HAL will be down for maintenance from Friday, June 10 at 4pm through Monday, June 13 at 9am. More information
Skip to Main content Skip to Navigation
Journal articles

The inhibition process of HIV-1 integrase by diketoacids molecules: Understanding the factors governing the better efficiency of dolutegravir

Abstract : The Human Immunodeficiency Virus-1 integrase is responsible for the covalent insertion of a newly synthesized double-stranded viral DNA into the host cells, and is an emerging target for antivirus drug design. Raltegravir (RAL) and elvitegravir (EVG) are the first two integrase strand transfer inhibitors used in therapy. However, treated patients eventually develop detrimental resistance mutations. By contrast, a recently approved drug, dolutegravir (DTG), presents a high barrier to resistance. This study aims to understand the increased efficiency of DTG upon focusing on its interaction properties with viral DNA. The results showed DTG to be involved in more extended interactions with viral DNA than EVG. Such interactions involve the halobenzene and scaffold of DTG and EVG and bases 5′G-43′, 3′A35'and 3′C45’.
Complete list of metadata

Cited literature [19 references]  Display  Hide  Download

https://hal.sorbonne-universite.fr/hal-01520237
Contributor : Gestionnaire Hal-Upmc Connect in order to contact the contributor
Submitted on : Wednesday, May 10, 2017 - 10:33:52 AM
Last modification on : Thursday, March 31, 2022 - 8:20:02 AM
Long-term archiving on: : Friday, August 11, 2017 - 12:27:33 PM

File

El_Khoury_The_inhibition.pdf
Files produced by the author(s)

Identifiers

Citation

Léa El Khoury, Jean-Philip Piquemal, Serge Fermandjian, Richard G. Maroun, Nohad Gresh, et al.. The inhibition process of HIV-1 integrase by diketoacids molecules: Understanding the factors governing the better efficiency of dolutegravir. Biochemical and Biophysical Research Communications, Elsevier, 2017, ⟨10.1016/j.bbrc.2017.05.001⟩. ⟨hal-01520237⟩

Share

Metrics

Record views

250

Files downloads

215