Structure-based design, synthesis and evaluation of bioactivity of anti-P-gp peptide mimetic / 药学学报

ABSTRACT

<p><b>AIM</b>To design and evaluate the small peptide mimetic of anti-P-glycoprotein (P-gp) antibody (PHMA02).</p><p><b>METHODS</b>From the three dementional structure analysis of computer modeling of PHMA02 CDR loops, a small peptide mimetic was designed and determined by flow cytometry.</p><p><b>RESULTS</b>Anti-P-gp peptide mimetic functionally similar to PHMA02 was developed. The peptide mimetic competitively inhibits PHMA02 binding to P-gp and partially block the P-gp function as a drug efflux pump in K562/A02 cells.</p><p><b>CONCLUSION</b>Some special conformational properties of CDR loops of antibody might serve as lead structures for develop new biological peptide mimetics. Antibody-structure-based design would develop new drug in the future.</p>