Published in J Med Chem on August 06, 2014
Screening-based translation of public research encounters painful problems. ACS Med Chem Lett (2015) 1.00
Mer receptor tyrosine kinase is frequently overexpressed in human non-small cell lung cancer, confirming resistance to erlotinib. Oncotarget (2015) 0.80
Small Molecule Inhibition of MERTK Is Efficacious in Non-Small Cell Lung Cancer Models Independent of Driver Oncogene Status. Mol Cancer Ther (2015) 0.79
MERTK as a novel therapeutic target in head and neck cancer. Oncotarget (2016) 0.79
The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. JCI Insight (2016) 0.78
Design and Synthesis of Novel Macrocyclic Mer Tyrosine Kinase Inhibitors. ACS Med Chem Lett (2016) 0.78
TAM receptor tyrosine kinases as emerging targets of innate immune checkpoint blockade for cancer therapy. Immunol Rev (2017) 0.77
MERTK Inhibition Induces Polyploidy and Promotes Cell Death and Cellular Senescence in Glioblastoma Multiforme. PLoS One (2016) 0.76
UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with Methotrexate in Leukemia Models. Clin Cancer Res (2016) 0.75
Discovery of Macrocyclic Pyrimidines as MerTK-specific Inhibitors. ChemMedChem (2016) 0.75
Ligand Activation of TAM Family Receptors-Implications for Tumor Biology and Therapeutic Response. Cancers (Basel) (2016) 0.75
Discovery of Mer kinase inhibitors by virtual screening using Structural Protein-Ligand Interaction Fingerprints. Bioorg Med Chem (2015) 0.75
Targeting the TAM Receptors in Leukemia. Cancers (Basel) (2016) 0.75
Can the pharmaceutical industry reduce attrition rates? Nat Rev Drug Discov (2004) 15.57
Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists. Methods Biochem Anal (2005) 5.37
Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding inhibitors. Biochim Biophys Acta (1969) 4.94
The art of the chemical probe. Nat Chem Biol (2010) 3.85
Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412. Blood (2004) 3.84
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol (2011) 3.72
TAM receptor tyrosine kinases: biologic functions, signaling, and potential therapeutic targeting in human cancer. Adv Cancer Res (2008) 3.63
Synopsis of some recent tactical application of bioisosteres in drug design. J Med Chem (2011) 3.31
Molecular target class is predictive of in vitro response profile. Cancer Res (2010) 3.27
In situ kinase profiling reveals functionally relevant properties of native kinases. Chem Biol (2011) 2.69
Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential. J Med Chem (2011) 1.94
Targeting Axl and Mer kinases in cancer. Mol Cancer Ther (2011) 1.88
Identification of Gas6 as a ligand for Mer, a neural cell adhesion molecule related receptor tyrosine kinase implicated in cellular transformation. Oncogene (1997) 1.70
Inhibition of Mer and Axl receptor tyrosine kinases in astrocytoma cells leads to increased apoptosis and improved chemosensitivity. Mol Cancer Ther (2010) 1.69
Ectopic expression of the proto-oncogene Mer in pediatric T-cell acute lymphoblastic leukemia. Clin Cancer Res (2006) 1.61
Lymphoblastic leukemia/lymphoma in mice overexpressing the Mer (MerTK) receptor tyrosine kinase. Oncogene (2006) 1.56
FLT3 internal tandem duplication mutations in adult acute myeloid leukaemia define a high-risk group. Br J Haematol (2000) 1.50
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. J Med Chem (2009) 1.39
MERTK receptor tyrosine kinase is a therapeutic target in melanoma. J Clin Invest (2013) 1.34
Mer or Axl receptor tyrosine kinase inhibition promotes apoptosis, blocks growth and enhances chemosensitivity of human non-small cell lung cancer. Oncogene (2012) 1.33
Comprehensive characterization of cytochrome P450 isozyme selectivity across chemical libraries. Nat Biotechnol (2009) 1.30
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia. ACS Med Chem Lett (2012) 1.22
Strain energy of small ring hydrocarbons. Influence of C-h bond dissociation energies. J Am Chem Soc (2004) 1.20
Activity-based kinase profiling of approved tyrosine kinase inhibitors. Genes Cells (2012) 1.11
Mer receptor tyrosine kinase inhibition impedes glioblastoma multiforme migration and alters cellular morphology. Oncogene (2011) 1.07
Structural insights into the inhibited states of the Mer receptor tyrosine kinase. J Struct Biol (2008) 1.04
Mer receptor tyrosine kinase promotes invasion and survival in glioblastoma multiforme. Oncogene (2012) 1.04
