Rational conversion of noncontinuous active region in proteins into a small orally bioavailable macrocyclic drug-like molecule: The HIV-1 CD4:gp120 paradigm

Bioorganic and Medicinal Chemistry

Volumn 18, Issue 15, 2010, Pages 5754-5761

  Hurevich, Mattan ^a   Swed, Avi ^b   Joubran, Salim ^a   Cohen, Shira ^a   Freeman, Noam S ^a   Britan Rosich, Elena ^d   Briant Longuet, Laurence ^c   Bardy, Martine ^c   Devaux, Christian ^c   Kotler, Moshe ^d   Hoffman, Amnon ^b   Gilon, Chaim ^a  

^a HEBREW UNIVERSITY OF JERUSALEM   (Israel)

^b HEBREW UNIVERSITY OF JERUSALEM   (Israel)

^c Institut de Biologie   (France)

^d HEBREW UNIVERSITY   (Israel)

Author keywords

Backbone cyclization; Drug design; HIV 1; Macrocycles; Proteomics

Indexed keywords

'CG 1'; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; CD4 ANTIGEN; GLYCOPROTEIN GP 120; MACROCYCLIC COMPOUND; UNCLASSIFIED DRUG; GP120 PROTEIN, HUMAN IMMUNODEFICIENCY VIRUS 1; PROTEIN BINDING;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BINDING SITE; BLOOD SAMPLING; CHEMICAL MODIFICATION; CYCLIZATION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG HALF LIFE; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; ISOMER; MALE; MATRIX ASSISTED LASER DESORPTION IONIZATION TIME OF FLIGHT MASS SPECTROMETRY; MAXIMUM PLASMA CONCENTRATION; MOLECULE; NONHUMAN; NUCLEAR MAGNETIC RESONANCE; PHARMACOPHORE; PROTEIN CONFORMATION; PROTEIN PROTEIN INTERACTION; PROTEOMICS; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION; WISTAR RAT; ANIMAL; CHEMISTRY; DRUG EFFECTS; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; METABOLISM; ORAL DRUG ADMINISTRATION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-HIV AGENTS; ANTIGENS, CD4; BINDING SITES; DRUG DESIGN; HIV ENVELOPE PROTEIN GP120; HIV-1; HUMANS; MACROCYCLIC COMPOUNDS; MALE; PROTEIN BINDING; RATS; RATS, WISTAR;

HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1; RATTUS;

EID: 77955422125     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2010.04.053     Document Type: Article

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