Exploiting differences in caspase-2 and -3 S2 subsites for selectivity: Structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors was written by Maillard, Michel C.;Brookfield, Frederick A.;Courtney, Stephen M.;Eustache, Florence M.;Gemkow, Mark J.;Handel, Rebecca K.;Johnson, Laura C.;Johnson, Peter D.;Kerry, Mark A.;Krieger, Florian;Meniconi, Mirco;Munoz-Sanjuan, Ignacio;Palfrey, Jordan J.;Park, Hyunsun;Schaertl, Sabine;Taylor, Malcolm G.;Weddell, Derek;Dominguez, Celia. And the article was included in Bioorganic & Medicinal Chemistry in 2011.Reference of 86069-86-5 The following contents are mentioned in the article:
Several caspases have been implicated in the pathogenesis of Huntington’s disease (HD); however, existing caspase inhibitors lack the selectivity required to investigate the specific involvement of individual caspases in the neuronal cell death associated with HD. In order to explore the potential role played by caspase-2, the potent but non-selective canonical Ac-VDVAD-CHO caspase-2 inhibitor 1 was rationally modified at the P2 residue in an attempt to decrease its activity against caspase-3. With the aid of structural information on the caspase-2, and -3 active sites and mol. modeling, a 3-(S)-substituted-
(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Reference of 86069-86-5
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem