Optimization of a novel peptide ligand targeting human carbonic anhydrase IX.

ABSTRACT:

Background

Carbonic anhydrase IX (CA IX) is a hypoxia-regulated transmembrane protein over-expressed in various types of human cancer. Recently, a new peptide with affinity for human carbonic anhydrase IX (CaIX-P1) was identified using the phage display technology. Aim of the present study is to characterize the binding site in the sequence of CaIX-P1, in order to optimize the binding and metabolic properties and use it for targeting purposes.

Methodology/principal findings

Various fragments of CaIX-P1 were synthesized on solid support using Fmoc chemistry. Alanine scanning was performed for identification of the amino acids crucial for target binding. Derivatives with increased binding affinity were radiolabeled and in vitro studies were carried out on the CA IX positive hu

SUBMITTER: Rana S 

PROVIDER: S-EPMC3365038 | biostudies-literature | 2012

REPOSITORIES: biostudies-literature