Thakur GA - Search Results

1

New Alpha9 nAChR Ligands Based on a 5-(Quinuclidin-3-ylmethyl)-1,2,4-oxadiazole Scaffold.

Dallanoce C, Richter K, Stokes C, Papotto C, Andleeb H, Thakur GA, Kerr A, Grau V, Papke RL. Dallanoce C, et al. Among authors: thakur ga. ACS Chem Neurosci. 2024 Feb 21;15(4):827-843. doi: 10.1021/acschemneuro.3c00720. Epub 2024 Feb 9. ACS Chem Neurosci. 2024. PMID: 38335726

2

Expeditious synthesis, enantiomeric resolution, and enantiomer functional characterization of (4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (4BP-TQS): an allosteric agonist-positive allosteric modulator of α7 nicotinic acetylcholine receptors.

Thakur GA, Kulkarni AR, Deschamps JR, Papke RL. Thakur GA, et al. J Med Chem. 2013 Nov 14;56(21):8943-7. doi: 10.1021/jm401267t. Epub 2013 Oct 25. J Med Chem. 2013. PMID: 24090443 Free PMC article.

3

The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface.

Papke RL, Horenstein NA, Kulkarni AR, Stokes C, Corrie LW, Maeng CY, Thakur GA. Papke RL, et al. Among authors: thakur ga. J Biol Chem. 2014 Feb 14;289(7):4515-31. doi: 10.1074/jbc.M113.524603. Epub 2013 Dec 20. J Biol Chem. 2014. PMID: 24362025 Free PMC article.

4

The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor.

Papke RL, Bagdas D, Kulkarni AR, Gould T, AlSharari SD, Thakur GA, Damaj MI. Papke RL, et al. Among authors: thakur ga. Neuropharmacology. 2015 Apr;91:34-42. doi: 10.1016/j.neuropharm.2014.12.002. Epub 2014 Dec 11. Neuropharmacology. 2015. PMID: 25497451 Free PMC article.

5

Critical Molecular Determinants of α7 Nicotinic Acetylcholine Receptor Allosteric Activation: SEPARATION OF DIRECT ALLOSTERIC ACTIVATION AND POSITIVE ALLOSTERIC MODULATION.

Horenstein NA, Papke RL, Kulkarni AR, Chaturbhuj GU, Stokes C, Manther K, Thakur GA. Horenstein NA, et al. Among authors: thakur ga. J Biol Chem. 2016 Mar 4;291(10):5049-67. doi: 10.1074/jbc.M115.692392. Epub 2016 Jan 7. J Biol Chem. 2016. PMID: 26742843 Free PMC article.

6

The α7 nicotinic receptor dual allosteric agonist and positive allosteric modulator GAT107 reverses nociception in mouse models of inflammatory and neuropathic pain.

Bagdas D, Wilkerson JL, Kulkarni A, Toma W, AlSharari S, Gul Z, Lichtman AH, Papke RL, Thakur GA, Damaj MI. Bagdas D, et al. Among authors: thakur ga. Br J Pharmacol. 2016 Aug;173(16):2506-20. doi: 10.1111/bph.13528. Epub 2016 Jul 18. Br J Pharmacol. 2016. PMID: 27243753 Free PMC article.

7

Human Cannabinoid Receptor 2 Ligand-Interaction Motif: Transmembrane Helix 2 Cysteine, C2.59(89), as Determinant of Classical Cannabinoid Agonist Activity and Binding Pose.

Zhou H, Peng Y, Halikhedkar A, Fan P, Janero DR, Thakur GA, Mercier RW, Sun X, Ma X, Makriyannis A. Zhou H, et al. Among authors: thakur ga. ACS Chem Neurosci. 2017 Jun 21;8(6):1338-1347. doi: 10.1021/acschemneuro.7b00003. Epub 2017 Mar 1. ACS Chem Neurosci. 2017. PMID: 28220706

8

Persistent activation of α7 nicotinic ACh receptors associated with stable induction of different desensitized states.

Papke RL, Stokes C, Damaj MI, Thakur GA, Manther K, Treinin M, Bagdas D, Kulkarni AR, Horenstein NA. Papke RL, et al. Among authors: thakur ga. Br J Pharmacol. 2018 Jun;175(11):1838-1854. doi: 10.1111/bph.13851. Epub 2017 Jun 8. Br J Pharmacol. 2018. PMID: 28477386 Free PMC article.

9

The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-α represents a new antinociceptive signaling pathway in mice.

Donvito G, Bagdas D, Toma W, Rahimpour E, Jackson A, Meade JA, AlSharari S, Kulkarni AR, Ivy Carroll F, Lichtman AH, Papke RL, Thakur GA, Imad Damaj M. Donvito G, et al. Among authors: thakur ga. Exp Neurol. 2017 Sep;295:194-201. doi: 10.1016/j.expneurol.2017.06.014. Epub 2017 Jun 9. Exp Neurol. 2017. PMID: 28606623 Free PMC article.

10

Macroscopic and Microscopic Activation of α7 Nicotinic Acetylcholine Receptors by the Structurally Unrelated Allosteric Agonist-Positive Allosteric Modulators (ago-PAMs) B-973B and GAT107.

Quadri M, Garai S, Thakur GA, Stokes C, Gulsevin A, Horenstein NA, Papke RL. Quadri M, et al. Among authors: thakur ga. Mol Pharmacol. 2019 Jan;95(1):43-61. doi: 10.1124/mol.118.113340. Epub 2018 Oct 22. Mol Pharmacol. 2019. PMID: 30348894 Free PMC article.

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