Phosphinic peptide
WebApr 13, 1999 · RXP 407, a phosphinic peptide, is a potent inhibitor of angiotensin I converting enzyme able to differentiate between its two active sites Vincent Dive, Joël … WebThree phosphinic acids 11a–c were synthesized according to literature protocols (see ESI ‡) and applied in an analogous silylation and Staudinger reaction sequence with immobilized …
Phosphinic peptide
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WebApr 13, 1999 · By screening phosphinic peptide libraries, we discovered a phosphinic peptide Ac-Asp-(L) Pheψ(PO 2-CH 2) (L) Ala-Ala-NH 2, called RXP 407, which is able to differentiate the two ACE active sites, with a dissociation constant three orders of magnitude lower for the N-domain of the enzyme. The usefulness of a combinatorial … WebFeb 12, 2024 · Among the plethora of bioactive scaffolds with numerous applications in drug discovery, phosphinic peptides undoubtedly hold a prominent position [1,2,3,4,5,6,7,8,9]. …
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. WebDec 27, 2024 · Currently, phosphinic peptides showing advantageous physicochemical and pharmacokinetic properties are intensively explored as a source of new bioactive compounds and drug candidates targeted to zinc-metalloproteases, such as angiotensin-converting enzyme, matrix metalloproteinases, and aminopeptidases [4, 5].
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). WebOct 12, 2024 · Phosphinic peptides are isosteres of natural peptides, in the molecule of which the NHC (O) peptide bond is replaced by a zinc chelating methylenephosphorylic …
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are an important class of metabolically stable, Zn-metalloprotease inhibitors in which the scissile peptide bond has been replaced by the chemically stable phosphinic
Webfamily 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]. shuffleboard table top materialWebMay 5, 2006 · Simple, rapid, and efficient methods for P1‘ diversification of phosphinic peptides have been developed, employing alkylation and Knoevenagel-type condensation … the others horror movieWebPhosphinic acid derivatives exhibit diverse biological activities and a high degree of structural diversity, rendering them a versatile tool in the development of new medicinal agents. Pronounced recent progress, coupled with previous research findings, highlights the impact of this moiety in medicinal chemistry. ... shuffleboard table top gameWebSep 6, 2024 · We designed an 11-mer cross-linking probe, designated DG023, with peptide sequence based on a known ERAP1 substrate 8, the nonhydrolyzable phosphinic group replacing the first peptide bond,... shuffleboard table with topWebpared to hydroxamate compounds, phosphinic peptides were often observed to display lower potency, suggesting that the phosphinic group is a weaker zinc-chelating group … shuffleboard tables used near methe others houseWebPhosphinic 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. the others horror