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Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT
Masitinib is a potent and selective tyrosine kinase inhibitor targeting KIT that is active, orally bioavailable in vivo, and has low toxicity.
Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells
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.
Discovery of specific inhibitors of human USP7/HAUSP deubiquitinating enzyme.
Selective Sirt2 inhibition by ligand-induced rearrangement of the active site
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.
Structure–Activity Studies on Suramin Analogues as Inhibitors of NAD+‐Dependent Histone Deacetylases (Sirtuins)
- Johannes Trapp, René Meier, Darunee Hongwiset, M. Kassack, W. Sippl, M. Jung
- Chemistry, BiologyChemMedChem
- 8 October 2007
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.
Regulation of G2/M Transition by Inhibition of WEE1 and PKMYT1 Kinases
- Matthias Schmidt, A. Rohe, Charlott Platzer, A. Najjar, F. Erdmann, W. Sippl
- 23 November 2017
In the cell cycle, there are two checkpoint arrests that allow cells to repair damaged DNA in order to maintain genomic integrity and inhibition by a small molecule inhibitor is proposed to be a promising option since WEE kinases bind Cdk1, altering equilibria and thus affecting G2/M transition.
AfroDb: A Select Highly Potent and Diverse Natural Product Library from African Medicinal Plants
The results prove that drug discovery, beginning with natural products from the African flora, could be highly promising and the 3D structures are available and could be useful for virtual screening and natural product lead generation programs.
Activation, regulation, and inhibition of DYRK1A
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.
The Emerging Therapeutic Potential of Histone Methyltransferase and Demethylase Inhibitors
- Astrid Spannhoff, Alexander-Thomas Hauser, R. Heinke, W. Sippl, M. Jung
- 5 October 2009
An overview of the mechanisms of action of histone methyltransferases and demethylases, their role in the formation of certain diseases, and available inhibitors is given.
Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo
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.