central University Hospital, Lodz, Poland.

Introduction: Excessive intake of fructose increases serum uric acid concentration. Hyperuricemia induces a negative effect on atherosclerosis and inflammation. Hyperuricemia is common in patients with arterial hypertension. Read More

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Dopamine D1 and D2 Receptors Are Important for Learning About Neutral-Valence Relationships in Sensory Preconditioning.

Front Behav Neurosci 2021 30;15:740992. Epub 2021 Aug 30.

School of Psychology, UNSW Sydney, Sydney, NSW, Australia.

Dopamine neurotransmission has been ascribed multiple functions with respect to both motivational and associative processes in reward-based learning, though these have proven difficult to tease apart. In order to better describe the role of dopamine in associative learning, this series of experiments examined the potential of dopamine D1- and D2-receptor antagonism (or combined antagonism) to influence the ability of rats to learn neutral valence stimulus-stimulus associations. Using a sensory preconditioning task, rats were first exposed to pairings of two neutral stimuli (S2-S1). Read More

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An Evidence-Based Review of OLZ/SAM for Treatment of Adults with Schizophrenia or Bipolar I Disorder.

Neuropsychiatr Dis Treat 2021 9;17:2885-2904. Epub 2021 Sep 9.

Alkermes Pharma Ireland Limited, Dublin, Ireland.

Olanzapine effectively treats schizophrenia and bipolar I disorder (BD-I); however, its use is limited by the risk of significant weight gain and metabolic effects. OLZ/SAM, a combination of olanzapine and samidorphan, was recently approved in the United States for the treatment of adults with schizophrenia or BD-I. OLZ/SAM provides the efficacy of olanzapine while mitigating olanzapine-associated weight gain through opioid-receptor blockade. Read More

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September 2021

Neoadjuvant hormonal therapy before radical prostatectomy in high-risk prostate cancer.

Nat Rev Urol 2021 Sep 15. Epub 2021 Sep 15.

Department of Urology, University Hospitals Leuven, Leuven, Belgium.

Patients with high-risk prostate cancer treated with curative intent are at an increased risk of biochemical recurrence, metastatic progression and cancer-related death compared with patients treated for low-risk or intermediate-risk disease. Thus, these patients often need multimodal therapy to achieve complete disease control. Over the past two decades, multiple studies on the use of neoadjuvant treatment have been performed using conventional androgen deprivation therapy, which comprises luteinizing hormone-releasing hormone agonists or antagonists and/or first-line anti-androgens. Read More

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September 2021

Chemerin regulates normal angiogenesis and hypoxia-driven neovascularization.

Angiogenesis 2021 Sep 15. Epub 2021 Sep 15.

WELBIO and I.R.I.B.H.M, Université Libre de Bruxelles, Campus Erasme, 808 route de Lennik, B-1070, Brussels, Belgium.

Chemerin is a multifunctional protein initially characterized in our laboratory as a chemoattractant factor for leukocyte populations. Its main functional receptor is CMKLR1. We identified previously chemerin as an anti-tumoral factor inhibiting the vascularization of tumor grafts. Read More

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September 2021

Delayed circadian rhythms and substance abuse: dopamine transmission's time has come.

J Clin Invest 2021 Sep;131(18)

Disrupted sleep and circadian rhythms are linked with substance abuse risk. Human studies that investigate relationships between sleep, circadian rhythm, and substance use reward generally rely on indirect means to infer dopaminergic function, such as functional magnetic resonance imaging. In this issue of the JCI, Zhang and colleagues used positron emission tomography (PET) to image striatal dopamine D1 (D1R) and D2/3 receptor (D/3R) availability in healthy adults. Read More

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September 2021

Endothelial Mineralocorticoid Receptor Ablation Confers Protection Towards Endothelial Dysfunction in Experimental Diabetes in Mice.

Acta Physiol (Oxf) 2021 Sep 14:e13731. Epub 2021 Sep 14.

Department of Cardiovascular and Renal Research, Institute of Molecular Medicine, University of Southern Denmark, Odense C, Denmark.

Aim: With diabetes comes significant risk of macrovascular and microvascular complications. Circulating aldosterone levels increase in patients with diabetes. Aldosterone can directly affect vascular function via activation of the mineralocorticoid receptor (MR). Read More

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September 2021

Subtype-Dependent Co-receptor Tropism in Cuban HIV-1-Infected Patients: Implications for Maraviroc Treatment.

MEDICC Rev 2021 Jul-Oct;23(3-4):29-36. Epub 2021 Aug 22.

Virology Department, Pedro Kourí Tropical Medicine Institute (IPK), Havana, Cuba.

Introduction: Unlike most high-income countries where subtype B viruses predominate, the Cuban HIV-1 epidemic is characterized by a great diversity of subtypes and circulating recombinant forms. Some studies have shown that HIV variants exhibiting a preference for the CXCR4 co-receptor (X4-tropic) could have impacts on disease pathogenesis, with clinical implications for antiviral treatment plans. Determination of HIV co-receptor tropism is crucial for clinicians in deciding whether maraviroc is an appropriate antiviral. Read More

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Potential Mechanisms Underlying Marijuana-Associated Periodontal Tissue Destruction.

J Dent Res 2021 Sep 13:220345211036072. Epub 2021 Sep 13.

Molecular Pathobiology, College of Dentistry, New York University, New York, USA.

While definitive evidence awaits, cannabis is emerging as a likely risk factor for periodontal tissue destruction. The mechanisms that underlie potential cannabis-induced or cannabis-enhanced periodontal diseases, however, remain to be elucidated. Herein, we 1) examine insights obtained from the endocannabinoid system, 2) summarize animal models of exposure to cannabinoid receptor agonists and antagonists, 3) review the evidence suggesting that cannabis and cannabis-derived molecules exert a profound influence on components of the oral microbiome, and 4) assess studies indicating that marijuana and phytocannabinoids compromise the immune response to plaque. Read More

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September 2021

Neurokinin 3 Receptor Antagonists Compared With Serotonin Norepinephrine Reuptake Inhibitors for Non-Hormonal Treatment of Menopausal Hot Flushes: A Systematic Qualitative Review.

Adv Ther 2021 Sep 12. Epub 2021 Sep 12.

School of Medicine, University of St Andrews, Medical and Biological Sciences Building, North Haugh, St Andrews, KY16 9TF, UK.

Introduction: Hot flushes/flashes (HFs) or other vasomotor symptoms affect between 45 and 97% of women during menopause. Hormone replacement therapy (HRT) is effective at alleviating menopausal symptoms, but some women cannot or prefer not to take HRT. Since current non-hormonal options have suboptimal efficacy/tolerability, there is a pressing need for an effective, well-tolerated alternative. Read More

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September 2021

A Review on Newer Ocular Drug Delivery Systems with an Emphasis on Glaucoma.

Adv Pharm Bull 2021 May 19;11(3):399-413. Epub 2020 Sep 19.

Amrita School of Pharmacy, Amrita Institute of Medical Science & Research Centre, Amrita Vishwa Vidyapeetham, Kochi-682041, India.

Glaucoma is an irreversible condition resulting from the increase in intraocular pressure (IOP); which leads to permanent loss of vision with the destruction of retinal ganglion cells (RGCs). The IOP elevations are controlled in normal by the physiological flow of aqueous humour. A population with age above 40 is more susceptible to glaucoma. Read More

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Gender Disparities in Anti-dementia Medication Use among Older Adults: Health Equity Considerations and Management of Alzheimer's Disease and Related Dementias.

Front Pharmacol 2021 25;12:706762. Epub 2021 Aug 25.

Department of Pharmaceutical and Administrative Sciences, Presbyterian College School of Pharmacy, Clinton, SC, United States.

The prevalence of Alzheimer's disease and related dementias (ADRD) in women is higher than men. However, the knowledge of gender disparity in ADRD treatment is limited. Therefore, this study aimed to determine the gender disparities in the receipt of anti-dementia medications among Medicare beneficiaries with ADRD in the U. Read More

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Recent Insights into the Management of Inflammation in Asthma.

J Inflamm Res 2021 2;14:4371-4397. Epub 2021 Sep 2.

Department of Respiratory Medicine, University Hospitals Southampton NHS Foundation Trust, Southampton, UK.

The present prevailing inflammatory paradigm in asthma is of T2-high inflammation orchestrated by key inflammatory cells like Type 2 helper lymphocytes, innate lymphoid cells group 2 and associated cytokines. Eosinophils are key components of this T2 inflammatory pathway and have become key therapeutic targets. Real-world evidence on the predominant T2-high nature of severe asthma is emerging. Read More

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September 2021

Cannabinoids for the treatment of refractory neuropathic pruritus in amyotrophic lateral sclerosis: A case report.

Palliat Med 2021 Sep 11:2692163211045314. Epub 2021 Sep 11.

Palliative Medicine, The University of British Columbia, Vancouver, BC, Canada.

Background: Neuropathic symptoms have a wide variety of manifestations, ranging from pain to pruritus. Neuropathic pruritus is a type of chronic pruritus related to damaged small fibers. Cannabinoids have evidence to manage neuropathic symptoms. Read More

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September 2021

Benzothiophene derivatives as selective estrogen receptor covalent antagonists: Design, synthesis and anti-ERα activities.

Bioorg Med Chem 2021 Sep 6;47:116395. Epub 2021 Sep 6.

State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China. Electronic address:

Estrogen receptor α emerged as a well validated therapeutic target of breast cancer for decades. However, approximately 50% of patients who initially responding to standard-of-care (SoC), such as undergo therapy of Tamoxifen, generally inevitably progress to an endocrine-resistance ER+ phenotype. Recently, selective estrogen receptor covalent antagonists (SERCAs) targeted to ERα have been demonstrated as a therapeutic alternative. Read More

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September 2021