Delving into the Latest Updates on LWG-301 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

GLS1

Action

modulators

Mechanism

GLS1 modulators(Glutaminase kidney isoform, mitochondrial modulators)

Therapeutic Areas

Infectious Diseases

Active Indication

Coronavirus Infections

Inactive Indication-

Originator Organization

China Pharmaceutical University

Active Organization

Sanford Burnham Prebys Medical Discovery Institute

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Tumor cells often exhibit metabolic reprogramming to maintain their rapid growth and proliferation. Glutaminase 1 (GLS1) has been viewed as a promising target in the glutamine metabolism pathway for the treatment of malignant tumors. Using structure-based drug design approaches, a novel series of GLS1 allosteric inhibitors were designed and synthesized. Compound 41a (LWG-301) with an alkane chain "tail" group had potent biochemical and cellular GLS1 activity, and improved metabolic stability. LWG-301 exhibited moderate antitumor effects in HCT116 xenograft model, with TGI of 38.9% in vivo. Mechanistically, LWG-301 could significantly block glutamine metabolism, resulting in changes in the corresponding amino acid levels in cells, induce a concentration-dependent increase in intracellular ROS levels, and induce apoptosis. Taken together, this paper provides more structural references and new design strategy for the development of GLS1 allosteric inhibitors.

100 Deals associated with LWG-301

Login to view more data