Phosphinic peptide
WebPhosphinic peptides are an important class of metabolically stable, Zn-metalloprotease inhibitors in which the scissile peptide bond has been replaced by the chemically stable phosphinic WebJan 1, 2014 · Phosphinic peptides, which share closed structural similarities with the transition-state of peptide substrate upon hydrolysis, have thus been considered for identifying potent inhibitors of proteases. Focusing on the zinc-proteases family, this review presents the most important synthetic efforts performed to obtain the desired compounds.
Phosphinic peptide
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WebPhosphinic acid peptides (phosphinic pseudopeptides) are peptide isosteres where one peptide bond is substituted by the nonhydrolysable phosphinate moiety -P(O)(OH)-CH2- or … WebIn particular, phosphinic peptides are peptidic isosters containing a chemically stable phosphinic acid moiety which mimics the transition state tetrahedral geometry of a …
WebPhosphinic peptides as potent inhibitors of zinc-metalloproteases The development of transition-state analogs is a major objective in enzymology, not only for developing potent inhibitors of enzymes but also for dissecting enzyme catalytic mechanisms. WebApr 15, 1998 · Phosphinic peptides, the first potent inhibitors of astacin, behave as extremely slow-binding inhibitors A series of phosphinic pseudo-peptides varying in length and composition have been designed as inhibitors of the crayfish zinc endopeptidase astacin, the prototype of the astacin family and of the metzincin superfamily of …
WebPhosphinic peptides as potent inhibitors of zinc-metalloproteases The development of transition-state analogs is a major objective in enzymology, not only for developing potent … WebPhosphinic peptide analogues are potent, reversible, and competitive inhibitors of metalloproteases, the enzymes that catalyze the cleavage of an amide bond in the …
WebC. Van Der Auwera is an academic researcher. The author has contributed to research in topic(s): Imino acid & Reagent. The author has an hindex of 3, co-authored 7 publication(s) receiving 32 citation(s).
WebThe utility potential of phosphinic peptides in drug design was greatly increased by development of a synthetic procedure leading to the Fmoc-Aa 1 [P(O)(OAd)CH 2 ]-Aa 2 building block [16]. data center bmsWebFeb 1, 2024 · Phosphinic peptide Angiotensin-converting enzyme 1. Introduction Angiotensin-converting enzyme (ACE) is one of the major therapeutic targets for … marriott ponte vedraWebThree phosphinic acids 11a–c were synthesized according to literature protocols (see ESI ‡) and applied in an analogous silylation and Staudinger reaction sequence with immobilized … datacenter bmsWebAug 1, 2004 · In particular, phosphinic peptides are peptidic isosters containing a chemically stable phosphinic acid moiety which mimics the transition state tetrahedral geometry of a scissile peptide bond ... marriott ponte vedra spaWebPhosphinites are prepared by alcoholysis of organophosphinous chlorides. For example, treatment of chlorodiphenylphosphine with methanol and base gives methyl … data center bitcoin miningWebApr 27, 2006 · General method for the synthesis of compounds of type 3 (3a-3d): R2 H N P O OH R1 OR3 OR4 O O HMDS activation: A suspension of the phosphinic acid (1mmol) and hexamethyldisilazane (4eq) was heated at 110oC for 1h under argon atmosphere.The appropriate acrylate 2 (1.1mmol) was added at this temperature dropwise for 15 min and … marriott portland oregon restaurantWebfamily of pseudo-peptides, termed phosphinic peptides. The chemical structure of phosphinic peptides shares some features with that of intermediates formed during the hydrolysis of peptides by proteolytic enzymes (fig. 1). Based on this analogy, phosphinic peptides have been proposed to represent a source of synthetic protease in-hibitors [1–3]. data center basics pdf