164267-55-4Relevant academic research and scientific papers
Synthesis of cell-permeable stapled BH3 peptide-based Mcl-1 inhibitors containing simple aryl and vinylaryl cross-linkers
Muppidi, Avinash,Doi, Kenichiro,Ramil, Carlo P.,Wang, Hong-Gang,Lin, Qing
, p. 7740 - 7745 (2014)
We report the synthesis of a series of distance-matching aryl and vinylaryl cross-linkers for constructing stapled peptides containing cysteines at i,i+7 positions. Langevin dynamics simulation studies helped to classify these cross-linkers into two categories: the rigid cross-linkers with narrower S-S distance distribution and the flexible cross-linkers with wider S-S distance distribution. The stapled Noxa BH3 peptides with the flexible distance-matching cross-linkers gave the highest degree of helicity as well as the most potent inhibitory activity against Mcl-1. However, the stapled peptides with the highest hydrophobicity showed the most efficient cellular uptake. Together, this work illustrates the divergent nature of binding affinity and cellular uptake, and the vital importance of choosing appropriate cross-linkers in constructing stapled peptides with the drug-like properties.
OXYNTOMODULIN ANALOGS AND METHODS OF MAKING AND USING SAME
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Paragraph 0080, (2017/08/08)
Provided are oxyntomodulin analogs. The peptide analogs have at least two cysteines. The two cysteines are separated by six amino acids such that they can be crosslinked using suitable crosslinking moieties. The crosslinked peptides have long half-lives and/or efficacy. For example, peptide analog compositions are used for inducing weight loss and/or reducing blood glucose levels.
