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The publication data currently available has been vetted by Vanderbilt faculty, staff, administrators and trainees. The data itself is retrieved directly from NCBI's PubMed and is automatically updated on a weekly basis to ensure accuracy and completeness.

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Results: 1 to 10 of 23

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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
Monitoring Therapeutic Response and Resistance: Analysis of Circulating Tumor DNA in Patients With ALK+ Lung Cancer.
Horn L, Whisenant JG, Wakelee H, Reckamp KL, Qiao H, Leal TA, Du L, Hernandez J, Huang V, Blumenschein GR, Waqar SN, Patel SP, Nieva J, Oxnard GR, Sanborn RE, Shaffer T, Garg K, Holzhausen A, Harrow K, Liang C, Lim LP, Li M, Lovly CM
(2019) J Thorac Oncol 14: 1901-1911
MeSH Terms: Adult, Aged, Aged, 80 and over, Anaplastic Lymphoma Kinase, Carcinoma, Non-Small-Cell Lung, Circulating Tumor DNA, Drug Resistance, Neoplasm, Female, Humans, Lung Neoplasms, Male, Middle Aged, Mutation, Oncogene Proteins, Fusion, Piperazines, Prognosis, Protein Kinase Inhibitors, Pyridazines
Added March 18, 2020
0 Communities
1 Members
0 Resources
18 MeSH Terms
Thrombotic microangiopathy as a cause of cardiovascular toxicity from the BCR-ABL1 tyrosine kinase inhibitor ponatinib.
Latifi Y, Moccetti F, Wu M, Xie A, Packwood W, Qi Y, Ozawa K, Shentu W, Brown E, Shirai T, McCarty OJ, Ruggeri Z, Moslehi J, Chen J, Druker BJ, López JA, Lindner JR
(2019) Blood 133: 1597-1606
MeSH Terms: Animals, Aorta, Cardiovascular Diseases, Endothelium, Fusion Proteins, bcr-abl, Humans, Imidazoles, Ischemia, Mice, Mice, Knockout, Platelet Adhesiveness, Protein Kinase Inhibitors, Pyridazines, Thrombotic Microangiopathies, Ventricular Dysfunction, von Willebrand Factor
Added February 24, 2019
0 Communities
1 Members
0 Resources
16 MeSH Terms
Ensartinib (X-396) in ALK-Positive Non-Small Cell Lung Cancer: Results from a First-in-Human Phase I/II, Multicenter Study.
Horn L, Infante JR, Reckamp KL, Blumenschein GR, Leal TA, Waqar SN, Gitlitz BJ, Sanborn RE, Whisenant JG, Du L, Neal JW, Gockerman JP, Dukart G, Harrow K, Liang C, Gibbons JJ, Holzhausen A, Lovly CM, Wakelee HA
(2018) Clin Cancer Res 24: 2771-2779
MeSH Terms: Adult, Aged, Aged, 80 and over, Anaplastic Lymphoma Kinase, Animals, Antineoplastic Agents, Carcinoma, Non-Small-Cell Lung, Cell Line, Tumor, Disease Models, Animal, Dose-Response Relationship, Drug, Female, Humans, Immunohistochemistry, In Situ Hybridization, Fluorescence, Kaplan-Meier Estimate, Lung Neoplasms, Male, Mice, Middle Aged, Mutation, Neoplasm Grading, Neoplasm Staging, Piperazines, Prognosis, Protein Kinase Inhibitors, Pyridazines, Rats, Treatment Outcome, Young Adult
Added September 10, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
Cardiovascular care of patients with chronic myeloid leukemia (CML) on tyrosine kinase inhibitor (TKI) therapy.
Barber MC, Mauro MJ, Moslehi J
(2017) Hematology Am Soc Hematol Educ Program 2017: 110-114
MeSH Terms: Aged, Dasatinib, Female, Fusion Proteins, bcr-abl, Humans, Hypertension, Pulmonary, Imidazoles, Leukemia, Myelogenous, Chronic, BCR-ABL Positive, Male, Middle Aged, Protein Kinase Inhibitors, Pyridazines, Pyrimidines
Added April 22, 2018
0 Communities
1 Members
0 Resources
13 MeSH Terms
Challenges in the development of an M PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.
Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW
(2017) Bioorg Med Chem Lett 27: 5179-5184
MeSH Terms: Allosteric Regulation, Amides, Azetidines, Drug Evaluation, Preclinical, Humans, Protein Binding, Pyridazines, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
2 Members
0 Resources
MeSH Terms
Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M PAM VU0467154.
Gould RW, Grannan MD, Gunter BW, Ball J, Bubser M, Bridges TM, Wess J, Wood MW, Brandon NJ, Duggan ME, Niswender CM, Lindsley CW, Conn PJ, Jones CK
(2018) Neuropharmacology 128: 492-502
MeSH Terms: Allosteric Regulation, Animals, Antipsychotic Agents, Brain, Cognition Disorders, Discrimination, Psychological, Disease Models, Animal, Dizocilpine Maleate, Dose-Response Relationship, Drug, Hyperkinesis, Male, Memory Disorders, Mice, Mice, Inbred C57BL, Mice, Knockout, Pyridazines, Receptor, Muscarinic M4, Schizophrenia, Thiophenes
Added March 3, 2020
0 Communities
2 Members
0 Resources
MeSH Terms
Restoring auditory cortex plasticity in adult mice by restricting thalamic adenosine signaling.
Blundon JA, Roy NC, Teubner BJW, Yu J, Eom TY, Sample KJ, Pani A, Smeyne RJ, Han SB, Kerekes RA, Rose DC, Hackett TA, Vuppala PK, Freeman BB, Zakharenko SS
(2017) Science 356: 1352-1356
MeSH Terms: 5'-Nucleotidase, Adenosine, Adenosine A1 Receptor Agonists, Adenosine A1 Receptor Antagonists, Animals, Auditory Cortex, Auditory Perception, GPI-Linked Proteins, Mice, Neuronal Plasticity, Piperidines, Pyridazines, Receptor, Adenosine A1, Signal Transduction, Thalamus
Added April 3, 2018
0 Communities
1 Members
0 Resources
MeSH Terms
Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.
Bender AM, Weiner RL, Luscombe VB, Ajmera S, Cho HP, Chang S, Zhan X, Rodriguez AL, Niswender CM, Engers DW, Bridges TM, Conn PJ, Lindsley CW
(2017) Bioorg Med Chem Lett 27: 3576-3581
MeSH Terms: Animals, Brain, CHO Cells, Cricetulus, Humans, Muscarinic Antagonists, Piperazine, Piperazines, Pyridazines, Rats, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
Optimization of M positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.
Melancon BJ, Wood MR, Noetzel MJ, Nance KD, Engelberg EM, Han C, Lamsal A, Chang S, Cho HP, Byers FW, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, Wu D, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW
(2017) Bioorg Med Chem Lett 27: 2296-2301
MeSH Terms: Allosteric Regulation, Animals, Crystallography, X-Ray, Drug Discovery, Hydrogen Bonding, Pyridazines, Rats, Structure-Activity Relationship, Thiophenes, Translational Medical Research
Added March 3, 2020
0 Communities
2 Members
0 Resources
MeSH Terms