UNC1062, a new and potent Mer inhibitor. Eur J Med Chem (2013) 1.03
Picornavirus inhibitors: trifluoromethyl substitution provides a global protective effect against hepatic metabolism. J Med Chem (1995) 1.02
Aberrant Mer receptor tyrosine kinase expression contributes to leukemogenesis in acute myeloid leukemia. Oncogene (2013) 1.01
Mer receptor tyrosine kinase is a therapeutic target in pre-B-cell acute lymphoblastic leukemia. Blood (2013) 1.00
Inhibition of MerTK increases chemosensitivity and decreases oncogenic potential in T-cell acute lymphoblastic leukemia. Blood Cancer J (2013) 1.00
MerTK inhibition is a novel therapeutic approach for glioblastoma multiforme. Oncotarget (2014) 0.98
Kinome-wide activity modeling from diverse public high-quality data sets. J Chem Inf Model (2013) 0.98
Mitigating heterocycle metabolism in drug discovery. J Med Chem (2012) 0.97
Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. J Med Chem (2013) 0.96
Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks. Invest New Drugs (2011) 0.96
LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models. Invest New Drugs (2012) 0.96
Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem (2013) 0.91
RNAi-induced down-regulation of FLT3 expression in AML cell lines increases sensitivity to MLN518. Blood (2004) 0.87
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer. J Med Chem (2011) 0.85
Will FLT3 inhibitors fulfill their promise in acute meyloid leukemia? Curr Opin Hematol (2014) 0.84
MERTK controls melanoma cell migration and survival and differentially regulates cell behavior relative to AXL. Pigment Cell Melanoma Res (2013) 0.84
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687). J Med Chem (2012) 0.83
Microwave-assisted, divergent solution-phase synthesis of 1,3,6-trisubstituted pyrazolo[3,4-d]pyrimidines. ACS Comb Sci (2011) 0.83
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. J Med Chem (2012) 0.83
First-Principles Calculation of the Intrinsic Aqueous Solubility of Crystalline Druglike Molecules. J Chem Theory Comput (2012) 0.82
New horizons in drug metabolism, pharmacokinetics and drug discovery. Drug News Perspect (2003) 0.80
Pyrazolopyridine inhibitors of B-Raf(V600E). Part 3: an increase in aqueous solubility via the disruption of crystal packing. Bioorg Med Chem Lett (2011) 0.76
A draft sequence of the rice genome (Oryza sativa L. ssp. indica). Science (2002) 42.78
Race, breast cancer subtypes, and survival in the Carolina Breast Cancer Study. JAMA (2006) 24.01
Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases. Cancer Cell (2011) 11.44
Receptor interacting protein kinase-3 determines cellular necrotic response to TNF-alpha. Cell (2009) 11.36
R2D2, a bridge between the initiation and effector steps of the Drosophila RNAi pathway. Science (2003) 9.53
The BioGRID Interaction Database: 2011 update. Nucleic Acids Res (2010) 8.46
Comparative genome sequencing of Drosophila pseudoobscura: chromosomal, gene, and cis-element evolution. Genome Res (2005) 8.38
Epidemiology of basal-like breast cancer. Breast Cancer Res Treat (2007) 7.08
Mule/ARF-BP1, a BH3-only E3 ubiquitin ligase, catalyzes the polyubiquitination of Mcl-1 and regulates apoptosis. Cell (2005) 6.86
TNF-alpha induces two distinct caspase-8 activation pathways. Cell (2008) 6.81
Mixed lineage kinase domain-like protein mediates necrosis signaling downstream of RIP3 kinase. Cell (2012) 6.56
Argonaute2 cleaves the anti-guide strand of siRNA during RISC activation. Cell (2005) 6.47
Elimination of Mcl-1 is required for the initiation of apoptosis following ultraviolet irradiation. Genes Dev (2003) 6.17
Cytochrome C-mediated apoptosis. Annu Rev Biochem (2004) 5.38
Specific ablation of the apoptotic functions of cytochrome C reveals a differential requirement for cytochrome C and Apaf-1 in apoptosis. Cell (2005) 5.37
WormBase: a comprehensive resource for nematode research. Nucleic Acids Res (2009) 5.20
Autocrine TNFalpha signaling renders human cancer cells susceptible to Smac-mimetic-induced apoptosis. Cancer Cell (2007) 5.09
Jaundice Constrain or Indication? Response. Radiology (2017) 5.07
A small molecule Smac mimic potentiates TRAIL- and TNFalpha-mediated cell death. Science (2004) 4.95
Exogenous plant MIR168a specifically targets mammalian LDLRAP1: evidence of cross-kingdom regulation by microRNA. Cell Res (2011) 4.55
The mitochondrial phosphatase PGAM5 functions at the convergence point of multiple necrotic death pathways. Cell (2012) 4.37
WormBase: new content and better access. Nucleic Acids Res (2006) 4.01
WormBase 2012: more genomes, more data, new website. Nucleic Acids Res (2011) 3.87
The complete genomes and proteomes of 27 Staphylococcus aureus bacteriophages. Proc Natl Acad Sci U S A (2005) 3.84
Delayed apoptotic cell clearance and lupus-like autoimmunity in mice lacking the c-mer membrane tyrosine kinase. J Exp Med (2002) 3.83
Epidemiological transition of stroke in China: twenty-one-year observational study from the Sino-MONICA-Beijing Project. Stroke (2008) 3.81
Dynamic reprogramming of the kinome in response to targeted MEK inhibition in triple-negative breast cancer. Cell (2012) 3.77
WormBase 2007. Nucleic Acids Res (2007) 3.69
TAM receptor tyrosine kinases: biologic functions, signaling, and potential therapeutic targeting in human cancer. Adv Cancer Res (2008) 3.63
Biochemical identification of Argonaute 2 as the sole protein required for RNA-induced silencing complex activity. Proc Natl Acad Sci U S A (2004) 3.63
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol (2011) 3.60
Distinctive roles of PHAP proteins and prothymosin-alpha in a death regulatory pathway. Science (2003) 3.59
Quantitative susceptibility map reconstruction from MR phase data using bayesian regularization: validation and application to brain imaging. Magn Reson Med (2010) 3.43
Degradation of Mcl-1 by beta-TrCP mediates glycogen synthase kinase 3-induced tumor suppression and chemosensitization. Mol Cell Biol (2007) 3.23
Three-dimensional structure of the apoptosome: implications for assembly, procaspase-9 binding, and activation. Mol Cell (2002) 3.06
Impact of high-throughput screening in biomedical research. Nat Rev Drug Discov (2011) 3.03
Resolving the distinct stages in erythroid differentiation based on dynamic changes in membrane protein expression during erythropoiesis. Proc Natl Acad Sci U S A (2009) 3.00
The ER UDPase ENTPD5 promotes protein N-glycosylation, the Warburg effect, and proliferation in the PTEN pathway. Cell (2010) 2.97
Too many roads not taken. Nature (2011) 2.93
Smoking during pregnancy and newborn neurobehavior. Pediatrics (2003) 2.93
The integrated response of the human cerebro-cerebellar and limbic systems to acupuncture stimulation at ST 36 as evidenced by fMRI. Neuroimage (2005) 2.86
Single-stranded RNAs use RNAi to potently and allele-selectively inhibit mutant huntingtin expression. Cell (2012) 2.83
Explaining the increase in coronary heart disease mortality in Beijing between 1984 and 1999. Circulation (2004) 2.81
Positive association of the oxytocin receptor gene (OXTR) with autism in the Chinese Han population. Biol Psychiatry (2005) 2.79
Indirect emissions from biofuels: how important? Science (2009) 2.71
Characterization of the "deqi" response in acupuncture. BMC Complement Altern Med (2007) 2.70
Toll-like receptors activate programmed necrosis in macrophages through a receptor-interacting kinase-3-mediated pathway. Proc Natl Acad Sci U S A (2011) 2.64
Future cardiovascular disease in china: markov model and risk factor scenario projections from the coronary heart disease policy model-china. Circ Cardiovasc Qual Outcomes (2010) 2.63
Dietary flavonoids: effects on xenobiotic and carcinogen metabolism. Toxicol In Vitro (2005) 2.60
H3K9 methylation is a barrier during somatic cell reprogramming into iPSCs. Nat Genet (2012) 2.47
Macrophages and dendritic cells use different Axl/Mertk/Tyro3 receptors in clearance of apoptotic cells. J Immunol (2007) 2.45
A soluble form of the Mer receptor tyrosine kinase inhibits macrophage clearance of apoptotic cells and platelet aggregation. Blood (2006) 2.41
WormBase 2014: new views of curated biology. Nucleic Acids Res (2013) 2.39
Activated Cdc42-associated kinase Ack1 promotes prostate cancer progression via androgen receptor tyrosine phosphorylation. Proc Natl Acad Sci U S A (2007) 2.34
A cross-sectional study of the microeconomic impact of cardiovascular disease hospitalization in four low- and middle-income countries. PLoS One (2011) 2.23
Mutant DNA-binding domain of HSF4 is associated with autosomal dominant lamellar and Marner cataract. Nat Genet (2002) 2.21
The role of oxygen during fracture healing. Bone (2012) 2.21
Activation of Mst1 causes dilated cardiomyopathy by stimulating apoptosis without compensatory ventricular myocyte hypertrophy. J Clin Invest (2003) 2.20
