nep 28

NEP-28 is an AR agonist. NEP28 is a new SARM exhibiting high selectivity for androgen receptor. NEP28 showed tissue-selective effect equivalent to or higher than existing SARMs. In addition, the administration of NEP28 increased the activity of neprilysin, a known Aβ-degrading enzyme.

GLP-1(28-36)amide TFA, a C-terminal nonapeptide derived from GLP-1 cleavage by neutral endopeptidase (NEP), is an antioxidant that targets mitochondria and inhibits mitochondrial permeability transition (MPT), demonstrating anti-diabetic and cardioprotective effects [1].

GLP-1(28-36)amide, a C-terminal nonapeptide derived from the cleavage of GLP-1 by neutral endopeptidase (NEP), is an important compound that functions as an antioxidant primarily targeting the mitochondrion to inhibit mitochondrial permeability transition (MPT), displaying anti-diabetic properties and cardioprotection effects[1].

MPT0B098 is a potent microtubule inhibitor through binding to the colchicine-binding site of tubulin. MPT0B098 is active against the growth of various human cancer cells, including chemoresistant cells with IC50 values ranging from 70 to 150 nmol/L. MPT0B098 arrests cells in the G2–M phase and subsequently induces cell apoptosis. In addition, MPT0B098 effectively suppresses VEGF-induced cell migration and capillary-like tube formation of HUVECs. Distinguished from other microtubule inhibitors, MPT0B098 not only inhibited the expression levels of HIF-1α protein but also destabilized HIF-1α mRNA. The mechanism of causing unstable of HIF-1α mRNA by MPT0B098 is through decreasing RNA-binding protein, HuR, translocation from the nucleus to the cytoplasm. Notably, MPT0B098 effectively suppresses tumor growth and microvessel density of tumor specimens in vivo. Taken together, our results provide a novel mechanism of inhibiting HIF-1α of a microtubule inhibitor MPT0B098. MPT0B098 is......