Last update 01 Nov 2024

SRD5A1

Last update 01 Nov 2024

Basic Info

Synonyms

3-oxo-5-alpha-steroid 4-dehydrogenase 1, S5AR 1, SR type 1

+ [4]

Introduction

Converts testosterone into 5-alpha-dihydrotestosterone and progesterone or corticosterone into their corresponding 5-alpha-3-oxosteroids. It plays a central role in sexual differentiation and androgen physiology.

Drugs associated with SRD5A1

MK-386

Target

SRD5A1

Mechanism

SRD5A1 inhibitors

Active Org.

Merck & Co., Inc.

Originator Org.

Merck & Co., Inc.

Active Indication-

Inactive Indication

Acne Vulgaris [+3]

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Compound 4(Chulalongkorn University)

Target

SRD5A1

Mechanism

SRD5A1 modulators

Active Org.

Ewha Womans University

Originator Org.

University of Chulalongkorn

Active Indication

Chemical and Drug Induced Liver Injury

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

XNA-2

Target

SRD5A1 x SRD5A2

Mechanism

SRD5A1 inhibitors [+1]

Active Org.-

Originator Org.

Xenna Corp.

Active Indication-

Inactive Indication

Neoplasms

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with SRD5A1

100 Translational Medicine associated with SRD5A1

0 Patents (Medical) associated with SRD5A1

558

Literatures (Medical) associated with SRD5A1

31 Dec 2024·Systems Biology in Reproductive Medicine

Identification of potential differences in salivary proteomic profiles between estrus and diestrus stage of estrous cycle in dairy cows

Article

Author: Manimaran, Ayyasamy ; Sinha, Manish Kumar ; Patil, Shivanagouda ; Nag, Pradeep ; Ramesha, Kerekoppa ; Kumaresan, Arumugam ; Jeyakumar, Sakthivel ; Shaji, Arsha ; Gowdar Veerappa, Vedamurthy

In the present study, a comparative global high-throughput proteomic analysis strategy was used to identify proteomic differences between estrus and diestrus stage of estrous cycle in dairy cows. Saliva was collected from cows during estrus and diestrus, and subjected to LC-MS/MS-based proteomic analysis. A total of 2842 proteins were detected in the saliva of cows, out of which, 2437 and 1428 non-redundant proteins were identified in estrous and diestrous saliva, respectively. Further, it was found that 1414 and 405 salivary proteins were specific to estrus and diestrus, respectively while 1023 proteins were common to both groups. Among the significantly dysregulated proteins, the expression of 56 proteins was down-regulated (abundance ratio <0.5) while 40 proteins were up-regulated (abundance ratio > 2) in estrous compared to diestrous saliva. The proteins, such as HSD17B12, INHBA, HSP70, ENO1, SRD5A1, MOS, AMH, ECE2, PDGFA, OPRK1, SYN1, CCNC, PLIN5, CETN1, AKR1C4, NMNAT1, CYP2E1, and CYP19A1 were detected only in the saliva samples derived from estrous cows. Considerable number of proteins detected in the saliva of estrous cows were found to be involved in metabolic pathway, PI3K-Akt signaling pathway, toll-like receptor signaling pathway, steroid biosynthesis pathway, insulin signaling pathway, calcium signaling pathway, estrogen signaling pathway, oxytocin signaling pathway, TGF-β signaling pathway and oocyte meiosis. On the other hand, proteins detected in saliva of diestrous cows were involved mainly in metabolic pathway. Collectively, these data provide preliminary evidence of a potential difference in salivary proteins at different stages of estrous cycle in dairy cows.

01 Dec 2024·Comparative Biochemistry and Physiology Part A: Molecular & Integrative Physiology

Evaluation of stress in farmed Atlantic salmon (Salmo salar) using different biological matrices

Article

Author: Gorissen, Marnix ; Keihani, Rouzbeh ; Balseiro, Pablo ; Arukwe, Augustine ; Gomes, Ana S ; Handeland, Sigurd O ; Handeland, Sigurd O. ; Gomes, Ana S.

Atlantic salmon were subjected to an acute crowding scenario, and their subsequent stress responses were observed under three distinct swimming speed/water flow (WF) conditions: 0.5, 1, and 1.5 body lengths per second (BL/s). Feces, dermal mucus, and plasma were collected for analysis at 1, 6, and 24 h (h) post-stress. Additionally, the head kidney and two regions of the brain (pituitary and POA) were collected for transcript expression analysis. Fish swimming at 0.5 BL/s exhibited higher pre-stress (baseline) cortisol levels. Across all groups and matrices, the highest cortisol/cortisol metabolites (CM) levels were observed at the 1 h post-stress sampling point. At 6 h (second sampling time point), a clear decline toward baseline levels were observe in all groups. Significant increases in mean plasma glucose levels were observed at 1 h post-stress for all groups. The mean plasma lactate levels varied based on WF treatments, with a significant increase observed at 1 h only for the 1.5 BL/s group. Additionally, significant decreases in mean plasma lactate were noted at 6 and 24 h post-stress for some groups. The mRNA abundances of the tested genes (star, cyp17a1, hsd11β2, srd5a1) increased following the stress events. These changes were not uniform across all groups and were tissue dependent. In summary, the results indicate that mucus and feces can be used as potentially less invasive matrices than blood for evaluating stress and, consequently, the welfare of Atlantic salmon in captivity.

01 Dec 2024·Journal of Hazardous Materials

Paraben preservatives exhibit inhibition on human and rat steroid 5α-reductase 1: A comprehensive 3D-QSAR and computational analysis

Article

Author: Ding, Chentao ; Tang, Yunbing ; Ge, Ren-Shan ; Ji, Zhongyao ; Li, Huitao ; Wang, Shaowei ; Zheng, Jingyi ; Zhu, He ; Ge, Ren-shan ; Zhu, Yang

Parabens are preservatives used in personal care products, cosmetics, and pharmaceuticals. Steroid 5α-reductase 1 (SRD5A1) catalyzes the conversion of testosterone to dihydrotestosterone and is present in the brain, contributing to neurosteroid production. This study aimed to assess the effects of nine paraben preservatives on SRD5A1 in human SF126 glioblastoma cell and rat brain microsomes, particularly focusing on dihydrotestosterone production in SF126 cells. The results showed that methyl, ethyl, propyl, butyl, hexyl, heptyl, nonyl, phenyl, and benzyl paraben inhibited human SRD5A1, with nonylparaben having the strongest effect (7.59 μM). Additionally, kinetic analysis indicated that parabens acted as mixed/noncompetitive inhibitors, leading to a significant decrease in dihydrotestosterone production in SF126 cells. While rat SRD5A1 exhibited lower sensitivity to parabens, docking analysis revealed that parabens bind to the NADPH-binding site of both human and rat SRD5A1. In conclusion, these results highlight the inhibitory effects of paraben preservatives on SRD5A1 and elucidate their binding mechanisms, underscoring their role in hormone production.

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SRD5A1

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