Craig J Thomas

Author PubWeight™ 111.29‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma. Nature 2010 8.78
2 Inhibition of pyruvate kinase M2 by reactive oxygen species contributes to cellular antioxidant responses. Science 2011 5.72
3 Noncanonical TGFβ signaling contributes to aortic aneurysm progression in Marfan syndrome mice. Science 2011 3.49
4 Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat Chem Biol 2012 3.40
5 Identification of oxadiazoles as new drug leads for the control of schistosomiasis. Nat Med 2008 2.90
6 Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550). J Immunol 2011 2.59
7 Fluorescence spectroscopic profiling of compound libraries. J Med Chem 2008 2.53
8 High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells. Proc Natl Acad Sci U S A 2014 2.50
9 Cooperative epigenetic modulation by cancer amplicon genes. Cancer Cell 2010 2.43
10 A low-molecular-weight antagonist for the human thyrotropin receptor with therapeutic potential for hyperthyroidism. Endocrinology 2008 2.03
11 Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants. Biochemistry 2008 1.82
12 Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase. J Med Chem 2008 1.81
13 CP-690,550, a therapeutic agent, inhibits cytokine-mediated Jak3 activation and proliferation of T cells from patients with ATL and HAM/TSP. Blood 2010 1.77
14 Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns. J Med Chem 2006 1.71
15 Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124. Proc Natl Acad Sci U S A 2010 1.64
16 Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase. J Med Chem 2010 1.61
17 Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice. Proc Natl Acad Sci U S A 2009 1.61
18 Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade. PLoS Negl Trop Dis 2008 1.58
19 Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease. J Med Chem 2010 1.45
20 A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR). J Biol Chem 2006 1.38
21 Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase. Bioorg Med Chem Lett 2010 1.37
22 A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution. J Med Chem 2009 1.34
23 Tuning the optical properties of fluorinated indolylfulgimides. J Org Chem 2003 1.29
24 Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition. J Med Chem 2007 1.26
25 Quantitative high-throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptor. J Biomol Screen 2008 1.25
26 Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H. J Med Chem 2011 1.24
27 "Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. J Med Chem 2005 1.21
28 A virtual screen for diverse ligands: discovery of selective G protein-coupled receptor antagonists. J Am Chem Soc 2008 1.20
29 A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. Endocrinology 2010 1.20
30 Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2008. J Comb Chem 2009 1.19
31 TCR signaling via Tec kinase ITK and interferon regulatory factor 4 (IRF4) regulates CD8+ T-cell differentiation. Proc Natl Acad Sci U S A 2012 1.13
32 Calcium-sensing receptor is a physiologic multimodal chemosensor regulating gastric G-cell growth and gastrin secretion. Proc Natl Acad Sci U S A 2010 1.13
33 Neuregulin 1-ErbB4-PI3K signaling in schizophrenia and phosphoinositide 3-kinase-p110δ inhibition as a potential therapeutic strategy. Proc Natl Acad Sci U S A 2012 1.12
34 Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria. ACS Med Chem Lett 2011 1.12
35 Solid-phase synthesis of bleomycin group antibiotics. Construction of a 108-member deglycobleomycin library. J Am Chem Soc 2003 1.09
36 Structure-guided design of a high-affinity platelet integrin αIIbβ3 receptor antagonist that disrupts Mg²⁺ binding to the MIDAS. Sci Transl Med 2012 1.07
37 Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk). Bioorg Med Chem Lett 2009 1.06
38 Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis. J Med Chem 2009 1.05
39 Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). J Med Chem 2008 1.04
40 Distinctive inhibition of O-GlcNAcase isoforms by an alpha-GlcNAc thiolsulfonate. J Am Chem Soc 2007 1.04
41 Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB. J Med Chem 2010 1.04
42 Comparison of bioluminescent kinase assays using substrate depletion and product formation. Assay Drug Dev Technol 2009 1.04
43 Selective targeting of ITK blocks multiple steps of HIV replication. Proc Natl Acad Sci U S A 2008 1.04
44 Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2007. J Comb Chem 2008 1.04
45 Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009. J Comb Chem 2010 1.03
46 The inhibition and treatment of breast cancer with poly (ADP-ribose) polymerase (PARP-1) inhibitors. Int J Biol Sci 2006 1.00
47 An O-GlcNAcase-specific inhibitor and substrate engineered by the extension of the N-acetyl moiety. J Am Chem Soc 2006 0.98
48 Structural properties of a series of photochromic fluorinated indolylfulgides. Acta Crystallogr C 2002 0.97
49 Genomic and functional characterizations of phosphodiesterase subtype 4D in human cancers. Proc Natl Acad Sci U S A 2013 0.95
50 Proteasome inactivation promotes p38 mitogen-activated protein kinase-dependent phosphatidylinositol 3-kinase activation and increases interleukin-8 production in retinal pigment epithelial cells. Mol Biol Cell 2009 0.95
51 Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death. Bioorg Med Chem 2009 0.95
52 2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase. Bioorg Med Chem Lett 2011 0.94
53 CD28 and ITK signals regulate autoreactive T cell trafficking. Nat Med 2013 0.93
54 A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety. ChemMedChem 2010 0.91
55 Insulin-dependent diabetes induced by pancreatic beta cell expression of IL-15 and IL-15Rα. Proc Natl Acad Sci U S A 2013 0.90
56 N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease. Bioorg Med Chem Lett 2007 0.89
57 Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk). Bioorg Med Chem Lett 2011 0.89
58 Synthesis and characterization of a BODIPY conjugate of the BCR-ABL kinase inhibitor Tasigna (nilotinib): evidence for transport of Tasigna and its fluorescent derivative by ABC drug transporters. Mol Pharm 2011 0.88
59 Synthesis of Oxadiazole-2-oxide Analogues as Potential Antischistosomal Agents. Tetrahedron Lett 2009 0.88
60 Integrated phosphoproteomic and metabolomic profiling reveals NPM-ALK-mediated phosphorylation of PKM2 and metabolic reprogramming in anaplastic large cell lymphoma. Blood 2013 0.87
61 Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorg Med Chem Lett 2013 0.87
62 Identification of a potent new chemotype for the selective inhibition of PDE4. Bioorg Med Chem Lett 2008 0.86
63 Inhibition of O-GlcNAcase by PUGNAc is dependent upon the oxime stereochemistry. Bioorg Med Chem 2005 0.85
64 A comparison of the ability of rilpivirine (TMC278) and selected analogues to inhibit clinically relevant HIV-1 reverse transcriptase mutants. Retrovirology 2012 0.85
65 Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation. Bioorg Med Chem Lett 2007 0.83
66 Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315. Bioorg Med Chem Lett 2013 0.82
67 A 1536-well quantitative high-throughput screen to identify compounds targeting cancer stem cells. J Biomol Screen 2012 0.82
68 Exploring the cellular activity of camptothecin-triple-helix-forming oligonucleotide conjugates. Mol Cell Biol 2006 0.81
69 Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors. Bioorg Med Chem Lett 2009 0.80
70 Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors. Bioorg Med Chem Lett 2012 0.79
71 Drug repurposing screen identifies lestaurtinib amplifies the ability of the poly (ADP-ribose) polymerase 1 inhibitor AG14361 to kill breast cancer associated gene-1 mutant and wild type breast cancer cells. Breast Cancer Res 2014 0.78
72 Exploratory analysis of kinetic solubility measurements of a small molecule library. Bioorg Med Chem 2011 0.78
73 Design and synthesis of new bicyclic diketopiperazines as scaffolds for receptor probes of structurally diverse functionality. Org Biomol Chem 2005 0.78
74 Activation of camptothecin derivatives by conjugation to triple helix-forming oligonucleotides. Biochemistry 2005 0.78
75 Multiplexing high-content flow (HCF) and quantitative high-throughput screening (qHTS) to identify compounds capable of decreasing cell viability, activating caspase 3/7, expressing annexin V, and changing mitochondrial membrane integrity. Curr Protoc Chem Biol 2013 0.77
76 Conformationally constrained analogues of bleomycin A5. J Am Chem Soc 2003 0.77
77 Chiral kinase inhibitors. Curr Top Med Chem 2011 0.77
78 The Synthesis and Evaluation of Dihydroquinazolin-4-ones and Quinazolin-4-ones as Thyroid Stimulating Hormone Receptor Agonists. Medchemcomm 2011 0.76
79 Phosphodiesterase 4 inhibitors enhance sexual pleasure-seeking activity in rodents. Pharmacol Biochem Behav 2011 0.76
80 A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases(). Medchemcomm 2012 0.76
81 Inhibition of erythroblast growth and fetal hemoglobin production by ribofuranose-substituted adenosine derivatives. Biochim Biophys Acta 2008 0.75
82 Synthesis of Substituted 2-phenylhistamines via a Microwave Promoted Suzuki Coupling. Tetrahedron Lett 2007 0.75
83 Playing well with others! Initiating and sustaining successful collaborations between industry, academia and government. Curr Top Med Chem 2014 0.75
84 Correction to "Synthesis and N-Methyl-d-aspartate (NMDA) Receptor Activity of Ketamine Metabolites". Org Lett 2017 0.75
85 Total synthesis of LL-Z1640-2 utilizing a late-stage intramolecular Nozaki-Hiyama-Kishi reaction. Tetrahedron Lett 2010 0.75
86 1-(Phenyl)isoquinoline carboxamides: a novel class of subtype selective inhibitors of thyrotropin-releasing hormone (TRH) receptors. Bioorg Med Chem Lett 2005 0.75