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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 46

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The delta isoform of phosphatidylinositol-3-kinase predominates in chronic myelomonocytic leukemia and can be targeted effectively with umbralisib and ruxolitinib.
Villaume MT, Arrate MP, Ramsey HE, Sunthankar KI, Jenkins MT, Moyo TK, Smith BN, Fischer MA, Childress MA, Gorska AE, Ferrell PB, Savona MR
(2021) Exp Hematol 97: 57-65.e5
MeSH Terms: Cell Line, Tumor, Cell Survival, Class I Phosphatidylinositol 3-Kinases, Drug Synergism, Heterocyclic Compounds, 4 or More Rings, Humans, Leukemia, Myelomonocytic, Chronic, Molecular Targeted Therapy, Nitriles, Phosphoinositide-3 Kinase Inhibitors, Pyrazoles, Pyrimidines
Added September 1, 2022
0 Communities
1 Members
0 Resources
MeSH Terms
Greater Weight Gain in Treatment-naive Persons Starting Dolutegravir-based Antiretroviral Therapy.
Bourgi K, Rebeiro PF, Turner M, Castilho JL, Hulgan T, Raffanti SP, Koethe JR, Sterling TR
(2020) Clin Infect Dis 70: 1267-1274
MeSH Terms: Adult, Female, HIV Infections, HIV Integrase Inhibitors, Heterocyclic Compounds, 3-Ring, Humans, Male, Oxazines, Piperazines, Pyridones, Reverse Transcriptase Inhibitors, Weight Gain
Added December 11, 2019
0 Communities
1 Members
0 Resources
12 MeSH Terms
Surveying heterocycles as amide bioisosteres within a series of mGlu NAMs: Discovery of VU6019278.
Reed CW, Washecheck JP, Quitlag MC, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 1211-1214
MeSH Terms: Allosteric Regulation, Amides, Animals, Central Nervous System, Hepatocytes, Heterocyclic Compounds, Inhibitory Concentration 50, Pyrazoles, Rats, Receptors, Metabotropic Glutamate, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu PAM development candidate.
Panarese JD, Engers DW, Wu YJ, Guernon JM, Chun A, Gregro AR, Bender AM, Capstick RA, Wieting JM, Bronson JJ, Macor JE, Westphal R, Soars M, Engers JE, Felts AS, Rodriguez AL, Emmitte KA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 342-346
MeSH Terms: Allosteric Regulation, Dose-Response Relationship, Drug, Drug Discovery, Heterocyclic Compounds, 2-Ring, Humans, Isoquinolines, Molecular Structure, Myotonin-Protein Kinase, Receptors, Metabotropic Glutamate, Structure-Activity Relationship
Added March 3, 2020
0 Communities
2 Members
0 Resources
MeSH Terms
Pore Polarity and Charge Determine Differential Block of Kir1.1 and Kir7.1 Potassium Channels by Small-Molecule Inhibitor VU590.
Kharade SV, Sheehan JH, Figueroa EE, Meiler J, Denton JS
(2017) Mol Pharmacol 92: 338-346
MeSH Terms: HEK293 Cells, Heterocyclic Compounds, 1-Ring, Humans, Mutation, Potassium Channel Blockers, Potassium Channels, Inwardly Rectifying, Structure-Activity Relationship
Added September 15, 2017
0 Communities
2 Members
0 Resources
7 MeSH Terms
Functional Redundancy Between Canonical Endocannabinoid Signaling Systems in the Modulation of Anxiety.
Bedse G, Hartley ND, Neale E, Gaulden AD, Patrick TA, Kingsley PJ, Uddin MJ, Plath N, Marnett LJ, Patel S
(2017) Biol Psychiatry 82: 488-499
MeSH Terms: Adaptation, Ocular, Animals, Anti-Anxiety Agents, Anxiety, Arachidonic Acids, Benzodioxoles, Brain, Cannabinoid Receptor Agonists, Cyclohexanols, Disease Models, Animal, Dronabinol, Endocannabinoids, Excitatory Postsynaptic Potentials, Glycerides, Heterocyclic Compounds, 1-Ring, Locomotion, Male, Mice, Mice, Inbred ICR, Piperidines, Polyunsaturated Alkamides, Pyridines, Signal Transduction
Added April 26, 2017
0 Communities
3 Members
0 Resources
23 MeSH Terms
Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel M PAM VU6004256.
Grannan MD, Mielnik CA, Moran SP, Gould RW, Ball J, Lu Z, Bubser M, Ramsey AJ, Abe M, Cho HP, Nance KD, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW, Jones CK
(2016) ACS Chem Neurosci 7: 1706-1716
MeSH Terms: Action Potentials, Animals, Cholinergic Agents, Cognition Disorders, Conditioning, Psychological, Disease Models, Animal, Drug Evaluation, Preclinical, Fear, Gene Knockdown Techniques, Heterocyclic Compounds, 4 or More Rings, Long-Term Synaptic Depression, Male, Mice, 129 Strain, Mice, Inbred C57BL, Mice, Transgenic, Motor Activity, Nerve Tissue Proteins, Nootropic Agents, Prefrontal Cortex, Pyramidal Cells, Receptors, N-Methyl-D-Aspartate, Recognition, Psychology, Tissue Culture Techniques
Added April 6, 2017
0 Communities
3 Members
0 Resources
23 MeSH Terms
Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration.
Panarese JD, Cho HP, Adams JJ, Nance KD, Garcia-Barrantes PM, Chang S, Morrison RD, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW
(2016) Bioorg Med Chem Lett 26: 3822-5
MeSH Terms: Allosteric Regulation, Animals, Central Nervous System, Central Nervous System Agents, Dose-Response Relationship, Drug, Drug Discovery, Heterocyclic Compounds, Molecular Structure, Pyridines, Pyrroles, Rats, Receptor, Muscarinic M1, Structure-Activity Relationship
Added April 6, 2017
0 Communities
2 Members
0 Resources
13 MeSH Terms
Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.
Garcia-Barrantes PM, Cho HP, Metts AM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW
(2016) Bioorg Med Chem Lett 26: 751-756
MeSH Terms: Allosteric Regulation, Animals, Antipsychotic Agents, Coumarins, Furans, Half-Life, Heterocyclic Compounds, Humans, Protein Binding, Rats, Receptors, Metabotropic Glutamate, Schizophrenia, Structure-Activity Relationship
Added February 18, 2016
0 Communities
2 Members
0 Resources
13 MeSH Terms
Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.
Engers JL, Rodriguez AL, Konkol LC, Morrison RD, Thompson AD, Byers FW, Blobaum AL, Chang S, Venable DF, Loch MT, Niswender CM, Daniels JS, Jones CK, Conn PJ, Lindsley CW, Emmitte KA
(2015) J Med Chem 58: 7485-500
MeSH Terms: Allosteric Regulation, Animals, Anti-Anxiety Agents, Antidepressive Agents, Brain, Calcium, Dogs, Heterocyclic Compounds, 2-Ring, Humans, Madin Darby Canine Kidney Cells, Mice, Microsomes, Liver, Permeability, Pyridines, Rats, Receptors, Metabotropic Glutamate, Stereoisomerism, Structure-Activity Relationship
Added February 18, 2016
0 Communities
3 Members
0 Resources
18 MeSH Terms