Human immunodeficiency virus (HIV) reverse transcriptase (RT)-associated ribonuclease H (RNase H) remains the only virally encoded enzymatic function yet to be exploited as an antiviral target. One of the possible challenges may be that targeting HIV RNase H is confronted with a steep substrate barrier. We have previously reported a 3-hydroxypyrimidine-2,4-dione (HPD) subtype that potently and selectively inhibited RNase H without inhibiting HIV in cell culture. We report herein a critical redesign of the HPD chemotype featuring an additional wing at the C5 position that led to drastically improved RNase H inhibition and significant antiviral activity. Structure–activity relationship (SAR) concerning primarily the length and flexibility of ...
Targeting the clinically unvalidated reverse transcriptase (RT) associated ribonuclease H (RNase H) ...
The HIV-1 genomic RNA reverse transcription is an essential step in the virus cycle carried out by t...
The HIV-1 genomic RNA reverse transcription is an essential step in the virus cycle carried out by t...
Human immunodeficiency virus (HIV) reverse transcriptase (RT) associated ribonuclease H (RNase H) re...
Multiple combinations of antiretroviral drugs have remarkably improved the treatment of HIV-1 infect...
Background. The HIV-1 RT has two associated activities: i) the DNA polymerase activity (both RNA and...
Since the human immunodeficiency virus (HIV) was discovered as the etiological agent of acquired imm...
Background. The HIV-1 RT has two associated activities: i) the DNA polymerase activity (both RNA and...
Persistent HIV infection requires lifelong treatment and among the 2.1 million new HIV infections th...
The current HIV-1 therapy, the Highly Active Antiretroviral Treatment (HAART), consists of a cocktai...
The current HIV-1 therapy, the Highly Active Antiretroviral Treatment (HAART), consists of a cocktai...
Persistent HIV infection requires lifelong treatment and among the 2.1 million new HIV infections th...
We tested three compounds for their ability to inhibit the RNase H (RH) and polymerase activities of...
Reverse transcriptase (RT) associated ribonuclease H (RNase H) remains the only virally encoded enzy...
Despite great efforts have been made in the prevention and therapy of human immunodeficiency virus (...
Targeting the clinically unvalidated reverse transcriptase (RT) associated ribonuclease H (RNase H) ...
The HIV-1 genomic RNA reverse transcription is an essential step in the virus cycle carried out by t...
The HIV-1 genomic RNA reverse transcription is an essential step in the virus cycle carried out by t...
Human immunodeficiency virus (HIV) reverse transcriptase (RT) associated ribonuclease H (RNase H) re...
Multiple combinations of antiretroviral drugs have remarkably improved the treatment of HIV-1 infect...
Background. The HIV-1 RT has two associated activities: i) the DNA polymerase activity (both RNA and...
Since the human immunodeficiency virus (HIV) was discovered as the etiological agent of acquired imm...
Background. The HIV-1 RT has two associated activities: i) the DNA polymerase activity (both RNA and...
Persistent HIV infection requires lifelong treatment and among the 2.1 million new HIV infections th...
The current HIV-1 therapy, the Highly Active Antiretroviral Treatment (HAART), consists of a cocktai...
The current HIV-1 therapy, the Highly Active Antiretroviral Treatment (HAART), consists of a cocktai...
Persistent HIV infection requires lifelong treatment and among the 2.1 million new HIV infections th...
We tested three compounds for their ability to inhibit the RNase H (RH) and polymerase activities of...
Reverse transcriptase (RT) associated ribonuclease H (RNase H) remains the only virally encoded enzy...
Despite great efforts have been made in the prevention and therapy of human immunodeficiency virus (...
Targeting the clinically unvalidated reverse transcriptase (RT) associated ribonuclease H (RNase H) ...
The HIV-1 genomic RNA reverse transcription is an essential step in the virus cycle carried out by t...
The HIV-1 genomic RNA reverse transcription is an essential step in the virus cycle carried out by t...