Structure-based design, synthesis and evaluation of bioactivity of anti-P-gp peptide mimetic / 药学学报
Acta Pharmaceutica Sinica
; (12): 826-830, 2003.
Article
en Zh
| WPRIM
| ID: wpr-266575
Biblioteca responsable:
WPRO
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>
Texto completo:
1
Base de datos:
WPRIM
Asunto principal:
Péptidos
/
Conformación Proteica
/
Unión Competitiva
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Diseño de Fármacos
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Química
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Miembro 1 de la Subfamilia B de Casetes de Unión a ATP
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Imitación Molecular
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Resistencia a Múltiples Medicamentos
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Células K562
/
Regiones Determinantes de Complementariedad
Límite:
Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2003
Tipo del documento:
Article