2023年4月3日 · Bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl (BPTES), a potent orally available GLS1 inhibitor that spares GLS2, shows promising antitumor effects against human...

In this study, we used a proprietary emulsification process to encapsulate bis-2- (5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES), a selective but relatively insoluble glutaminase inhibitor, in nanoparticles. BPTES nanoparticles demonstrated improved pharmacokinetics and efficacy compared with unencapsulated BPTES.

2016年9月6日 · In this study, we used a proprietary emulsification process to encapsulate bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES), a selective but relatively insoluble glutaminase inhibitor, in nanoparticles.

BPTES prolongs survival of a genetically engineered mouse model of liver cancer. Based on the observation that loss of 1 copy of Gls could delay tumorigenesis, we sought to determine whether pharmacological inhibition of GLS with BPTES could prolong survival in immunocompetent transgenic mice.

BPTES is a selective inhibitor of Glutaminase GLS1. Vaccinia virus (VACV) requires glutamine metabolism for its optimal replication. Inhibition of glutaminolysis by bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) can be a potential method to treat poxvirus infections.

2023年7月5日 · Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal.

2023年7月5日 · Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal.

BPTES (10 μM) reduces glutaminase activity in both WT and mutant IDH1 expressing cells, diminishes glutamate and α-KG levels, and increases glycolytic intermediates while leaving total 2-HG levels unaffected.

2021年1月15日 · BPTES treatment eliminated the SA–β-gal–positive population and improved serum free fatty acids (FFAs) in the aged mice . It alleviated adipose tissue atrophy and macrophage invasion in adipose tissue in aged mice (100-week-old males) ( Fig. 4E ).

2021年5月23日 · BPTES. The GLS1 selective inhibitor bis-2-(5-phenylacetamido-1, 3, 4-thiadiazol-2-yl) ethyl sulfide (BPTES) introduced by Robinson is known to inhibit GAC through an allosteric mechanism by stabilizing inactive tetramers [38, 90].