Featured Publications
Structural insights into the recognition of nucleoside reverse transcriptase inhibitors by HIV‐1 reverse transcriptase: First crystal structures with reverse transcriptase and the active triphosphate forms of lamivudine and emtricitabine
Bertoletti N, Chan AH, Schinazi RF, Yin YW, Anderson KS. Structural insights into the recognition of nucleoside reverse transcriptase inhibitors by HIV‐1 reverse transcriptase: First crystal structures with reverse transcriptase and the active triphosphate forms of lamivudine and emtricitabine. Protein Science 2019, 28: 1664-1675. PMID: 31301259, PMCID: PMC6699100, DOI: 10.1002/pro.3681.Peer-Reviewed Original ResearchConceptsHIV-1Severe drug toxicityActive antiretroviral therapySuccessful treatment regimenMajor health issueActive triphosphate formHIV-1 drugsReverse transcriptaseHIV-1 reverse transcriptaseAntiretroviral therapyOff-target side effectsTreatment regimenRetroviruses HIV-1Drug toxicityReverse transcriptase enzymeSide effectsRT inhibitorsNew infectionsViral replicationHealth issuesTarget toxicityTriphosphate formNext-generation therapeuticsNRTIsTranscriptase enzyme
2019
Mutational and structural studies uncover crucial amino acids determining activity and stability of 17β-HSD14
Badran M, Bertoletti N, Keils A, Heine A, Klebe G, Marchais-Oberwinkler S. Mutational and structural studies uncover crucial amino acids determining activity and stability of 17β-HSD14. The Journal Of Steroid Biochemistry And Molecular Biology 2019, 189: 135-144. PMID: 30836176, DOI: 10.1016/j.jsbmb.2019.02.009.Peer-Reviewed Original ResearchConceptsAmino acidsAdjacent monomersSite-directed mutagenesisCrucial amino acidsIndividual amino acidsEnzymatic functionCatalytic triadEnzyme variantsActive siteTerminal loopPresence of NADDisulfide bridgesNeighboring monomerCatalytic centerX-ray crystallographyDimer formationEnzyme kineticsStructural studiesTyr253His93Gln148EnzymeLatter interactionCys255Type 14