An NNRTI and active metabolite of elsulfavirine
Ro 0335 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and an active metabolite of the antiviral prodrug elsulfavirine.1 It inhibits HIV-1 reverse transcriptase in a cell-free assay and the replication of HIV-1 in MT-4 cells (IC50s = 8.1 and 1.1 nM, respectively). Ro 0335 also selectively inhibits human carbonic anhydrase VII (CAVII; Ki = 9.7 nM) over human CAI and CAIII-VI (Kis = >125 nM for all) but also inhibits human CAII, CAIX, CAXII, CAXIII, and CAXIV (Kis = 35.5, 72.1, 62.3, 52.2, and 15.4 nM, respectively).2
1.Javanbakht, H., Ptak, R., G., Chow, E., et al.In vitro resistance development for RO-0335, a novel diphenylether nonnucleoside reverse transcriptase inhibitorAntiviral Res.86(2)212-219(2010) 2.Supuran, C.T., Nocentini, A., Yakubova, E., et al.Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida?) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoformsJ. Enzyme Inhib. Med. Chem.36(1)1056-1060(2021)
动态评分
0.0