2017
Structural and Preclinical Studies of Computationally-Designed Non-nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection
Kudalkar SN, Beloor J, Chan AH, Lee WG, Jorgensen WL, Kumar P, Anderson KS. Structural and Preclinical Studies of Computationally-Designed Non-nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection. Molecular Pharmacology 2017, 91: mol.116.107755. PMID: 28167742, PMCID: PMC5363707, DOI: 10.1124/mol.116.107755.Peer-Reviewed Original ResearchConceptsNon-nucleoside reverse transcriptase inhibitorBALB/c miceReverse transcriptase inhibitorHIV infectionC miceTranscriptase inhibitorAntiviral activityCompound INew non-nucleoside reverse transcriptase inhibitorHIV-1 non-nucleoside reverse transcriptase inhibitorDetectable acute toxicityTreating HIV InfectionSingle intraperitoneal doseAnti-HIV-1 potencyMT-2 cellsDrug-resistant variantsCompound IISerum residence timeAnti-viral potencyHIV-1 RTClinical benefitClinical efficacyIntraperitoneal doseWild-type HIV-1 RTPlasma clearance
2012
Crystal Structures of HIV‑1 Reverse Transcriptase with Picomolar Inhibitors Reveal Key Interactions for Drug Design
Frey KM, Bollini M, Mislak AC, Cisneros J, Gallardo-Macias R, Jorgensen WL, Anderson KS. Crystal Structures of HIV‑1 Reverse Transcriptase with Picomolar Inhibitors Reveal Key Interactions for Drug Design. Journal Of The American Chemical Society 2012, 134: 19501-19503. PMID: 23163887, PMCID: PMC3518392, DOI: 10.1021/ja3092642.Peer-Reviewed Original ResearchSmall‐Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α
Buckley DL, Gustafson JL, Van Molle I, Roth AG, Tae HS, Gareiss PC, Jorgensen WL, Ciulli A, Crews CM. Small‐Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α. Angewandte Chemie International Edition 2012, 51: 11463-11467. PMID: 23065727, PMCID: PMC3519281, DOI: 10.1002/anie.201206231.Peer-Reviewed Original Research
2011
Efficient Discovery of Potent Anti-HIV Agents Targeting the Tyr181Cys Variant of HIV Reverse Transcriptase
Jorgensen WL, Bollini M, Thakur VV, Domaoal RA, Spasov KA, Anderson KS. Efficient Discovery of Potent Anti-HIV Agents Targeting the Tyr181Cys Variant of HIV Reverse Transcriptase. Journal Of The American Chemical Society 2011, 133: 15686-15696. PMID: 21853995, PMCID: PMC3183387, DOI: 10.1021/ja2058583.Peer-Reviewed Original ResearchConceptsHuman immunodeficiency virusWild-type HIV-1HIV-1Potent Anti-HIV AgentsInfected human T cellsNon-nucleoside reverseAnti-HIV AgentsHuman T cellsHIV reverse transcriptaseImmunodeficiency virusT cellsHIV RTViral strainsHIV agentsPresent reportReverse transcriptaseNM potencyCritical contributorPotential benefits