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Showing 1 to 4 of 4 for “"Pin1 inhibitors"”.
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Pin1 Inhibitors: Towards Understanding the Enzymatic Mechanism
An important role of Pin1 is to catalyze the cis-trans isomerization of pSer/Thr-Pro bonds; as such, it plays an important role in many cellular events through the effects of conformational change on the function of its biological substrates, including Cdc25, c-Jun, and p53. The expression of Pin1 …
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Design, Syntheses, and Bioactivities of Conformationally Locked Pin1 Ground State Inhibitors
Pin1 (protein interacting with NIMA 1) is a peptidyl-prolyl isomerase involved in mitosis. As a potential anti-cancer drug target, Pin1 interacts and regulates the activity of an increasing number of cell cycle enzymes by an unknown mechanism. These cell cycle enzymes include Cdc25, Cdc27, Cyclin …
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Part 1 Design, Synthesis and Bioactivity of a Phosphorylated Prodrug for the Inhibition of Pin1; Part 2 Conformational Specificity of Cdc25c Substrate for Cdc2 Kinase using LC-MS/MS
… PPIase (peptidyl prolyl isomerase), Pin1 (Protein interacting with NIMA#1), has been found to regulate cell cycle through a simple conformational change, the cis-trans isomerization of phospho-Ser/Thr-Pro amide bonds. A variety of key cell cycle regulatory phosphoproteins, including …
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Pin1: WW domain ligands, catalytic inhibitors, and the mechanism
… that might arrest cancer proliferation. Pin1 is the first phosphorylation-dependent PPIase enzyme to be discovered. The Pin1 regulatory mechanism, acting on other mitotic proteins in vivo and in vitro, remains largely unknown. For the study of Pin1 function, two types of assays were used …