Elsulfavirine (R-1206) is an orally active human carbonic anhydrase ( carbonic anhydrase , CA ) inhibitor and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase ( NNRT ). Elsulfavirine also targets and blocks the interaction between adenylosuccinate lyase ( ADSL ) and insulin-induced gene proteins INSIG1/2 , blocks SREBP-1 -mediated de novo lipid synthesis, and inhibits the proliferation of liver cancer cells. The combination of Elsulfavirine and Lenvatinib ( HY-10981 ) produces a synergistic anti-tumor effect. Elsulfavirine is converted into the active metabolite VM1500A in vivo, blocks the DNA polymerase activity of reverse transcriptase , and inhibits HIV-1 replication. Elsulfavirine exhibits a K i of 1960 nM-52400 nM against human carbonic anhydrase isoforms including I, VII, VI, VA, VB, IX, XIII, XIV . Elsulfavirine is used in studies related to HIV-1 infection and liver cancer .
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