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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 387

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N-[F]-Fluoroacetylcrizotinib: A potentially potent and selective PET tracer for molecular imaging of non-small cell lung cancer.
Buck JR, Saleh S, Claus T, Lovly C, Hight MR, Nickels ML, Noor Tantawy M, Charles Manning H
(2020) Bioorg Med Chem Lett 30: 127257
MeSH Terms: Anaplastic Lymphoma Kinase, Carcinoma, Non-Small-Cell Lung, Cell Line, Tumor, Cell Proliferation, Crizotinib, Dose-Response Relationship, Drug, Fluorine Radioisotopes, Humans, Lung Neoplasms, Molecular Imaging, Molecular Structure, Positron-Emission Tomography, Protein Kinase Inhibitors, Structure-Activity Relationship
Added September 10, 2020
0 Communities
1 Members
0 Resources
14 MeSH Terms
Algal Toxin Goniodomin A Binds Potassium Ion Selectively to Yield a Conformationally Altered Complex with Potential Biological Consequences.
Tainter CJ, Schley ND, Harris CM, Stec DF, Song AK, Balinski A, May JC, McLean JA, Reece KS, Harris TM
(2020) J Nat Prod 83: 1069-1081
MeSH Terms: Actin Cytoskeleton, Actins, Animals, Dinoflagellida, Ethers, Ethers, Cyclic, Humans, Ions, Macrolides, Magnetic Resonance Spectroscopy, Molecular Structure, Potassium
Added March 3, 2020
0 Communities
1 Members
0 Resources
12 MeSH Terms
An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders.
Porter JD, Vivas O, Weaver CD, Alsafran A, DiMilo E, Arnold LA, Dickson EJ, Dockendorff C
(2019) Bioorg Med Chem Lett 29: 126681
MeSH Terms: Anthracenes, Dose-Response Relationship, Drug, KCNQ2 Potassium Channel, KCNQ3 Potassium Channel, Mental Disorders, Molecular Structure, Neurodegenerative Diseases, Potassium Channel Blockers, Structure-Activity Relationship
Added March 27, 2020
0 Communities
1 Members
0 Resources
9 MeSH Terms
Validation of Human Sterol 14α-Demethylase (CYP51) Druggability: Structure-Guided Design, Synthesis, and Evaluation of Stoichiometric, Functionally Irreversible Inhibitors.
Friggeri L, Hargrove TY, Wawrzak Z, Guengerich FP, Lepesheva GI
(2019) J Med Chem 62: 10391-10401
MeSH Terms: 14-alpha Demethylase Inhibitors, Animals, Catalytic Domain, Crystallography, X-Ray, Drug Design, Humans, Molecular Structure, Mutagenesis, Site-Directed, Protozoan Proteins, Sterol 14-Demethylase
Added March 3, 2020
0 Communities
2 Members
0 Resources
10 MeSH Terms
Discovery of a novel 3,4-dimethylcinnoline carboxamide M positive allosteric modulator (PAM) chemotype via scaffold hopping.
Temple KJ, Engers JL, Long MF, Gregro AR, Watson KJ, Chang S, Jenkins MT, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 126678
MeSH Terms: Allosteric Regulation, Amides, Azetidines, Benzene, Molecular Structure, Protein Binding, Pyrazines, Pyridines, Pyrimidines, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
11 MeSH Terms
The anti-parasitic agent suramin and several of its analogues are inhibitors of the DNA binding protein Mcm10.
Paulson CN, John K, Baxley RM, Kurniawan F, Orellana K, Francis R, Sobeck A, Eichman BF, Chazin WJ, Aihara H, Georg GI, Hawkinson JE, Bielinsky AK
(2019) Open Biol 9: 190117
MeSH Terms: Animals, Cell Survival, DNA Replication, DNA-Binding Proteins, Drug Discovery, Enzyme Inhibitors, Gene Expression, High-Throughput Nucleotide Sequencing, Humans, Kinetics, Minichromosome Maintenance Proteins, Molecular Structure, Protein Binding, Suramin, Xenopus
Added August 26, 2019
0 Communities
2 Members
0 Resources
15 MeSH Terms
Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu NAMs: Challenging SAR, enantiospecific activity and in vivo efficacy.
Yamada Y, Yohn SE, Gilliland K, Loch MT, Schulte ML, Rodriguez AL, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 2670-2674
MeSH Terms: Animals, Anti-Anxiety Agents, Antidepressive Agents, Dose-Response Relationship, Drug, Mice, Molecular Structure, Pyridones, Rats, Receptors, Metabotropic Glutamate, Stereoisomerism, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
11 MeSH Terms
VU6005806/AZN-00016130, an advanced M positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.
Engers DW, Melancon BJ, Gregro AR, Bertron JL, Bollinger SR, Felts AS, Konkol LC, Wood MR, Bollinger KA, Luscombe VB, Rodriguez AL, Jones CK, Bubser M, Yohn SE, Wood MW, Brandon NJ, Dugan ME, Niswender CM, Conn PJ, Bridges TM, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 1714-1718
MeSH Terms: Allosteric Regulation, Molecular Structure, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
2 Members
0 Resources
4 MeSH Terms
The abundant DNA adduct -methyl deoxyguanosine contributes to miscoding during replication by human DNA polymerase η.
Njuma OJ, Su Y, Guengerich FP
(2019) J Biol Chem 294: 10253-10265
MeSH Terms: DNA Adducts, DNA Damage, DNA Repair, DNA Replication, DNA-Directed DNA Polymerase, Deoxyguanosine, Humans, Molecular Structure
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
Oxidation of Flavone, 5-Hydroxyflavone, and 5,7-Dihydroxyflavone to Mono-, Di-, and Tri-Hydroxyflavones by Human Cytochrome P450 Enzymes.
Nagayoshi H, Murayama N, Kakimoto K, Tsujino M, Takenaka S, Katahira J, Lim YR, Kim D, Yamazaki H, Komori M, Guengerich FP, Shimada T
(2019) Chem Res Toxicol 32: 1268-1280
MeSH Terms: Cytochrome P-450 Enzyme System, Flavones, Flavonoids, Humans, Molecular Structure, Oxidation-Reduction
Added March 3, 2020
0 Communities
1 Members
0 Resources
6 MeSH Terms