Biomaterial Database

Rapid synthesis and in situ screening of potent HIV-1 protease dimerization inhibitors. 2006

Song-Gil Lee, and Jean Chmielewski

Department of Chemistry, Purdue University, West Lafayette, Indiana 47907, USA.

A library of dimerization inhibitors of HIV-1 protease is described based on crosslinked interfacial peptides. The 54 component library was designed to contain two modifications to the starting structure, one each in the Northern and Southern fragments. A rapid synthesis and in situ screening method in microtiter plates was developed to facilitate the generation and evaluation of the library members. More than 90% of the doubly modified agents were more potent than their respective singly mutated parent compounds, and five of the most potent dimerization inhibitors of HIV-1 protease described to date were identified. The free energy of binding for the combined two modifications was generally found to be additive, demonstrating the predictive value of earlier libraries.

UI	MeSH Term	Description	Entries
D008826	Microbial Sensitivity Tests	Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).	Bacterial Sensitivity Tests,Drug Sensitivity Assay, Microbial,Minimum Inhibitory Concentration,Antibacterial Susceptibility Breakpoint Determination,Antibiogram,Antimicrobial Susceptibility Breakpoint Determination,Bacterial Sensitivity Test,Breakpoint Determination, Antibacterial Susceptibility,Breakpoint Determination, Antimicrobial Susceptibility,Fungal Drug Sensitivity Tests,Fungus Drug Sensitivity Tests,Sensitivity Test, Bacterial,Sensitivity Tests, Bacterial,Test, Bacterial Sensitivity,Tests, Bacterial Sensitivity,Viral Drug Sensitivity Tests,Virus Drug Sensitivity Tests,Antibiograms,Concentration, Minimum Inhibitory,Concentrations, Minimum Inhibitory,Inhibitory Concentration, Minimum,Inhibitory Concentrations, Minimum,Microbial Sensitivity Test,Minimum Inhibitory Concentrations,Sensitivity Test, Microbial,Sensitivity Tests, Microbial,Test, Microbial Sensitivity,Tests, Microbial Sensitivity
D009842	Oligopeptides	Peptides composed of between two and twelve amino acids.	Oligopeptide
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D015497	HIV-1	The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte.	Human immunodeficiency virus 1,HIV-I,Human Immunodeficiency Virus Type 1,Immunodeficiency Virus Type 1, Human
D017320	HIV Protease Inhibitors	Inhibitors of HIV PROTEASE, an enzyme required for production of proteins needed for viral assembly.	HIV Protease Inhibitor,Inhibitor, HIV Protease,Inhibitors, HIV Protease,Protease Inhibitor, HIV,Protease Inhibitors, HIV
D019151	Peptide Library	A collection of cloned peptides, or chemically synthesized peptides, frequently consisting of all possible combinations of amino acids making up an n-amino acid peptide.	Phage Display Peptide Library,Random Peptide Library,Peptide Phage Display Library,Phage Display Library, Peptide,Synthetic Peptide Combinatorial Library,Synthetic Peptide Library,Libraries, Peptide,Libraries, Random Peptide,Libraries, Synthetic Peptide,Library, Peptide,Library, Random Peptide,Library, Synthetic Peptide,Peptide Libraries,Peptide Libraries, Random,Peptide Libraries, Synthetic,Peptide Library, Random,Peptide Library, Synthetic,Random Peptide Libraries,Synthetic Peptide Libraries
D019281	Dimerization	The process by which two molecules of the same chemical composition form a condensation product or polymer.	Dimerizations
D020836	Protein Structure, Quaternary	The characteristic 3-dimensional shape and arrangement of multimeric proteins (aggregates of more than one polypeptide chain).	Quaternary Protein Structure,Protein Structures, Quaternary,Quaternary Protein Structures
D024882	Drug Resistance, Viral	The ability of viruses to resist or to become tolerant to chemotherapeutic agents or antiviral agents. This resistance is acquired through gene mutation.	Antiviral Drug Resistance,Antiviral Drug Resistances,Drug Resistances, Viral
D066298	In Vitro Techniques	Methods to study reactions or processes taking place in an artificial environment outside the living organism.	In Vitro Test,In Vitro Testing,In Vitro Tests,In Vitro as Topic,In Vitro,In Vitro Technique,In Vitro Testings,Technique, In Vitro,Techniques, In Vitro,Test, In Vitro,Testing, In Vitro,Testings, In Vitro,Tests, In Vitro,Vitro Testing, In