Yves Pommier

TL;DR: The development of SBPs for topoisomerase I, an anticancer target with an unusual ligand binding pocket consisting of protein and DNA atoms is presented and it is revealed that the choice of pharmacophore feature clustering and selection methods has a large impact on the virtual screening hit lists.

TL;DR: This work systematically study the antitumor activity of CYB-L10, a novel indolizinoquinolinedione TOP1 catalytic inhibitor discovered in the laboratory that mainly acts on TOP1 in cancer cells and is not a substrate of the P-glycoprotein.

TL;DR: The quinoline inhibitors are oxoquinolines of the following formula (I) that can be used for preventing or treating AIDS or HIV infection in a subject as mentioned in this paper, wherein Z is selected from -C(O)OR2 then at least one of R3, R4, R5 or R6 is -C (O)CH2C( O)X and wherein R1, R2, R3 and R4 are as disclosed herein.

TL;DR: A four-step total synthesis of lu serotonin is deployed to make a small library of AB-ring substituted analogues, which show weak activity in a standard topoisomerase I mediated DNA cleavage assay.

TL;DR: The authors' studies indicate that 1 shows anti-HIV-1 activity in the low micromolar range and has pronounced gp120 binding and HIV-1 integrase inhibitory capacity, however, gp120binding rather than integrase inhibition seems to be the primary mechanism of antiviral activity of 1.