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178 articles for “receptors”
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Efficacy of Combination Therapy with Osimertinib and Afatinib in epidermal growth factor receptor-mutant non-small-cell lung cancer Patients
Abstract: Treatment options for patients with non-small-cell lung cancer who have epidermal growth factor receptor mutations are constrained by the emergence of resistance to epidermal growth factor receptor tyrosine kinase inhibitors. Osimertinib or afatinib alone, when tested in a laboratory model, led to the formation of drug-resistant clones harboring epidermal growth factor receptor secondary mutations. However, combining these drugs prevented the emergence of such mutations. In a Phase II clinical trial, …
Published in Research and Reviews: Journal of Oncology and Hematology · Vol. 13, Issue 1, 2024 · pp. 13–24 Read article
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Synthesis and Evaluation of Novel Peroxisome Proliferator Activated Receptor-γ (PPAR-γ) Agonists for the Treatment of Diabetes
Abstract: A series of novel thiazolidinedione derivatives as peroxisome proliferator activated receptor-gamma (PPAR-gamma) agonists bearing different fatty acid esters and amides as substituents in the positions 3 and 4 of the benzylidene moiety have been designed, synthesized and tested as potential antihyperglycemic agents. The compounds containing stearic acid (A1TU, A2TU, A3TU, A2TS and A3TS) exhibited the maximum activity (64.7-70.3 % BG reduction) among all the synthesized compounds. The capric acid containing …
Published in Research and Reviews: A Journal of Toxicology · Vol. 6, Issue 2, 2016 · pp. 1–12 Read article
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Deciphering the Roles of Estrogen Receptors and 27-Hydroxycholesterol in BC Progression
Abstract: Breast cancer (BC) ranks among the top causes of cancer-related deaths in women worldwide. Many risk factors of BC are linked to estrogen. Experiments of Beatson in 1896 show the role of steroid hormones as major determinant in BC. Action of steroid hormones is mediated by their receptors including Estrogen receptors (ERs). ERs are part of a subfamily of ligand-regulated transcription factors. Their primary role is to translate hormone signals …
Published in International Journal of Genetic Modifications and Recombinations · Vol. 2, Issue 2, 2024 · pp. 18–26 Read article
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The Relationship Between LOH Severity and Androgen Receptor Gene CAG Repeat Length of Korean Men Affected with LOH
Abstract: Context: There have been no investigations on the severity of late-onset hypogonadism (LOH) of Korean male according to their androgen receptor gene CAG repeat length. Aim: To investigate the relationship between late-onset hypogonadism (LOH) and androgen receptor gene CAG repeat length in Korean men. A total of 106 patients with LOH from Pyongyang City participated in this study. LOH was diagnosed in individuals who had a serum testosterone level below …
Published in Research and Reviews: A Journal of Medicine · Vol. 15, Issue 1, 2025 · pp. 32–37 Read article
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Protease activated receptor-2 as an imperative target in nociceptive responses: A minireview
Abstract: PARs (protease-activated receptors) are a family of seven-transmembrane G-protein coupled receptor for proteases from circulation, inflammatory cells and endothelial tissues. To date, four members of PAR family have been cloned, namely PAR1 to PAR4. This minireview focuses on role of PAR2 receptor in inflammatory and nociceptive processes. Numerous studies documented for activation of PAR2 receptors through several proteases suggests its role in pain and inflammation. However, mechanism of PAR2 underlying …
Published in Research and Reviews: A Journal of Pharmacology · Vol. 1, Issue 1, 2011 · pp. 8–13 Read article
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In- silico Design of Novel Inhibitors for 5-HT2A Receptor to Recuperate Schizophrenia
Abstract: Schizophrenia is a mental disorder characterized by positive symptoms such as disorganized speech, delusions and hallucinations and negative symptoms such as deficits of attention, affective flattening and social withdrawal in nature. There are several receptor involve in schizophrenia, one of these 5-HT2A receptor i.e. serotonin receptor. The serotonin receptor 5-HT2A has been involved in several neurological conditions and potent 5-HT2A inhibitors have therapeutic effects that use for the treatment of …
Published in Research & Reviews: A Journal of Bioinformatics · Vol. 2, Issue 2, 2015 · pp. 11–17 Read article
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Computational Molecular Docking Studies to Design Novel 2, 3-Substituted-1-(4-(Piperidin-1-yl) butyl)-1H- indol-5-ol Derivatives for Estrogen Receptor Alfa in AF-2 Domain
Abstract: The present manuscript describes the designing of novel 2, 3-Substituted-1-(4-(Piperidin-1-yl) butyl)- 1H-indol-5-ol derivatives as specific estrogen receptor alfa modulators and their screening by docking studies to determine the binding interaction for the best-fit conformations in the binding site of the ERα receptor. Based on the results of docking studies, the selected ligands reveal the all- important functional groups of the ligands that interact with active amino acid residues in the …
