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Symmetrically substituted dichlorophenes inhibit -acyl-phosphatidylethanolamine phospholipase D.
Aggarwal G, Zarrow JE, Mashhadi Z, Flynn CR, Vinson P, Weaver CD, Davies SS
(2020) J Biol Chem 295: 7289-7300
MeSH Terms: Animals, Bacterial Proteins, Bithionol, Dichlorophen, Enzyme Inhibitors, HEK293 Cells, Hexachlorophene, Humans, Mice, Phospholipase D, Quinazolines, Streptomyces, Sulfonamides
Added August 18, 2020
0 Communities
1 Members
0 Resources
13 MeSH Terms
Discovery of structurally distinct tricyclic M positive allosteric modulator (PAM) chemotypes.
Temple KJ, Long MF, Engers JL, Watson KJ, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW
(2020) Bioorg Med Chem Lett 30: 126811
MeSH Terms: Allosteric Regulation, Animals, Drug Design, Half-Life, Humans, Inhibitory Concentration 50, Pyridazines, Quinazolines, Rats, Receptor, Muscarinic M4, Structure-Activity Relationship, Triazoles
Added March 3, 2020
0 Communities
1 Members
0 Resources
12 MeSH Terms
Epidermal growth factor receptor inhibition downregulates -induced epithelial inflammatory responses, DNA damage and gastric carcinogenesis.
Sierra JC, Asim M, Verriere TG, Piazuelo MB, Suarez G, Romero-Gallo J, Delgado AG, Wroblewski LE, Barry DP, Peek RM, Gobert AP, Wilson KT
(2018) Gut 67: 1247-1260
MeSH Terms: Animals, Antineoplastic Agents, Cell Culture Techniques, Epithelial Cells, ErbB Receptors, Gastritis, Gefitinib, Gerbillinae, Helicobacter Infections, Helicobacter pylori, Mice, Mice, Inbred C57BL, Quinazolines, Stomach Neoplasms
Added June 29, 2017
0 Communities
2 Members
0 Resources
14 MeSH Terms
An Acquired Gatekeeper Mutation Induces Resistance to Neratinib in a Patient with HER2 Mutant-Driven Breast Cancer.
Hanker AB, Brewer MR, Sheehan JH, Koch JP, Sliwoski GR, Nagy R, Lanman R, Berger MF, Hyman DM, Solit DB, He J, Miller V, Cutler RE, Lalani AS, Cross D, Lovly CM, Meiler J, Arteaga CL
(2017) Cancer Discov 7: 575-585
MeSH Terms: Afatinib, Antineoplastic Agents, Breast Neoplasms, Cell Line, Tumor, Drug Resistance, Neoplasm, Female, Humans, Middle Aged, Mutation, Phenotype, Protein Kinase Inhibitors, Quinazolines, Quinolines, Receptor, ErbB-2
Added April 8, 2017
1 Communities
3 Members
0 Resources
14 MeSH Terms
A comparative assessment of preclinical chemotherapeutic response of tumors using quantitative non-Gaussian diffusion MRI.
Xu J, Li K, Smith RA, Waterton JC, Zhao P, Ding Z, Does MD, Manning HC, Gore JC
(2017) Magn Reson Imaging 37: 195-202
MeSH Terms: Animals, Bayes Theorem, Colonic Neoplasms, Diffusion Magnetic Resonance Imaging, Dimethyl Sulfoxide, Disease Models, Animal, Female, Humans, Mice, Mice, Nude, Models, Statistical, Organophosphates, Protein Kinase Inhibitors, Quinazolines
Added April 6, 2017
0 Communities
3 Members
0 Resources
14 MeSH Terms
Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.
Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, Bubser M, Jones CK, Hopkins CR, Emmitte KA, Niswender CM, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW
(2016) Bioorg Med Chem Lett 26: 3029-3033
MeSH Terms: Allosteric Regulation, Animals, Brain, Humans, Microsomes, Liver, Piperidines, Pyrimidines, Quinazolines, Rats, Receptor, Muscarinic M4, Structure-Activity Relationship, Thiophenes
Added April 6, 2017
0 Communities
3 Members
0 Resources
12 MeSH Terms
InsR/IGF1R Pathway Mediates Resistance to EGFR Inhibitors in Glioblastoma.
Ma Y, Tang N, Thompson RC, Mobley BC, Clark SW, Sarkaria JN, Wang J
(2016) Clin Cancer Res 22: 1767-76
MeSH Terms: Animals, Antineoplastic Agents, Cell Line, Tumor, Disease Models, Animal, Drug Resistance, Neoplasm, ErbB Receptors, Gefitinib, Glioblastoma, Humans, Insulin, Insulin-Like Growth Factor I, Mice, Protein Kinase Inhibitors, Proto-Oncogene Proteins c-akt, Quinazolines, Receptor, IGF Type 1, Receptor, Insulin, Signal Transduction, Tumor Burden, Xenograft Model Antitumor Assays
Added April 18, 2017
0 Communities
1 Members
0 Resources
20 MeSH Terms
EGFR Kinase Domain Duplication (EGFR-KDD) Is a Novel Oncogenic Driver in Lung Cancer That Is Clinically Responsive to Afatinib.
Gallant JN, Sheehan JH, Shaver TM, Bailey M, Lipson D, Chandramohan R, Red Brewer M, York SJ, Kris MG, Pietenpol JA, Ladanyi M, Miller VA, Ali SM, Meiler J, Lovly CM
(2015) Cancer Discov 5: 1155-63
MeSH Terms: Adult, Afatinib, Antineoplastic Agents, Drug Resistance, Neoplasm, ErbB Receptors, Gene Duplication, Gene Frequency, Humans, Lung Neoplasms, Male, Models, Molecular, Molecular Targeted Therapy, Mutation, Neoplasm Staging, Protein Conformation, Protein Interaction Domains and Motifs, Protein Kinase Inhibitors, Protein Multimerization, Quinazolines, Tomography, X-Ray Computed, Treatment Outcome
Added January 26, 2016
1 Communities
5 Members
0 Resources
21 MeSH Terms
Receptor tyrosine kinase ERBB4 mediates acquired resistance to ERBB2 inhibitors in breast cancer cells.
Canfield K, Li J, Wilkins OM, Morrison MM, Ung M, Wells W, Williams CR, Liby KT, Vullhorst D, Buonanno A, Hu H, Schiff R, Cook RS, Kurokawa M
(2015) Cell Cycle 14: 648-55
MeSH Terms: Animals, Breast Neoplasms, Cell Line, Tumor, Drug Resistance, Neoplasm, Female, Gene Expression Regulation, Neoplastic, Gene Knockdown Techniques, Lapatinib, Mice, Quinazolines, Receptor, ErbB-2, Receptor, ErbB-4, Trastuzumab
Added February 12, 2015
1 Communities
1 Members
0 Resources
13 MeSH Terms
A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma.
Galloway TJ, Wirth LJ, Colevas AD, Gilbert J, Bauman JE, Saba NF, Raben D, Mehra R, Ma AW, Atoyan R, Wang J, Burtness B, Jimeno A
(2015) Clin Cancer Res 21: 1566-73
MeSH Terms: Aged, Antineoplastic Agents, Carcinoma, Squamous Cell, Chemoradiotherapy, Cisplatin, ErbB Receptors, Female, Head and Neck Neoplasms, Histone Deacetylases, Humans, Hydroxamic Acids, Male, Maximum Tolerated Dose, Middle Aged, Quinazolines, Radiotherapy, Receptor, ErbB-2, Squamous Cell Carcinoma of Head and Neck
Added February 17, 2015
0 Communities
1 Members
0 Resources
18 MeSH Terms