From cycloheptathiophene-3-carboxamide to oxazinone-based derivatives as allosteric HIV-1 ribonuclease H inhibitors [PDF]
The paper focussed on a step-by-step structural modification of a cycloheptathiophene-3-carboxamide derivative recently identified by us as reverse transcriptase (RT)-associated ribonuclease H (RNase H) inhibitor.
Serena Massari +12 more
doaj +2 more sources
Ribonuclease H1 (RNase H) enzymes are well-conserved endonucleases that are present in all domains of life and are particularly important in the life cycle of retroviruses as domains within reverse transcriptase.
Kate A. Stafford, Arthur G. Palmer III
doaj +2 more sources
Scaffold hopping and optimisation of 3’,4’-dihydroxyphenyl- containing thienopyrimidinones: synthesis of quinazolinone derivatives as novel allosteric inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H [PDF]
Bioisosteric replacement and scaffold hopping are powerful strategies in drug design useful for rationally modifying a hit compound towards novel lead therapeutic agents.
Graziella Tocco +8 more
doaj +2 more sources
The folding and unfolding behavior of ribonuclease H on the ribosome. [PDF]
Jensen MK +4 more
europepmc +3 more sources
Evidence from molecular dynamics simulations of conformational preorganization in the ribonuclease H active site [v1; ref status: indexed, http://f1000r.es/2z7] [PDF]
Ribonuclease H1 (RNase H) enzymes are well-conserved endonucleases that are present in all domains of life and are particularly important in the life cycle of retroviruses as domains within reverse transcriptase.
Kate A. Stafford, Arthur G. Palmer III
doaj +2 more sources
A mid-throughput HBV replication inhibition assay capable of detecting ribonuclease H inhibitors. [PDF]
Li Q, Edwards TC, Ponzar NL, Tavis JE.
europepmc +3 more sources
HIV-1 Reverse Transcriptase Polymerase and RNase H (Ribonuclease H) Active Sites Work Simultaneously and Independently. [PDF]
Li A, Li J, Johnson KA.
europepmc +3 more sources
Atomistic details of the phosphodiester cleavage of ribonuclease H [PDF]
Elsässer B, Fels G
doaj +2 more sources
Purification and enzymatic characterization of the hepatitis B virus ribonuclease H, a new target for antiviral inhibitors. [PDF]
Villa JA +6 more
europepmc +2 more sources
Hydroxylated tropolones inhibit hepatitis B virus replication by blocking viral ribonuclease H activity. [PDF]
Lu G +13 more
europepmc +3 more sources

