Piptides: New, Easily Accessible Chemotypes For Interactions With Biomolecules. Academic Article

abstract

• Small molecule probe development is pivotal in biomolecular science. Research described here was undertaken to develop a non-peptidic chemotype, piptides, that is amenable to convenient, iterative solid-phase syntheses, and useful in biomolecular probe discovery. Piptides can be made from readily accessible pip acid building blocks and have good proteolytic and pH stabilities. An illustrative application of piptides against a protein-protein interaction (PPI) target was explored. The Exploring Key Orientations (EKO) strategy was used to evaluate piptide candidates for this. A library of only 14 piptides contained five members that disrupted epidermal growth factor (EGF) and its receptor, EGFR, at low micromolar concentrations. These piptides also caused apoptotic cell death, and antagonized EGF-induced phosphorylation of intracellular tyrosine residues in EGFR.

authors

• Burgess, Kevin

published proceedings

• Angew Chem Int Ed Engl

altmetric score

• 1.5

author list (cited authors)

• Arancillo, M., Taechalertpaisarn, J., Liang, X., & Burgess, K.

citation count

• 1

complete list of authors

• Arancillo, Maritess||Taechalertpaisarn, Jaru||Liang, Xiaowen||Burgess, Kevin

publication date

• March 2021

publisher

• Wiley  Publisher

published in

• Angewandte Chemie International Edition  Journal

keywords

• Cancer
• Egf
• Epidermal Growth Factor
• ErbB Receptors
• Humans
• Hydrogen-Ion Concentration
• Molecular Structure
• Peptides
• Peptidomimetics
• Phosphorylation
• Protein Binding
• Protein-protein Interactions
• Solid-phase Synthesis

PubMed Central ID

• 33319463

Digital Object Identifier (DOI)

• 10.1002/anie.202015203

start page

• 6653

end page

• 6659

volume

• 60

issue

• 12

URL

• http://dx.doi.org/10.1002/anie.202015203