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Full-Text Articles in Chemicals and Drugs
Structural And Thermodynamic Basis Of Amprenavir/Darunavir And Atazanavir Resistance In Hiv-1 Protease With Mutations At Residue 50, Seema Mittal, Rajintha Bandaranayake, Nancy King, Moses Prabu-Jeyabalan, Madhavi Nalam, Ellen Nalivaika, Nese Yilmaz, Celia Schiffer
Structural And Thermodynamic Basis Of Amprenavir/Darunavir And Atazanavir Resistance In Hiv-1 Protease With Mutations At Residue 50, Seema Mittal, Rajintha Bandaranayake, Nancy King, Moses Prabu-Jeyabalan, Madhavi Nalam, Ellen Nalivaika, Nese Yilmaz, Celia Schiffer
Celia A. Schiffer
Drug resistance occurs through a series of subtle changes that maintain substrate recognition but no longer permit inhibitor binding. In HIV-1 protease, mutations at I50 are associated with such subtle changes that confer differential resistance to specific inhibitors. Residue I50 is located at the protease flap tips, closing the active site upon ligand binding. Under selective drug pressure, I50V/L substitutions emerge in patients, compromising drug susceptibility and leading to treatment failure. The I50V substitution is often associated with amprenavir (APV) and darunavir (DRV) resistance, while the I50L substitution is observed in patients failing atazanavir (ATV) therapy. To explain how APV, …
Structure And Dynamics Of A Primordial Catalytic Fold Generated By In Vitro Evolution, Fa-An Chao, Aleardo Morelli, John C. Haugner Iii, Lewis Churchfield, Lei Shi, Larry R. Masterson, Ritimukta Sarangi, Gianluigi Veglia, Burckhard Seelig
Structure And Dynamics Of A Primordial Catalytic Fold Generated By In Vitro Evolution, Fa-An Chao, Aleardo Morelli, John C. Haugner Iii, Lewis Churchfield, Lei Shi, Larry R. Masterson, Ritimukta Sarangi, Gianluigi Veglia, Burckhard Seelig
Larry Masterson