Published in Research and Reviews: A Journal of Pharmaceutical Science · Vol. 12, Issue 3, 2025 · pp. 15–49 Read article
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Molecular Docking studies of Benzodiazepine Derivatives With GABA(B) Receptor
Abstract: Benzodiazepines (BZDs) are pharmacologically significant compounds that act by binding to GABA A neurotransmitter receptors, subsequently augmenting GABA-induced chloride ion flux, consequently inducing neuronal hyperpolarization. Benzodiazepines are commonly used in the treatment of sleep disorders, anxiety, muscle spasms, seizure disorders, and some forms of depression. The primary inhibitory neurotransmitter, GABA, functions on two types of receptors: the ligand-gated GABA A/C receptors and the G protein-coupled GABA B receptors. These neurotransmitters …
Published in International Journal of Toxins and Toxics · Vol. 1, Issue 2, 2024 · pp. 1–14 Read article
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Role of Gastric Receptors in Gastrointestinal Disorder
Abstract: The established and potential roles of cholecystokinin1 and cholecystokinin2 receptors in gastrointestinal and metabolic diseases are analyzed, along with findings from human studies involving agonists and antagonists. While there is considerable evidence implicating cholecystokinin1R in various diseases such as pancreatic disorders, motility disorders, tumor growth, satiety regulation, and cholecystokinin-deficient states, its specific role in these conditions remains ambiguous. Conversely, the role of cholecystokinin2R in physiological (e.g., atrophic gastritis) and pathological …
Published in International Journal of Biomedical Innovations and Engineering · Vol. 2, Issue 2, 2024 · pp. 37–49 Read article
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Molecular Docking Analysis of Berberis aristata Phytocompounds as Potential Growth Factor Receptor Blockers in Cancer Therapy
Abstract: Middle-aged and older women are susceptible to breast cancer (BC), a potentially fatal condition. When breast cancer is diagnosed, the median age is 62. Breast cancer diagnoses in women under 45 are comparatively uncommon, whereas the bulk of breast cancer diagnoses occur in women 62 and older. Growth factor receptors are interesting therapeutic targets because of their critical role in the pathophysiology of cancer. Vascular endothelial growth factor receptors (VEGFR-2) …
Published in International Journal of Cell Biology and Cellular Functions · Vol. 3, Issue 2, 2025 · pp. 1–10 Read article
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Molecular Docking Studies of Nyctanthes arbor-tristis Phytochemicals for Targeting TNF Receptor in Arthritis
Abstract: Rheumatoid Arthritis is an autoimmune disorder which results in inflammation. Tumor necrosis factor-alpha (TNF-α) is responsible for the progression of inflammatory arthritis by promoting immune cell activation and cytokine release. The present study explores the potential of bioactive compounds derived from Nyctanthes arbor-tristis (Parijat) in modulating TNF receptor activity through molecular docking. Computational methods were employed to evaluate the binding affinity of selected phytocompounds from N. arbor-tristis against the extracellular …
Published in International Journal of Cell Biology and Cellular Functions · Vol. 3, Issue 2, 2025 · pp. 11–21 Read article
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GLP-1 Receptor Agonists: A Dual Therapeutic Strategy for the Management of Type 2 Diabetes Mellitus and Obesity
Abstract: For the treatment of obesity and type 2 diabetes mellitus (T2DM), glucagon-like peptide-1 receptor agonists (GLP-1 RAs) have become a revolutionary class of pharmaceutical drugs. These drugs were first created as glucose-lowering treatments, but they have now shown other advantages, such as notable weight loss, better cardiovascular results, and general metabolic control. The objective of this narrative review is to assess the pharmacological mechanisms, clinical efficacy, safety profile, and therapeutic …
Published in Research and Reviews: A Journal of Pharmacology · Vol. 16, Issue 1, 2026 · pp. 69–75 Read article
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Molecular Dynamics and Therapeutic Architectures of Cannabinoid Receptors: A Comprehensive Review
Abstract: Expanding on these foundations, recent structural biology studies using cryo-electron microscopy have provided high-resolution insights into the conformational dynamics of CB₁ and CB₂ receptors. These findings have enabled a more precise understanding of ligand–receptor interactions, particularly how agonists, antagonists, and reverse agonists stabilize distinct receptor states. Such knowledge is critical for rational drug design, allowing researchers to selectively modulate downstream signaling pathways. For instance, CB₁ receptors primarily couple to Gi/o …
Published in International Journal of Cheminformatics · Vol. 4, Issue 1, 2026 · pp. 36–40 Read article
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A Review on the Clinical and Pathological Significance of Prorenin Receptor [(P)RR]
