Design, synthesis, structure-activity relationship studies, and evaluation of novel GLS1 inhibitors

Article Multidisciplinary Sciences

Senolysis by glutaminolysis inhibition ameliorates various age-associated disorders

Yoshikazu Johmura et al.

Summary: Research has shown that senescent cells rely on glutaminolysis for survival, and inhibiting this process can induce senolysis. Lysosomal membrane damage lowers intracellular pH in senescent cells, inducing KGA expression, leading to glutaminolysis, and ultimately producing ammonia to neutralize low pH and improve cell survival.

SCIENCE (2021)

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Article Chemistry, Medicinal

Discovery and optimization of novel 3-benzyl-N-phenyl-1H-pyrazole-5-carboxamides as bifunctional antidiabetic agents stimulating both insulin secretion and glucose uptake

Jeyun Jo et al.

Summary: A novel series of compounds were designed, synthesized, and evaluated for their effects on glucose-stimulated insulin secretion. The most active compound was identified through optimization and further studies showed the importance of N-hydrogen in the core structure. The compound was found to increase insulin secretion by activating the upstream effector of PDX-1 and promoting GSIS, while also enhancing glucose uptake in myotube cells.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Medicinal

Design, Synthesis, and Biological Evaluation of Novel 1,3-Oxazole Sulfonamides as Tubulin Polymerization Inhibitors

Edward Sisco et al.

Summary: A series of novel 1,3-oxazole sulfonamides show promising potential in inhibiting cancer cell growth, with high specificity for leukemia cell lines and effective binding to tubulin leading to microtubule depolymerization.

ACS MEDICINAL CHEMISTRY LETTERS (2021)

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Article Biochemistry & Molecular Biology