Identification of a potent and selective covalent Pin1 inhibitor was written by Pinch, Benika J.;Doctor, Zainab M.;Nabet, Behnam;Browne, Christopher M.;Seo, Hyuk-Soo;Mohardt, Mikaela L.;Kozono, Shingo;Lian, Xiaolan;Manz, Theresa D.;Chun, Yujin;Kibe, Shin;Zaidman, Daniel;Daitchman, Dina;Yeoh, Zoe C.;Vangos, Nicholas E.;Geffken, Ezekiel A.;Tan, Li;Ficarro, Scott B.;London, Nir;Marto, Jarrod A.;Buratowski, Stephen;Dhe-Paganon, Sirano;Zhou, Xiao Zhen;Lu, Kun Ping;Gray, Nathanael S.. And the article was included in Nature Chemical Biology.Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:
Peptidyl-prolyl cis/trans isomerase NIMA-interacting 1 (Pin1) is commonly over-expressed in human cancers, including pancreatic ductal adenocarcinoma (PDAC). While Pin1 is dispensable for viability in mice, it is required for activated Ras to induce tumorigenesis, suggesting a role for Pin1 inhibitors in Ras-driven tumors, such as PDAC. We report the development of rationally designed peptide inhibitors that covalently target Cys113, a highly conserved cysteine located in the Pin1 active site. The inhibitors were iteratively optimized for potency, selectivity and cell permeability to give BJP-06-005-3, a versatile tool compound with which to probe Pin1 biol. and interrogate its role in cancer. In parallel to inhibitor development, we employed genetic and chem.-genetic strategies to assess the consequences of Pin1 loss in human PDAC cell lines. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).
(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Name: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem