105356-66-9Relevant academic research and scientific papers
Slow-binding inhibition of 2-keto-3-deoxy-6-phosphogluconate (KDPG) aldolase
Braga, Remi,Hecquet, Laurence,Blonski, Casimir
, p. 2965 - 2972 (2004)
2-Keto-3-deoxy-6-phosphogluconate (KDPG) aldolase is a key enzyme in the Entner-Doudoroff pathway of bacteria. It catalyzes the reversible production of KDPG from pyruvate and D-glyceraldehyde 3-phosphate through a class I Schiff base mechanism. On the basis of aldolase mechanistic pathway, various pyruvate analogues bearing β-diketo structures were designed and synthesized as potential inhibitors. Their capacity to inhibit aldolase catalyzed reaction by forming stabilized iminium ion or conjugated enamine were investigated by enzymatic kinetics and UV-vis difference spectroscopy. Depending of the substituent R (methyl or aromatic ring), a competitive or a slow-binding inhibition takes place. These results were examined on the basis of the three-dimensional structure of the enzyme.
SMALL MOLECULES FOR DISRUPTING THE SUPER ELONGATION COMPLEX AND INHIBITING TRANSCRIPTION ELONGATION FOR CANCER THERAPY
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, (2019/10/15)
Disclosed are compounds which may be utilized to inhibit transcription by RNA Polymerase II (Pol II), and in particular to disrupt the Super Elongation Complex (SEC). The compounds may be utilized in pharmaceutical compositions and methods for treating di
Targeting Processive Transcription Elongation via SEC Disruption for MYC-Induced Cancer Therapy
Liang, Kaiwei,Smith, Edwin R.,Aoi, Yuki,Stoltz, Kristen L.,Katagi, Hiroaki,Woodfin, Ashley R.,Rendleman, Emily J.,Marshall, Stacy A.,Murray, David C.,Wang, Lu,Ozark, Patrick A.,Mishra, Rama K.,Hashizume, Rintaro,Schiltz, Gary E.,Shilatifard, Ali
, p. 766 - 17,779 (2018/10/09)
The super elongation complex (SEC) is required for robust and productive transcription through release of RNA polymerase II (Pol II) with its P-TEFb module and promoting transcriptional processivity with its ELL2 subunit. Malfunction of SEC contributes to
