3-Mercaptopropionic acid-mediated synthesis of peptide and protein thioesters
作者:Jaskiranjit Kang、Jonathan P. Richardson、Derek Macmillan
DOI:10.1039/b815888f
日期:——
Peptides and proteins fragment sequence-specifically in the presence of 3-mercaptopropionic acid to afford thioesters which can be used in native chemical ligation reactions.
A new series of IGF-1R inhibitors related to hydantoins were identified from a lead originating from HTS. Their noncompetitive property as well as their slow binding characteristics provided a series of compounds with unique selectivity and excellent cellular activities.
Probing Protein Surfaces: QSAR Analysis with Helix Mimetics
作者:Valeria Azzarito、Philip Rowell、Anna Barnard、Thomas A. Edwards、Andrew Macdonald、Stuart L. Warriner、Andrew J. Wilson
DOI:10.1002/cbic.201500504
日期:2016.4.15
Rationalising behaviour: Using a helix mimeticbased on an oligoamide scaffold, we have exploited a modular synthesis to access compounds that can readily be used to understand the noncovalent determinants of hDM2 recognition by cell‐active p53/hDM2 inhibitors.
合理化行为:使用基于寡酰胺支架的螺旋模拟物,我们利用模块化合成来获取化合物,这些化合物可以很容易地用于理解细胞活性 p53/ h DM2 抑制剂识别h DM2 的非共价决定因素。
Stereocontrolled protein surface recognition using chiral oligoamide proteomimetic foldamers
作者:Valeria Azzarito、Jennifer A. Miles、Julie Fisher、Thomas A. Edwards、Stuart L. Warriner、Andrew J. Wilson
DOI:10.1039/c4sc03559c
日期:——
An oligoamide helix mimicking foldamer with well-defined conformation is shown to recognize its target protein hDM2 in a manner that depends upon the composition, spatial projection and stereochemistry of functional groups appended to the scaffold.
A water-soluble derivative of N-fused porphyrin (NFP) possessing a nona-arginine (R9) peptide tail was synthesized for the first time by a Cu(I)-catalyzed azide-alkyne 'click' reaction. In aqueous solution, at pH 8, the conjugated molecule (NFP-R9) exists as free base and protonated below pH < 6.5 to form monoprotonated species dominantly, and diprotonated one below pH < 2.3, while such clear two-step protonation behavior was not observed in the DMF solution. (c) 2009 Elsevier Ltd. All rights reserved.