Abstract: The (pro)renin receptor (P)RR discovery, which is a novel constituent of Renin Angiotensin-Aldosteron System (RAS) has brought renin and (pro)renin back into spotlight. The (P)RR binds both renin and its inactive precursor (pro)renin, this binding triggers a cascade of intracellular signalling that eventually leads to upregulation of the expression of profibrotic genes, potentially leading to pathogenesis of cardiac and renal fibrosis, growth and remodelling. Clinically, it is also seen that …
Published in Research and Reviews: A Journal of Pharmacology · Vol. 5, Issue 2, 2015 · pp. 11–17 Read article
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Modulation of Receptor Proteins: A Recent Paradigm in Drug Discovery and Target
Abstract: The main aim in drug discovery is to design different ligands those work on specific drug targets. However, various effective drugs work through the modulation of many proteins than single target. Advancement in system biology are establishing a phenotypic strength and a network structure, which suggests that, the excellent selective compounds may be performed less than desired clinical efficacy in comparison to multi-target drugs. In this new appreciation of the …
Published in Research & Reviews: A Journal of Drug Design & Discovery · Vol. 5, Issue 1, 2018 · pp. 14–24 Read article
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Virtual Screening of Novel 2-substituted -5-hydroxy-1- (2-methyl-3-morpholinopropyl)-1H-indole-3- carboxamide Derivatives for Estrogen Receptor alpha in AF-2 domain for effective Anticancer Treatment
Abstract: Present manuscript describes designing of novel 2-substituted -5-hydroxy-1-(2-methyl-3- morpholinopropyl)-1H-indole-3-carboxamide derivatives as specific ERα modulators, discuss the selection criteria for 1ERR, several interactions between the ligand and the amino acid residues that would probably elicit fruitful modulation of the receptor. Accordingly, a ligand was observed to yield Gscore of -10.016 which was found comparable with the standard ligand Raloxifene (-11.869). The present work has been designed to discover some novel 2-substituted …
Published in Research and Reviews: A Journal of Pharmaceutical Science · Vol. 12, Issue 2, 2025 · pp. 31–55 Read article
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Therapeutic Potential of Plant-Derived Phytochemicals in Targeting Receptor Pathways Related to Non-Enzymatic Glycation: A Meta-Analysis
Abstract: Background: Non-enzymatic glycation, where reducing sugars react with proteins, lipids, and nucleic acids, contributes to various pathological conditions, such as diabetic complications and cardiovascular diseases. This process is facilitated by the receptor for advanced glycation end-products (RAGE), which is pivotal in driving inflammation and causing tissue damage. Objective: This meta-analysis evaluates the effects of plant-derived phytochemicals on RAGE expression and associated signaling pathways, assessing their therapeutic potential in glycation-related diseases. …
Published in International Journal of Cell Biology and Cellular Functions · Vol. 3, Issue 1, 2025 · pp. 60–73 Read article
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Molecular Docking of Abroma augusta Phytocompounds Against Estrogen Receptor Alpha (Er-Α) for the Treatment of Menstrual Disorders
Abstract: Menstrual disorders, including dysmenorrhea (painful menstruation), amenorrhea (absence of menstruation), and irregular menstrual cycles, significantly impact women’s reproductive health and overall well-being. These conditions often arise from hormonal imbalances, inflammation, and uterine dysfunction, necessitating effective therapeutic interventions. Current treatments, such as hormonal therapies (oral contraceptives, progestin-only pills), NSAIDs, and surgical procedures (endometrial ablation, hysterectomy), provide relief but often target symptoms rather than addressing the underlying causes. Consequently, there is a …
Published in International Journal of Molecular Biotechnological Research · Vol. 3, Issue 2, 2025 · pp. 1–12 Read article
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A Review of the Cardioprotective Effects of Plant Derived and Synthetic Derivatives Targeting the Cannabinoid Receptors
Abstract: Cannabinoids are chemicals that were discovered in the Cannabis sativa plant for the first time. They've been used to treat a variety of ailments for thousands of years. The endocannabinoid system is made up of cannabinoid receptors, endocannabinoids, and the enzymes that catalyse their synthesis and breakdown. It plays a vital role in cardiovascular system function. The findings so far point to endocannabinoids playing a role in the pathogenesis of …
Published in Trends in Drug Delivery · Vol. 9, Issue 1, 2022 · pp. 21–38 Read article
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Metabotropic Receptor Based Target for Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus
Abstract: G protein coupled receptors (GPCRs) moreover called as metabotropic receptor addresses the greatest gathering of film proteins in the human genome. GPCRs share a regular essential characteristic of seven hydrophobic transmembrane (TM) sections (heptahelical structure), with an extracellular amino end and an intracellular carboxyl end their assistant and valuable closeness of GPCRs stays rather than the fundamental OK assortment of the ordinary GPCR ligands. GPCRs keep on being critical revelation …
Published in Trends in Drug Delivery · Vol. 5, Issue 1, 2018 · pp. 17–27 Read article