WebPeptidomimetic approaches have been utilized to design small molecules that selectively kill cancer cells, an approach known as targeted chemotherapy, by inducing programmed cell death by a process called apoptosis. WebUnderstanding the position of mutations across experimental protein structures, and their juxtapositions with known and predicted small-molecule binding sites also provided in COSMIC-3D, paves the way for using mutation data to generate hypotheses of the impacts of mutations on protein structure and function, and for "Mutation-Guided Drug Design" in …
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Web1 okt. 2015 · It is however desirable to have small molecule alternatives: a helix mimetic (proteomimetic) is a generic small molecule scaffold that projects functional groups in a … Web1 feb. 2014 · The rational design of helix mimetics is an appealing small-molecule strategy for the mediation of aberrant PPIs, however the first generation of scaffolds presented a relatively small number of residues on a single recognition surface. eglin mpf hours
Rapid Evaluation of Staple Placement in Stabilized α Helices Using ...
Web1 jan. 2016 · The oxopiperazine helix mimetics can be assembled from α-amino acids using standard solid-phase peptide synthesis methodology, enabling rapid diversification of the scaffold and discovery of ligands for protein targets. We have evaluated the biological potential of the oxopiperazine mimetics in cell-free, cell culture, and in vivo models. Web1 feb. 2015 · We highlight HTS methods for the identification of small-molecule α-helix mimetics. α-Helices are the most common protein secondary structure and play a key … WebGiven the significant involvement of ACE2 N-terminal helix in the interactions with SARS-CoV- 2 RBM, we hypothesized that targeting the latter by small molecule α-helix … folding cabinet bed sarah goode