Discovery of Potent Antagonists of the Antiapoptotic Protein XIAP for the Treatment of Cancer was written by Oost, Thorsten K.;Sun, Chaohong;Armstrong, Robert C.;Al-Assaad, Ali-Samer;Betz, Stephen F.;Deckwerth, Thomas L.;Ding, Hong;Elmore, Steven W.;Meadows, Robert P.;Olejniczak, Edward T.;Oleksijew, Andrew;Oltersdorf, Tilman;Rosenberg, Saul H.;Shoemaker, Alexander R.;Tomaselli, Kevin J.;Zou, Hua;Fesik, Stephen W.. And the article was included in Journal of Medicinal Chemistry in 2004.Recommanded Product: 86069-86-5 The following contents are mentioned in the article:
Inhibitor of apoptosis (IAP) proteins are overexpressed in many cancers and have been implicated in tumor growth, pathogenesis, and resistance to chemo- or radiotherapy. On the basis of the NMR structure of a SMAC peptide complexed with the BIR3 domain of X-linked IAP (XIAP), a novel series of XIAP antagonists was discovered. The most potent compounds in this series bind to the baculovirus IAP repeat 3 (BIR3) domain of XIAP with single-digit nanomolar affinity and promote cell death in several human cancer cell lines. In a MDA-MB-231 breast cancer mouse xenograft model, these XIAP antagonists inhibited the growth of tumors. Close structural analogs that showed only weak binding to the XIAP-BIR3 domain were inactive in the cellular assays and showed only marginal in vivo activity. Our results are consistent with a mechanism in which ligands for the BIR3 domain of XIAP induce apoptosis by freeing up caspases. The present study validates the BIR3 domain of XIAP as a target and supports the use of small mol. XIAP antagonists as a potential therapy for cancers that overexpress XIAP. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Recommanded Product: 86069-86-5).
(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Recommanded Product: 86069-86-5
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem