PubRank

Nathanael S Gray

Author PubWeight™ 265.73‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 Systematic identification of genomic markers of drug sensitivity in cancer cells. Nature 2012 15.91
2 An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem 2009 12.73
3 EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clin Cancer Res 2008 9.29
4 Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer 2009 9.26
5 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A 2007 8.23
6 Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 2009 7.05
7 Activating mutations in ALK provide a therapeutic target in neuroblastoma. Nature 2008 6.80
8 The mTOR-regulated phosphoproteome reveals a mechanism of mTORC1-mediated inhibition of growth factor signaling. Science 2011 6.75
9 Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res 2008 6.71
10 MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proc Natl Acad Sci U S A 2009 6.58
11 A unifying model for mTORC1-mediated regulation of mRNA translation. Nature 2012 6.44
12 DEPTOR is an mTOR inhibitor frequently overexpressed in multiple myeloma cells and required for their survival. Cell 2009 5.97
13 Rational design of inhibitors that bind to inactive kinase conformations. Nat Chem Biol 2006 5.03
14 In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. Proc Natl Acad Sci U S A 2008 4.80
15 Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer. Cancer Discov 2011 4.80
16 A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Res 2011 4.22
17 Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A 2006 3.83
18 Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature 2010 3.39
19 Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem 2013 3.27
20 Inhibitor-sensitive FGFR1 amplification in human non-small cell lung cancer. PLoS One 2011 3.23
21 Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat Struct Mol Biol 2008 3.18
22 The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers. Cancer Res 2010 3.16
23 Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol 2006 2.96
24 Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat Chem Biol 2011 2.91
25 mTORC1 phosphorylation sites encode their sensitivity to starvation and rapamycin. Science 2013 2.71
26 In situ kinase profiling reveals functionally relevant properties of native kinases. Chem Biol 2011 2.69
27 An efficient rapid system for profiling the cellular activities of molecular libraries. Proc Natl Acad Sci U S A 2006 2.51
28 Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discov 2012 2.47
29 Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway-dependent and PI3K pathway-independent mechanisms. Nat Med 2011 2.34
30 A general strategy for creating "inactive-conformation" abl inhibitors. Chem Biol 2006 2.27
31 Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol 2010 2.26
32 Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene. Cancer Res 2010 2.20
33 High-throughput kinase profiling as a platform for drug discovery. Nat Rev Drug Discov 2008 2.12
34 Synthetic small molecules that control stem cell fate. Proc Natl Acad Sci U S A 2003 2.06
35 The evolving war on cancer. Cell 2011 2.02
36 Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Chem 2010 2.00
37 Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency. Cancer Res 2010 1.94
38 A public-private partnership to unlock the untargeted kinome. Nat Chem Biol 2013 1.83
39 TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia. Cancer Discov 2013 1.81
40 The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma. Cancer Cell 2012 1.81
41 Developing irreversible inhibitors of the protein kinase cysteinome. Chem Biol 2013 1.81
42 A combinatorial scaffold approach toward kinase-directed heterocycle libraries. J Am Chem Soc 2002 1.79
43 Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein. Cancer Cell 2010 1.72
44 Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway. Cancer Res 2012 1.66
45 A small-molecule inducer of the antioxidant response element. Chem Biol 2010 1.65
46 Golgicide A reveals essential roles for GBF1 in Golgi assembly and function. Nat Chem Biol 2009 1.65
47 Identification of a novel protein regulating microtubule stability through a chemical approach. Chem Biol 2004 1.64
48 Small molecules that induce cardiomyogenesis in embryonic stem cells. J Am Chem Soc 2004 1.63
49 Discovery of potent and selective covalent inhibitors of JNK. Chem Biol 2012 1.55
50 Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc Natl Acad Sci U S A 2012 1.52
51 Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 - 2011). Expert Opin Ther Pat 2012 1.51
52 Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma. Cancer Res 2013 1.51
53 Conformational disturbance in Abl kinase upon mutation and deregulation. Proc Natl Acad Sci U S A 2009 1.47
54 A structure-guided approach to creating covalent FGFR inhibitors. Chem Biol 2010 1.46
55 Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer. J Med Chem 2011 1.45
56 Small molecule modulators of antioxidant response pathway. Curr Opin Chem Biol 2010 1.44
57 mTOR Mediated Anti-Cancer Drug Discovery. Drug Discov Today Ther Strateg 2009 1.41
58 Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angew Chem Int Ed Engl 2013 1.34
59 Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells. Nat Biotechnol 2013 1.33
60 Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. J Biol Chem 2012 1.33
61 Metabolic and functional genomic studies identify deoxythymidylate kinase as a target in LKB1-mutant lung cancer. Cancer Discov 2013 1.27
62 High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors. Chem Biol 2011 1.27
63 Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett 2009 1.26
64 A small molecule with osteogenesis-inducing activity in multipotent mesenchymal progenitor cells. J Am Chem Soc 2002 1.26
65 Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery? ACS Chem Biol 2014 1.23
66 Pharmacological cyclin-dependent kinase inhibitors inhibit replication of wild-type and drug-resistant strains of herpes simplex virus and human immunodeficiency virus type 1 by targeting cellular, not viral, proteins. J Virol 2002 1.23
67 Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett 2012 1.22
68 Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. Bioorg Med Chem Lett 2008 1.17
69 Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site. Biochim Biophys Acta 2010 1.16
70 A genome-wide overexpression screen in yeast for small-molecule target identification. Chem Biol 2005 1.16
71 GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg Med Chem Lett 2012 1.16
72 Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR. Cancer Res 2013 1.16
73 Fibroblast growth factor receptor 1-transformed mammary epithelial cells are dependent on RSK activity for growth and survival. Cancer Res 2009 1.15
74 Allosteric interactions between the myristate- and ATP-site of the Abl kinase. PLoS One 2011 1.12
75 Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol 2013 1.08
76 Synthesis and target identification of hymenialdisine analogs. Chem Biol 2004 1.05
77 N-myristoylated c-Abl tyrosine kinase localizes to the endoplasmic reticulum upon binding to an allosteric inhibitor. J Biol Chem 2009 1.04
78 Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC. J Clin Invest 2014 1.03
79 Characterization of TAE684 as a potent LRRK2 kinase inhibitor. Bioorg Med Chem Lett 2012 1.02
80 Identification of homeodomain proteins, PBX1 and PREP1, involved in the transcription of murine leukemia virus. Mol Cell Biol 2003 1.02
81 Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase. Chembiochem 2002 1.01
82 Discovery of selective aminothiazole aurora kinase inhibitors. ACS Chem Biol 2008 1.00
83 Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I. Bioorg Med Chem Lett 2008 0.99
84 Systematic kinome shRNA screening identifies CDK11 (PITSLRE) kinase expression is critical for osteosarcoma cell growth and proliferation. Clin Cancer Res 2012 0.99
85 Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol Cancer Ther 2013 0.99
86 Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs. J Natl Cancer Inst 2013 0.96
87 A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. J Med Chem 2010 0.96
88 Antimitotic agents of natural origin. Curr Drug Targets 2006 0.96
89 Microenvironmental influence on pre-clinical activity of polo-like kinase inhibition in multiple myeloma: implications for clinical translation. PLoS One 2011 0.95
90 Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1. ACS Med Chem Lett 2011 0.92
91 Dual blockade of lipid and cyclin-dependent kinases induces synthetic lethality in malignant glioma. Proc Natl Acad Sci U S A 2012 0.90
92 Discovery of a selective irreversible BMX inhibitor for prostate cancer. ACS Chem Biol 2013 0.89
93 TSC1 involvement in bladder cancer: diverse effects and therapeutic implications. J Pathol 2013 0.89
94 Discovery of a potent, covalent BTK inhibitor for B-cell lymphoma. ACS Chem Biol 2014 0.88
95 Chemical proteomics identifies unanticipated targets of clinical kinase inhibitors. ACS Chem Biol 2007 0.87
96 Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem 2014 0.87
97 Acquired resistance to dasatinib in lung cancer cell lines conferred by DDR2 gatekeeper mutation and NF1 loss. Mol Cancer Ther 2013 0.87
98 BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner. PLoS One 2012 0.87
99 Discovery of selective irreversible inhibitors for EGFR-T790M. Bioorg Med Chem Lett 2010 0.86
100 Modulation of TNFalpha, IL-10 and IL-12p40 levels by a ceramide-1-phosphate analog, PCERA-1, in vivo and ex vivo in primary macrophages. Immunol Lett 2009 0.86
101 X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J Med Chem 2013 0.86
102 Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy. Mol Biosyst 2012 0.86
103 Resin-capture and release strategy toward combinatorial libraries of 2,6,9-substituted purines. J Comb Chem 2002 0.85
104 Cell-based optimization of novel benzamides as potential antimalarial leads. Bioorg Med Chem Lett 2009 0.85
105 A ceramide-1-phosphate analogue, PCERA-1, simultaneously suppresses tumour necrosis factor-alpha and induces interleukin-10 production in activated macrophages. Immunology 2009 0.85
106 DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors. ACS Chem Biol 2014 0.84
107 Discovery and characterization of novel mutant FLT3 kinase inhibitors. Mol Cancer Ther 2010 0.84
108 Identification and characterization of small-molecule inducers of epidermal keratinocyte differentiation. ACS Chem Biol 2007 0.83
109 Verification of a designed intramolecular hydrogen bond in a drug scaffold by nuclear magnetic resonance spectroscopy. J Med Chem 2007 0.83
110 Expanding the diversity of allosteric bcr-abl inhibitors. J Med Chem 2010 0.83
111 Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials. Bioorg Med Chem Lett 2010 0.82
112 Small-molecule inhibitors of the c-Fes protein-tyrosine kinase. Chem Biol 2012 0.81
113 Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J 2014 0.81
114 Broad spectrum alkynyl inhibitors of T315I Bcr-Abl. Bioorg Med Chem Lett 2010 0.81
115 Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae. ACS Chem Biol 2012 0.81
116 Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. ACS Med Chem Lett 2011 0.80
117 Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem 2013 0.80
118 Fluorescent visualization of Src by using dasatinib-BODIPY. Chembiochem 2014 0.78
119 A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cells. BMC Cancer 2014 0.78
120 An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRα and kit. Bioorg Med Chem Lett 2012 0.78
121 Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability. Bioorg Med Chem Lett 2011 0.78
122 Development of ATP-competitive mTOR inhibitors. Methods Mol Biol 2012 0.78
123 Development of 'DFG-out' inhibitors of gatekeeper mutant kinases. Bioorg Med Chem Lett 2012 0.77
124 Corrigendum: A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate. Nat Chem Biol 2016 0.76
125 Chemical interrogation of the malaria kinome. Chembiochem 2014 0.75
126 Protected amine labels: a versatile molecular scaffold for multiplexed nominal mass and sub-Da isotopologue quantitative proteomic reagents. J Am Soc Mass Spectrom 2014 0.75
127 Corrigendum: THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors. Nat Commun 2017 0.75
128 Corrigendum: SIKs control osteocyte responses to parathyroid hormone. Nat Commun 2017 0.75
129 Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency. Cell Stem Cell 2014 0.75
130 Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency. Cell Stem Cell 2014 0.75
131 Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II. Bioorg Med Chem Lett 2009 0.75