BU224

BPTES

BPTES is a small molecule inhibitor that specifically targets the enzyme glutaminase, which plays a crucial role in the metabolism of glutamine. This compound has garnered significant interest in the field of cancer research due to its potential to disrupt the metabolic pathways that cancer cells rely on for growth and survival.

Mechanism of Action

BPTES inhibits glutaminase, an enzyme that catalyzes the conversion of glutamine to glutamate. This reaction is a key step in the glutaminolysis pathway, which is essential for the production of energy and biosynthetic precursors in rapidly proliferating cells, such as cancer cells. By inhibiting glutaminase, BPTES effectively reduces the availability of glutamate, thereby disrupting the tricarboxylic acid (TCA) cycle and limiting the production of ATP and other critical metabolites.

Applications in Cancer Research

Cancer cells often exhibit altered metabolism, known as the Warburg effect, where they rely heavily on glycolysis and glutaminolysis for energy production and growth. BPTES has been shown to selectively inhibit the growth of cancer cells that are dependent on glutamine metabolism. Studies have demonstrated that BPTES can reduce tumor growth in various cancer models, including breast cancer, lung cancer, and glioblastoma.

Pharmacokinetics and Administration

BPTES is typically administered in preclinical studies via intraperitoneal injection or oral gavage. The compound has been optimized for stability and bioavailability, although further studies are needed to fully understand its pharmacokinetic properties in humans. Current research is focused on improving the delivery and efficacy of BPTES in clinical settings.

Challenges and Future Directions

While BPTES shows promise as a therapeutic agent, there are challenges that need to be addressed. One major challenge is the development of resistance mechanisms by cancer cells, which may bypass the need for glutamine metabolism. Additionally, the potential toxicity and side effects of long-term glutaminase inhibition are not fully understood. Future research is aimed at overcoming these challenges by developing combination therapies and identifying biomarkers for patient stratification.

Also see

• Glutaminase
• Cancer metabolism
• Warburg effect
• Targeted cancer therapy

{{Drugbox | verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = N-[[4-(2,5-dichlorophenoxy)phenyl]sulfonyl]-L-glutamic acid | image = BPTES_structure.png | width = 200 | CAS_number = 314045-39-1 | PubChem = 9826522 | ChemSpiderID = 8001863 | UNII = 3F0K3T4OSW | ChEMBL = 109481 | SMILES = C1=CC(=CC=C1OC2=CC(=C(C=C2)Cl)Cl)S(=O)(=O)NC(CCC(=O)O)C(=O)O }}