Extension into the entrance channel of HIV-1 reverse transcriptase-Crystallography and enhanced solubility.

Bollini M, Frey KM, Cisneros JA, Spasov KA, Das K, Bauman JD, Arnold E, Anderson KS, Jorgensen WL
Bioorganic & medicinal chemistry letters (2013)
PubMed entry Publisher's site

Abstract:

Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are ...
Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that feature extension into the entrance channel near Glu138. Complexes of the parent anilinylpyrimidine 1 and the morpholinoethoxy analog 2j with HIV-RT have received crystallographic characterization confirming the designs. Measurement of aqueous solubilities of 2j, 2k, the parent triazene 2a, and other NNRTIs demonstrate profound benefits for addition of the morpholinyl substituent.

Polymerases:

HIV RT

Topics:

Structure and Structure/Function

Status:

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Version:20241007

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