Click-Addressable Cassette for Photoaffinity Labeling. Academic Article

abstract

• A small molecule 1 was designed to contain an alkyne, a trifluoromethyl phenyldiazirine, and a free piperidine-NH for facile conjugation to protein binding ligands. This "cassette" 1 was synthesized via a relatively direct route involving only routine steps. In this proof-of-concept study, putative ligands for carbonic anhydrase IX and for TrkC were conjugated to 1. Photoaffinity labeling was performed using purified extracellular regions of both these protein-receptors, and using cells that express these receptors (isolation via a pull-down procedure), labeling of the protein was observed in all four experiments.

authors

• Burgess, Kevin

published proceedings

• ACS Med Chem Lett

altmetric score

• 2.85

author list (cited authors)

• Zhao, B., & Burgess, K.

citation count

• 6

complete list of authors

• Zhao, Bosheng||Burgess, Kevin

publication date

• February 2018

publisher

• American Chemical Society (ACS)  Publisher

published in

• ACS Medicinal Chemistry Letters  Journal

keywords

• Carbonic Anhydrase Ix
• Click Chemistry
• Photoaffinity Labeling
• Targeting
• Trkc

PubMed Central ID

• 29456805

Digital Object Identifier (DOI)

• 10.1021/acsmedchemlett.7b00516

start page

• 155

end page

• 158

volume

• 9

issue

• 2

URL

• http://dx.doi.org/10.1021/acsmedchemlett.7b00516