publication . Article . 2000

The role of steric hindrance in 3TC resistance of human immunodeficiency virus type-1 reverse transcriptase 1 1Edited by A. R. Fersht

Gao, Hong-Qiang; Boyer, Paul L; Sarafianos, Stefan G; Arnold, Edward; Hughes, Stephen H;
Open Access
  • Published: 01 Jan 2000
  • Publisher: Elsevier BV
Abstract
Treating HIV infections with drugs that block viral replication selects for drug-resistant strains of the virus. Particular inhibitors select characteristic resistance mutations. In the case of the nucleoside analogs 3TC and FTC, resistant viruses are selected with mutations at amino acid residue 184 of reverse transcriptase (RT). The initial change is usually to M184I; this virus is rapidly replaced by a variant carrying the mutation M184V. 3TC and FTC are taken up by cells and converted into 3TCTP and FTCTP. The triphosphate forms of these nucleoside analogs are incorporated into DNA by HIV-1 RT and act as chain terminators. Both of the mutations, M184I and M1...
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free text keywords: Molecular Biology, Structural Biology, Biology, Mutation, medicine.disease_cause, medicine, RNase H, biology.protein, Resistance mutation, Polymerase, Nucleoside triphosphate, chemistry.chemical_compound, chemistry, Biochemistry, Molecular biology, Binding site, Reverse transcriptase, Nucleoside analogue, medicine.drug
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