Inhibition of endogenous thioredoxin in the heart increases oxidative stress and cardiac hypertrophy. J Clin Invest (2003) 2.19
Comparative genomic analysis of 18 Pseudomonas aeruginosa bacteriophages. J Bacteriol (2006) 2.18
Formation of apoptosome is initiated by cytochrome c-induced dATP hydrolysis and subsequent nucleotide exchange on Apaf-1. Proc Natl Acad Sci U S A (2005) 2.18
Effects of electroacupuncture versus manual acupuncture on the human brain as measured by fMRI. Hum Brain Mapp (2005) 2.15
The long non-coding RNA HOTAIR indicates a poor prognosis and promotes metastasis in non-small cell lung cancer. BMC Cancer (2013) 2.11
Nutrient starvation elicits an acute autophagic response mediated by Ulk1 dephosphorylation and its subsequent dissociation from AMPK. Proc Natl Acad Sci U S A (2011) 2.06
Successful treatment of severe aplastic anemia in children using standardized immunosuppressive therapy with antithymocyte globulin and cyclosporine A. Pediatr Blood Cancer (2004) 2.06
Morphology enabled dipole inversion (MEDI) from a single-angle acquisition: comparison with COSMOS in human brain imaging. Magn Reson Med (2011) 2.05
Efficacy and safety of intracameral triamcinolone acetonide to control postoperative inflammation after phacotrabeculectomy. J Cataract Refract Surg (2013) 2.00
The infant development, environment, and lifestyle study: effects of prenatal methamphetamine exposure, polydrug exposure, and poverty on intrauterine growth. Pediatrics (2006) 1.98
Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy. Proc Natl Acad Sci U S A (2011) 1.98
Activated tyrosine kinase Ack1 promotes prostate tumorigenesis: role of Ack1 in polyubiquitination of tumor suppressor Wwox. Cancer Res (2005) 1.97
LGN regulates mitotic spindle orientation during epithelial morphogenesis. J Cell Biol (2010) 1.95
Child mortality estimation: appropriate time periods for child mortality estimates from full birth histories. PLoS Med (2012) 1.93
Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J Med Chem (2009) 1.92
Prenatal methamphetamine use and neonatal neurobehavioral outcome. Neurotoxicol Teratol (2007) 1.90
Cytochrome P450 2E1 contributes to ethanol-induced fatty liver in mice. Hepatology (2008) 1.90
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol (2013) 1.89
Maternal farm exposure modulates neonatal immune mechanisms through regulatory T cells. J Allergy Clin Immunol (2009) 1.89
A novel background field removal method for MRI using projection onto dipole fields (PDF). NMR Biomed (2011) 1.88
Chloroquine sensitizes breast cancer cells to chemotherapy independent of autophagy. Autophagy (2012) 1.86
Proteotoxic stress induces a cell-cycle arrest by stimulating Lon to degrade the replication initiator DnaA. Cell (2013) 1.86
Autologous bone marrow mesenchymal stem cell transplantation in liver failure patients caused by hepatitis B: short-term and long-term outcomes. Hepatology (2011) 1.83
Dual inhibition of focal adhesion kinase and epidermal growth factor receptor pathways cooperatively induces death receptor-mediated apoptosis in human breast cancer cells. J Biol Chem (2002) 1.82
Methamphetamine and other substance use during pregnancy: preliminary estimates from the Infant Development, Environment, and Lifestyle (IDEAL) study. Matern Child Health J (2006) 1.81
The TAM family: phosphatidylserine sensing receptor tyrosine kinases gone awry in cancer. Nat Rev Cancer (2014) 1.77
Impairment of T-regulatory cells in cord blood of atopic mothers. J Allergy Clin Immunol (2008) 1.76
Taking aim at Mer and Axl receptor tyrosine kinases as novel therapeutic targets in solid tumors. Expert Opin Ther Targets (2010) 1.76
HIV/STD prevalence among men who have sex with men in Chengdu, China and associated risk factors for HIV infection. J Acquir Immune Defic Syndr (2010) 1.76
Adiponectin modulates the glycogen synthase kinase-3beta/beta-catenin signaling pathway and attenuates mammary tumorigenesis of MDA-MB-231 cells in nude mice. Cancer Res (2006) 1.75
An RCS-like retinal dystrophy phenotype in mer knockout mice. Invest Ophthalmol Vis Sci (2003) 1.75
Cytokines in alcoholic liver disease. Arch Toxicol (2012) 1.74
JNK suppresses apoptosis via phosphorylation of the proapoptotic Bcl-2 family protein BAD. Mol Cell (2004) 1.73
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem (2010) 1.73
Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol (2013) 1.72