Structure-based design， synthesis and evaluation of bioactivity of anti-P-gp peptide mimetic

AimTo design and evaluate the small peptide mimetic of anti-P-glycoprotein ( P-gp ) antibody (PHMA02 ). MethodsFrom the three dementional structure analysis of computer modeling of PHMA02 CDR loops, a small peptide mimetic was designed and determined by flow cytometry. ResultsAnti-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. ConclusionSome 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.