Delving into the Latest Updates on GA-32 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

AR x GR

Mechanism

AR antagonists(Androgen Receptor antagonists), GR antagonists(Glucocorticoid receptor antagonists)

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication

Castration-Resistant Prostatic Cancer

Inactive Indication-

Originator Organization

Zhejiang Normal University

Active Organization

Zhejiang Normal University

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Androgen receptor (AR) antagonists play important roles in the treatment of castration-resistant prostate cancer (CRPC). The glucocorticoid receptor (GR) upregulation leads to drug resistance for clinically used antiandrogens. Therefore, blocking AR/GR signaling simultaneously has become an efficient strategy to overcome the drug resistance of CRPC. Our previous work indicated that Z19 could inhibit the activity of both AR and GR. Herein, we optimized the structure of Z19 and identified GA32 as a potent AR/GR dual inhibitor. GA32 efficiently reduced the mRNA and protein levels of AR/GR downstream genes. GA32 efficiently inhibited the proliferation of enzalutamide resistance CRPC both in vitro and in vivo. GA32 could directly bind to AR and GR, and the predicted binding modes for GA32 with AR/GR suggested that GA32 binds to the AR or GR hormone binding pocket. This work provides a potential lead compound with dual AR/GR inhibitory activity to conquer the drug resistance of CRPC.

21 May 1971·ScienceQ1 · CROSS-FIELD

GA ₃₂ : A Polar Gibberellin with High Biological Potency

Q1 · CROSS-FIELD

Article

Author: Coombe, B. G.

A new gibberellin, GA 32 , purified from Prunus seed, has three interesting properties: (i) it is the most polar of the 34 gibberellins presently known, (ii) it is the most potent of all gibberellins tested in the barley endosperm bioassay, and (iii) it is very active in promoting the growth of unpollinated apricot ovaries with a normal ratio of length to diameter.

100 Deals associated with GA-32

Login to view more data