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Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT
TLDR
Masitinib is a potent and selective tyrosine kinase inhibitor targeting KIT that is active, orally bioavailable in vivo, and has low toxicity. Expand
Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells
TLDR
HBX 41,108 is reported, a small-molecule compound that inhibits USP7 deubiquitinating activity with an IC50 in the submicromolar range, providing a structural basis for the development of new anticancer drugs. Expand
Discovery of specific inhibitors of human USP7/HAUSP deubiquitinating enzyme.
TLDR
The data presented in this report provide proof of principle that USP7 inhibitors may be a valuable therapeutic for cancer and the discovery of such molecules offers interesting tools for studying deubiquitination. Expand
Structure–Activity Studies on Suramin Analogues as Inhibitors of NAD+‐Dependent Histone Deacetylases (Sirtuins)
TLDR
A diverse set of suramin analogues were tested to elucidate the inhibition of the NAD+‐dependent histone deacetylases SIRT1 and SIRT2 and selective inhibitors of human sirtuins with potency in the two‐digit nanomolar range were discovered. Expand
Activation, regulation, and inhibition of DYRK1A
TLDR
The current knowledge about the initial self‐activation of DYRK1A by tyrosine autophosphorylation is reviewed and it is proposed that this mechanism presents an ancestral feature of the CMGC group of kinases. Expand
Target-based approach to inhibitors of histone arginine methyltransferases.
TLDR
Employing a fungal PRMT for screening and a human enzyme for validation, the first target-based approach to protein arginine methyltransferase (PRMT) inhibitors is presented, identifying seven inhibitors of PRMTs in vitro. Expand
Inhibitors to understand molecular mechanisms of NAD(+)-dependent deacetylases (sirtuins).
TLDR
An overview of the many sirtuin inhibitors that have provided insight into the biological role of sirtuins is presented. Expand
Selective Sirt2 inhibition by ligand-induced rearrangement of the active site
TLDR
High-resolution structures of human Sirt2 in complex with highly selective drug-like inhibitors that show a unique inhibitory mechanism are presented and structural insights into this unique mechanism of selective sirtuin inhibition provide the basis for further inhibitor development and selective tools for sIRTuin biology. Expand
Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo
TLDR
It is shown that two selected pyridoisothiazolone HAT inhibitors, PU139 and PU141, induce cellular histone hypoacetylation and inhibit growth of several neoplastic cell lines originating from different tissues. Expand
Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition.
TLDR
This work presents a systematic approach using adenosine mimics from one cofactor class (kinase inhibitors) as a viable method to generate new lead structures in another co Factor class (sirtuin inhibitors) that has broad implications for medicinal chemistry and specifically for sirtuin inhibitor design. Expand
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