Associated Papers
Cryo-EM structures of CRAF/MEK1/14-3-3 complexes in autoinhibited and open-monomer states reveal features of RAF regulation.
Jang DM et al.
Nature Communications, 2025
A first-in-class Wiskott-Aldrich syndrome protein activator with antitumor activity in hematologic cancers.
Spriano F et al.
Haematologica, 2024
Strain-release alkylation of Asp12 enables mutant selective targeting of K-Ras-G12D.
Zheng Q et al.
Nature Chemical Biology, 2024
The Pan-RAF-MEK Nondegrading Molecular Glue NST-628 Is a Potent and Brain-Penetrant Inhibitor of the RAS-MAPK Pathway with Activity across Diverse RAS- and RAF-Driven Cancers.
Ryan MB et al.
Cancer Discovery, 2024
Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390.
Pike KG et al.
Journal of Medicinal Chemistry, 2024
Structural Basis for Highly Selective Class II Alpha Phosphoinositide-3-Kinase Inhibition.
Kücükdisli M et al.
Journal of Medicinal Chemistry, 2023
Discovery and Optimization of the First ATP Competitive Type-III c-MET Inhibitor.
Michaelides IN et al.
Journal of Medicinal Chemistry, 2023
An atlas of substrate specificities for the human serine/threonine kinome.
Johnson JL et al.
Nature, 2023
Discovery of 1H-Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors.
Leśniak RK et al.
Acs Medicinal Chemistry Letters, 2022
Phosphoproteome Profiling of the Receptor Tyrosine Kinase MuSK Identifies Tyrosine Phosphorylation of Rab GTPases.
Budayeva HG et al.
Molecular & Cellular Proteomics : Mcp, 2022
Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
Collie GW et al.
Acs Medicinal Chemistry Letters, 2021
A-loop interactions in Mer tyrosine kinase give rise to inhibitors with two-step mechanism and long residence time of binding.
Pflug A et al.
The Biochemical Journal, 2020
RAF inhibitors promote RAS-RAF interaction by allosterically disrupting RAF autoinhibition.
Jin T et al.
Nature Communications, 2017
Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations.
Johnson AR et al.
Acs Chemical Biology, 2016
Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling.
Dhawan NS et al.
Nature, 2016
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
Johnson TW et al.
Journal of Medicinal Chemistry, 2014
Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions.
King AJ et al.
Plos One, 2013
Differential sensitivity of melanoma cell lines with differing B-Raf mutational status to the new oncogenic B-Raf kinase inhibitor UI-152.
Kim YK et al.
Cancer Letters, 2012
The C-terminus of Raf-1 acts as a 14-3-3-dependent activation switch.
Dhillon AS et al.
Cellular Signalling, 2009
Raf-1: a novel cardiac troponin T kinase.
Pfleiderer P et al.
Journal of Muscle Research and Cell Motility, 2009
Characterization of Ser338 phosphorylation for Raf-1 activation.
Zang M et al.
The Journal of Biological Chemistry, 2008
CK2 Is a component of the KSR1 scaffold complex that contributes to Raf kinase activation.
Ritt DA et al.
Current Biology : Cb, 2007
Regulation of RKIP binding to the N-region of the Raf-1 kinase.
Park S et al.
Febs Letters, 2006
Rheb inhibits C-raf activity and B-raf/C-raf heterodimerization.
Karbowniczek M et al.
The Journal of Biological Chemistry, 2006
Regulation of the Raf-MEK-ERK pathway by protein phosphatase 5.
von Kriegsheim A et al.
Nature Cell Biology, 2006
A phosphatase holoenzyme comprised of Shoc2/Sur8 and the catalytic subunit of PP1 functions as an M-Ras effector to modulate Raf activity.
Rodriguez-Viciana P et al.
Molecular Cell, 2006
Raf kinase inhibitory protein regulates Raf-1 but not B-Raf kinase activation.
Trakul N et al.
The Journal of Biological Chemistry, 2005
Identification of residues and domains of Raf important for function in vivo and in vitro.
Harding A et al.
The Journal of Biological Chemistry, 2003
The requirement of specific membrane domains for Raf-1 phosphorylation and activation.
Carey KD et al.
The Journal of Biological Chemistry, 2003
Phosphorylation of 338SSYY341 regulates specific interaction between Raf-1 and MEK1.
Xiang X et al.
The Journal of Biological Chemistry, 2002
Characterization of Raf-1 activation in mitosis.
Laird AD et al.
The Journal of Biological Chemistry, 1999
Mutations of critical amino acids affect the biological and biochemical properties of oncogenic A-Raf and Raf-1.
Bosch E et al.
Oncogene, 1997
Activity of plasma membrane-recruited Raf-1 is regulated by Ras via the Raf zinc finger.
Roy S et al.
The Journal of Biological Chemistry, 1997
Mechanisms regulating Raf-1 activity in signal transduction pathways.
Morrison DK
Molecular Reproduction and Development, 1995