Drug intelligence / Profile preview

GQ-16

Development stage
Preclinical
Lead developer
University of Brasília
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

GQ-16 is a **synthetic small molecule partial agonist of peroxisome proliferator-activated receptor gamma (PPARγ)**, belonging to the thiazolidinedione (TZD) class. Unlike full agonists such as rosiglitazone, GQ-16 selectively stabilizes the β-sheet region of PPARγ and potently blocks Cdk5-mediated phosphorylation of Ser-273, which is strongly linked to its **insulin-sensitizing effects without causing weight gain or edema** in animal models. GQ-16 demonstrates anti-diabetic efficacy comparable to rosiglitazone and has also shown **antifibrotic and immunomodulatory properties in preclinical models of systemic sclerosis**. The unique binding mode of GQ-16 results in partial agonism with minimal classical activation of PPARγ transcriptional activities, supporting its potential as a next-generation insulin sensitizer and anti-fibrotic agent[1][3][5][7][13][14].

Other names
LPSF/GQ-16 PPAR Agonist IX
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)Peroxisome proliferator-activated receptor gamma (PPARγ) Serine 273

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