Transcription of TG-1601 is a novel BET inhibitor with strong binding ...
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TG-1601 is a novel BET inhibitor with strong binding ...
5790. < strong >TG-1601strong > is a < strong >novelstrong > BET < strong >inhibitorstrong > with strong < strong >bindingstrong > affinity and long-lasting effect in preclinical models Emmanuel Normant1, Leonid Gorelik2, Rama Shmeis1, Henry Le1, Robert Nisch1, Karen TenHuisen1, Teja Turpuseema1, James Oliviero2, Dhanalakshmi Sivanandhan3, Payal Kiran Parikh3, Hari P. Miskin1, Peter Sportelli1 and Michael S. Weiss1. 1) TG Therapeutics, New York, NY; 2) Checkpoint Therapeutics, New York, NY, 3) Jubilant Biosys, Bangalore, India Background In vitro and in vivo Pharmacodynamic activity In vivo anti-tumor activity Pharmacodynamic markers BET (bromodomain and extra-terminal) proteins bind to acetylated Kd (nM) In vitro pharmacodynamic activity of < strong >TG-1601strong > In vivo anti-tumor activity in MM1s multiple myeloma model In vivo and ex-vivo validation of CCR2 and IL1RN. lysine residues on chromatin and participate in the regulation of gene < strong >TG-1601strong > and two related BET inhibitors transcription. Inhibition of BET protein < strong >bindingstrong > to chromatin with small bromodomain < strong >TG-1601strong > JQ1 OTX-015.
TG-) TG-1601 (µM) –24h TG-1601 (µM) TG-1601 (µM) TG-1601 (µM) TG-1601 is a novel BET inhibitor with strong binding affinity and long-lasting effect in preclinical models
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