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Vorinostat interferes with the signaling transduction pathway of T-cell receptor and synergizes with phosphoinositide-3 kinase inhibitors in cutaneous T-cell lymphoma
Background Vorinostat (suberoylanilide hydroxamic acid, SAHA), an inhibitor of class I and II histone deacetylases, has been approved for the treatment of cutaneous T-cell lymphoma. In spite ofExpand
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Abstract A275: Co-targeting PIM and PI3K/mTOR pathways with a single molecule: Novel orally available combined PIM/PI3K and PIM/PI3K/mTOR kinase inhibitors.
The PI3K/AKT pathway is commonly activated in human cancer. Multiple small-molecule inhibitors have been developed to target PI3K/mTOR or AKT kinases, but the efficacy of these drugs is compromisedExpand
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Abstract 4524: Combined inhibition of PIM and PI3 kinases shows an enhanced efficacy in a number of solid tumour cell lines
Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA Introduction: PIM kinases play an important role in a number of aspects of the regulation of cell cycle and proliferation. OverExpand
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Abstract 4337: Novel potent and selective orally available CDK8/19 kinase inhibitors
CDK8 and its paralog CDK19 are cyclin-dependent kinases and together with CDK7 and CDK9 belongs to the group of C-terminal domain (CTD) kinases that phosphorylate the CTD of RNA polymerase II, thusExpand
Abstract B228: Discovery of 6-Methyl-3-aryl-7,8-dihydro-6H-9-oxa-1,2,3a,4,6-pentaaza-cyclopenta[a]naphthalen-5-ylamine compounds as Pim kinase inhibitors with potent activity in tumoral cell lines
Proviral integration site for Moloney murine leukemia virus (PIM) kinases are potent oncogens. Pim-1, 2 and 3 are highly conserved kinases that have unique structural properties, and areExpand
Dérivés de triazolo[4,3-b]pyridazines au cycle 6,7 fusionné utilisés en tant qu'inhibiteurs de pim
L'invention concerne des composes de formule I, dans laquelle R 1 , R 2 , R 3 et R 4 (et la fraction -CH 2 -CH 2 ) ont les significations donnees dans la description, et des esters, amides, solvatesExpand
Composés bicycliques destinés à être utilisés en tant qu'inhibiteurs de kinases
L'invention concerne des composes de formule (I), dans laquelle R 1 , R 2 , R 3 et R 4 ont les significations proposees dans la description, et leurs esters, amides, solvates ou selsExpand
Abstract B227: Discovery of 3-aryl-3H-[1,2,3]triazolo[4,5-b]pyridin-5-ylamine compounds as potent, selective and orally bioavailable inhibitors of PIM kinases.
The PIM family of serine/threonine kinases (PIM-1, 2 and 3) has been originally identified as proviral integration sites involved in lymphomagenesis induced by murine leukemia virus. In almost all ofExpand