Steroid Recognition in Adhesion <scp>GPCRs</scp> : A Structural and Pharmacological Perspective

Emerging evidence suggests steroids may act as generalizable ligands for adhesion GPCRs, a receptor class with considerable pharmacological potential. While most studies have focused on the ADGR'G' subfamily, recent cryo-EM structures of the androgens 5α-dihydrotestosterone (5α-DHT) and methenolone bound to ADGRD1 revealed a putative steroid-binding pocket and enabled the rational design of a selective synthetic agonist. This perspective considers the broader significance of these findings amid some debate about the reproducibility and physiological relevance of steroid binding to adhesion GPCRs, reviewing all structural evidence and presenting comparative docking and homology modeling to evaluate conserved features and the plausibility of a shared recognition mechanism.

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Publication Details

Journal
Pharmacology Research & Perspectives
Published
2026-02-16
DOI
https://doi.org/10.1002/prp2.70221
Primary Topic
Receptor Mechanisms and Signaling
Type
article
Field-Weighted Citation Impact
0.00
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article

Steroid Recognition in Adhesion GPCRs : A Structural and Pharmacological Perspective

Bethany Fleming, Abdul‐Akim Guseinov, Nicole A. Perry‐Hauser, Irina G. Tikhonova et al.
Pharmacology Research & Perspectives
Receptor Mechanisms and Signaling
article

Steroid Recognition in Adhesion GPCRs : A Structural and Pharmacological Perspective

Bethany Fleming, Abdul‐Akim Guseinov, Nicole A. Perry‐Hauser, Irina G. Tikhonova, Graeme Milligan
article en

Abstract

Emerging evidence suggests steroids may act as generalizable ligands for adhesion GPCRs, a receptor class with considerable pharmacological potential. While most studies have focused on the ADGR'G' subfamily, recent cryo-EM structures of the androgens 5α-dihydrotestosterone (5α-DHT) and methenolone bound to ADGRD1 revealed a putative steroid-binding pocket and enabled the rational design of a selective synthetic agonist. This perspective considers the broader significance of these findings amid some debate about the reproducibility and physiological relevance of steroid binding to adhesion GPCRs, reviewing all structural evidence and presenting comparative docking and homology modeling to evaluate conserved features and the plausibility of a shared recognition mechanism.

Pharmacology Research & PerspectivesVol. 14(2)
Belfast Metropolitan College (GB), University of Glasgow (GB)
Openalex Percentile: Top 54%
Receptor Mechanisms and Signaling
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