Selective androgen receptor modulators in drug discovery: medicinal chemistry and therapeutic potential.

Curr Top Med Chem

GlaxoSmithKline Inc, Metabolic and Viral Diseases Drug Discovery, Research Triangle Park, PO Box 13398, NC 27705, USA.

Published: June 2006

Modulation of the androgen receptor has the potential to be an effective treatment for hypogonadism, andropause, and associated conditions such as sarcopenia, osteoporosis, benign prostatic hyperplasia, and sexual dysfunction. Side effects associated with classical anabolic steroid treatments have driven the quest for drugs that demonstrate improved therapeutic profiles. Novel, non-steroidal compounds that show tissue selective activity and improved pharmacokinetic properties have been developed. This review provides an overview of current advances in the development of selective androgen receptor modulators (SARMs).

Download full-text PDF

Source
http://dx.doi.org/10.2174/156802606776173456DOI Listing

Publication Analysis

Top Keywords

androgen receptor
12
selective androgen
8
receptor modulators
8
modulators drug
4
drug discovery
4
discovery medicinal
4
medicinal chemistry
4
chemistry therapeutic
4
therapeutic potential
4
potential modulation
4

Similar Publications

Genomic biomarkers of survival in patients with metastatic hormone-sensitive prostate cancer undergoing intensified androgen deprivation therapy.

Prostate Cancer Prostatic Dis

January 2025

Division of Medical Oncology, Department of Internal Medicine, Huntsman Cancer Institute, University of Utah, Salt Lake City, UT, USA.

Introduction: Androgen deprivation therapy intensification (ADTi) with androgen receptor pathway inhibitors (ARPI), docetaxel or both has been shown to improve survival outcomes in patients with metastatic hormone-sensitive prostate cancer (mHSPC). Currently, baseline tumor genomic markers have no role in clinical decision-making in patients with mHSPC.

Methods: In this IRB-approved retrospective study, patients diagnosed with mHSPC who underwent comprehensive genomic profiling from primary tissue or metastatic sites and treated with ADTi were included.

View Article and Find Full Text PDF

Diabetes is a detriment to male reproductive health, notably through its capacity to diminish secretion from accessory glands such as the seminal vesicles and prostate, which are crucial for reproductive function. Curcumin, a naturally derived polyphenol renowned for its anti-inflammatory and antioxidative attributes, has demonstrated potential in mitigating tissue damage across various organs in diabetic patients. Despite its established benefits, the specific impact of curcumin on seminal vesicle damage in the context of diabetes remains underexplored.

View Article and Find Full Text PDF

Identification, structure, and agonist design of an androgen membrane receptor.

Cell

January 2025

Key Laboratory Experimental Teratology of the Ministry of Education, New Cornerstone Science Laboratory, Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, and Advanced Medical Research Institute, NHC Key Laboratory of Otorhinolaryngology, Qilu hospital, Cheeloo College of Medicine, Shandong University, Jinan 250012, China; Department of Physiology and Pathophysiology, School of Basic Medical Sciences, State Key Laboratory of Vascular Homeostasis and Remodeling, Beijing Key Laboratory of Cardiovascular Receptors Research, Peking University, Beijing 100191, China. Electronic address:

Androgens, such as 5α-dihydrotestosterone (5α-DHT), regulate numerous functions by binding to nuclear androgen receptors (ARs) and potential unknown membrane receptors. Here, we report that the androgen 5α-DHT activates membrane receptor GPR133 in muscle cells, thereby increasing intracellular cyclic AMP (cAMP) levels and enhancing muscle strength. Further cryoelectron microscopy (cryo-EM) structural analysis of GPR133-Gs in complex with 5α-DHT or its derivative methenolone (MET) reveals the structural basis for androgen recognition.

View Article and Find Full Text PDF

Background: Metastatic castration-resistant prostate cancer (mCRPC) treatment is advancing yet Nordic, real-world evidence for its use is scarce. In this population-based cohort study, we describe characteristics of patients with mCRPC, and their treatment patterns and survival outcomes in Finland.

Methods: Incident patients with mCRPC diagnosed during 2013-2021 were identified from data lakes in two large and representative, Finnish hospital districts, and linked to data on drug purchases and causes of death from national registries.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!