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Systematic identification of genomic markers of drug sensitivity in cancer cells
TLDR
It was found that mutated cancer genes were associated with cellular response to most currently available cancer drugs, and systematic pharmacogenomic profiling in cancer cell lines provides a powerful biomarker discovery platform to guide rational cancer therapeutic strategies. Expand
A Landscape of Pharmacogenomic Interactions in Cancer
TLDR
It is reported how cancer-driven alterations identified in 11,289 tumors from 29 tissues can be mapped onto 1,001 molecularly annotated human cancer cell lines and correlated with sensitivity to 265 drugs. Expand
Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer.
TLDR
Findings suggest that gain-of-function mutations in DDR2 are important oncogenic events and are amenable to therapy with dasatinib, and provide a rationale for designing clinical trials with the FDA-approved drug d asatinib in patients with lung SCCs. Expand
Characterization of a selective inhibitor of the Parkinson’s disease kinase LRRK2
TLDR
It is demonstrated that inhibition of LRRK2 induces dephosphorylation of Ser910/Ser935 and accumulation of L RRK2 within aggregate structures, which will serve as a versatile tool to pharmacologically interrogate LRRk2 biology and study its role in Parkinson’s disease. Expand
Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors
TLDR
The results show that therapeutically relevant inhibition of Bcr–Abl activity can be achieved with inhibitors that bind to the myristate-binding site and that combining allosteric and ATP-competitive inhibitors can overcome resistance to either agent alone. Expand
Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.
TLDR
A small-molecule inhibitor of the kinase activity of BMK1, XMD8-92, blocked tumor cell proliferation in vitro and significantly inhibited tumor growth in vivo by 95%, demonstrating the efficacy and tolerability ofBMK1-targeted cancer treatment in animals. Expand
Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders
TLDR
Treatment with CY-09 shows remarkable therapeutic effects on mouse models of cryopyrin-associated autoinflammatory syndrome (CAPS) and type 2 diabetes and indicates that NLRP3 can be targeted in vivo to combatNLRP3-driven diseases. Expand
Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration
TLDR
The pharmacological modulation of MST1/2 kinase activities provides a novel approach to potentiate tissue repair and regeneration, with XMU-MP-1 as the first lead for the development of targeted regenerative therapeutics. Expand
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
TLDR
The discovery and characterization of 2-arylmethyloxy-5-subtitutent-N-arylbenzamides with potent LRRK2 activities exemplified by GSK2578215A which exhibits biochemical IC(50)s of around 10 nM against both wild-type L RRK2 and the G2019S mutant. Expand
Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases
TLDR
The results of the present study indicate that WZ4003 and HTH-01-015 will serve as useful chemical probes to delineate the biological roles of the NUAK kinases. Expand
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