Bifunctional anti-human immunodeficiency virus type 1 small molecules with two novel mechanisms of action.
A class of betulinic acid derivatives was synthesized to target two critical steps in the human immunodeficiency virus type 1 (HIV-1) replication cycle, entry and maturation. Each mechanism of HIV-1 inhibition is distinct from clinically available anti-HIV therapeutics. The viral determinants of the antientry and antimaturation activities are the bridging sheet of HIV-1 gp120 and the P24/p2 cleavage site, respectively.
Huang
Li
L
Department of Surgery, Duke University Medical Center, Durham, North Carolina 27710, USA.
Yuan
Xiong
X
Aiken
Christopher
C
Chen
Chin Ho
CH
D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019556:COS Cells; D002522:Chlorocebus aethiops; D016655:HIV Core Protein p24 / Q000187:drug effects; D015699:HIV Envelope Protein gp120 / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects* / Q000254:growth & development; D053978:Pentacyclic Triterpenes; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D014779:Virus Replication / Q000187:drug effects; D000094062:Betulinic Acid
D019380:Anti-HIV Agents; D016655:HIV Core Protein p24; D015699:HIV Envelope Protein gp120; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D000094062:Betulinic Acid