Selected Scientific Publications

Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer’s disease model
Spangenberg E, et al. Nat Commun. 2019 Aug 21;10(1):3758. doi: 10.1038/s41467-019-11674-z.

RAF inhibitor PLX8394 selectively disrupts BRAF dimers and RAS-independent BRAF-mutant-driven signaling
Yao Z, et al. Nat Med. 2019 Feb;25(2):284-291. doi: 10.1038/s41591-018-0274-5.

BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor
Ozer HG, et al. Cancer Discov. 2018 Apr;8(4):458-477. doi: 10.1158/2159-8290.CD-17-0902. E

RAF inhibitors that evade paradoxical MAPK pathway activation
Zhang C, et al. Nature. 2015 Oct 22;526(7574):583-6. doi: 10.1038/nature14982.

Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor
Tap WD, et al. N Engl J Med. 2015 Jul 30;373(5):428-37. doi: 10.1056/NEJMoa1411366.

Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 “Gatekeeper” F691L Mutation with PLX3397
Smith CC, et al. Cancer Discov. 2015 Jun;5(6):668-79. doi: 10.1158/2159-8290.CD-15-0060.

Colony-stimulating factor 1 receptor signaling is necessary for microglia viability, unmasking a microglia progenitor cell in the adult brain
Elmore MR, et al. Neuron. 2014 Apr 16;82(2):380-97. doi: 10.1016/j.neuron.2014.02.040.

Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor
Zhang C, et al. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94. doi: 10.1073/pnas.1219457110.

Vemurafenib: the first drug approved for BRAF-mutant cancer
Bollag G, et al. Nat Rev Drug Discov. 2012 Nov;11(11):873-86. doi: 10.1038/nrd3847.

RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors
Su F, et al. N Engl J Med. 2012 Jan 19;366(3):207-15. doi: 10.1056/NEJMoa1105358.

Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy
DeNardo DG, et al. Cancer Discov. 2011 Jun;1(1):54-67. doi: 10.1158/2159-8274.CD-10-0028.

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF
Poulikakos PI, et al. Nature. 2010 Mar 18;464(7287):427-30. doi: 10.1038/nature08902.

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma
Bollag G, et al. Nature. 2010 Sep 30;467(7315):596-9. doi: 10.1038/nature09454.

Scaffold-based design of kinase inhibitors for cancer therapy
Zhang C, et al. Curr Opin Genet Dev. 2010 Feb;20(1):79-86. doi: 10.1016/j.gde.2009.10.010.

Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent
Artis DR, et al. Proc Natl Acad Sci U S A. 2009 Jan 6;106(1):262-7. doi: 10.1073/pnas.0811325106.

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
Tsai J, et al. Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6. doi: 10.1073/pnas.0711741105.

Structural characterization of autoinhibited c-Met kinase produced by coexpression in bacteria with phosphatase
Wang W, et al. Proc Natl Acad Sci U S A. 2006 Mar 7;103(10):3563-8. doi: 10.1073/pnas.0600048103.

The crystal structures of human steroidogenic factor-1 and liver receptor homologue-1
Wang W, et al. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7505-10. doi: 10.1073/pnas.0409482102.

Crystal structures of proto-oncogene kinase Pim1: a target of aberrant somatic hypermutations in diffuse large cell lymphoma
Kumar A, et al. J Mol Biol. 2005 Apr 22;348(1):183-93. doi: 10.1016/j.jmb.2005.02.039.

A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Card GL, et al. Nat Biotechnol. 2005 Feb;23(2):201-7. doi: 10.1038/nbt1059.

A glutamine switch mechanism for nucleotide selectivity by phosphodiesterases
Zhang KY, et al. Mol Cell. 2004 Jul 23;15(2):279-86. doi: 10.1016/j.molcel.2004.07.005.

 

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