Drug intelligence / Profile preview

GA-017

Development stage
Preclinical
Lead developer
Nissan Chemical
Modality
Small Molecules
Administration
Oral
01

Overview

GA-017 is a small molecule inhibitor of Large Tumor Suppressor (LATS) kinases, which are key components of the Hippo signaling pathway. By inhibiting LATS, GA-017 prevents the phosphorylation and subsequent degradation of Yes-associated protein 1 (YAP), thereby promoting its nuclear translocation and activation. In the context of cardiac research, GA-017 has been shown to activate endogenous YAP in cardiomyocytes, leading to the induction of SHP-2. This mechanism suppresses IFN-γ/STAT1 signaling and STAT1 nuclear localization, which helps attenuate myocardial injury and promote tissue repair in models of experimental autoimmune myocarditis (EAM). It is being investigated as a potential therapeutic strategy for heart failure following myocarditis.

02

Targets

SGK2 (Serum/glucocorticoid regulated kinase 2)LATS2 (Large tumor suppressor kinase 2)PRKACB (cAMP-dependent protein kinase catalytic subunit beta)PKA (Cyclic amp-dependent protein kinase)LATS1SGK3 (Serum/glucocorticoid regulated kinase family member 3)RPS6KB1 (Ribosomal protein S6 kinase beta-1)

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