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  • Kyle Emmitte
2019

Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

Felts, A. S., Bollinger, K. A., Brassard, C. J., Rodriguez, A. L., Morrison, R. D., Scott Daniels, J., Blobaum, A. L., Niswender, C. M., Jones, C. K., Jeffrey Conn, P., Emmitte, K. A. & Lindsley, C. W., 1 Jan 2019, In : Bioorganic and Medicinal Chemistry Letters. 29, 1, p. 47-50 4 p.

Research output: Contribution to journalArticle

1 Scopus citations

Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu 2 ) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores

Childress, E. S., Wieting, J. M., Felts, A. S., Breiner, M. M., Long, M. F., Luscombe, V. B., Rodriguez, A. L., Cho, H. P., Blobaum, A. L., Niswender, C. M., Emmitte, K. A., Conn, P. J. & Lindsley, C. W., 1 Oct 2019, In : Journal of Medicinal Chemistry. 62, 1, p. 378-384 7 p.

Research output: Contribution to journalArticle

3 Scopus citations

Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M 1 Positive Allosteric Modulators

Engers, J. L., Bender, A. M., Kalbfleisch, J. J., Cho, H. P., Lingenfelter, K. S., Luscombe, V. B., Han, C., Melancon, B. J., Blobaum, A. L., Dickerson, J. W., Rook, J. M., Niswender, C. M., Emmitte, K. A., Conn, P. J. & Lindsley, C. W., 20 Mar 2019, In : ACS Chemical Neuroscience. 10, 3, p. 1035-1042 8 p.

Research output: Contribution to journalArticle

1 Scopus citations

Discovery of VU2957 (Valiglurax): An mGlu 4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease

Panarese, J. D., Engers, D. W., Wu, Y. J., Bronson, J. J., Macor, J. E., Chun, A., Rodriguez, A. L., Felts, A. S., Engers, J. L., Loch, M. T., Emmitte, K. A., Castelhano, A. L., Kates, M. J., Nader, M. A., Jones, C. K., Blobaum, A. L., Conn, P. J., Niswender, C. M., Hopkins, C. R. & Lindsley, C. W., 14 Mar 2019, In : ACS Medicinal Chemistry Letters. 10, 3, p. 255-260 6 p.

Research output: Contribution to journalArticle

6 Scopus citations

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate

Panarese, J. D., Engers, D. W., Wu, Y. J., Guernon, J. M., Chun, A., Gregro, A. R., Bender, A. M., Capstick, R. A., Wieting, J. M., Bronson, J. J., Macor, J. E., Westphal, R., Soars, M., Engers, J. E., Felts, A. S., Rodriguez, A. L., Emmitte, K. A., Jones, C. K., Blobaum, A. L., Jeffrey Conn, P. & 3 others, Niswender, C. M., Hopkins, C. R. & Lindsley, C. W., 15 Jan 2019, In : Bioorganic and Medicinal Chemistry Letters. 29, 2, p. 342-346 5 p.

Research output: Contribution to journalArticle

2 Scopus citations
2018

Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

Felts, A. S., Rodriguez, A. L., Morrison, R. D., Blobaum, A. L., Byers, F. W., Daniels, J. S., Niswender, C. M., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 1 Jun 2018, In : Bioorganic and Medicinal Chemistry Letters. 28, 10, p. 1679-1685 7 p.

Research output: Contribution to journalArticle

1 Scopus citations

Stress and interferon signalling-mediated apoptosis contributes to pleiotropic anticancer responses induced by targeting NGLY1

Zolekar, A., Lin, V. J. T., Mishra, N. M., Ho, Y. Y., Hayatshahi, H. S., Parab, A., Sampat, R., Liao, X., Hoffmann, P., Liu, J., Emmitte, K. A. & Wang, Y. C., 11 Dec 2018, In : British Journal of Cancer. 119, 12, p. 1538-1551 14 p.

Research output: Contribution to journalArticle

3 Scopus citations
2017

Co-activation of metabotropic glutamate receptor 3 and beta-adrenergic receptors modulates cyclic-AMP and long-term potentiation, and disrupts memory reconsolidation

Walker, A. G., Sheffler, D. J., Lewis, A. S., Dickerson, J. W., Foster, D. J., Senter, R. K., Moehle, M. S., Lv, X., Stansley, B. J., Xiang, Z., Rook, J. M., Emmitte, K. A., Lindsley, C. W. & Conn, P. J., 1 Dec 2017, In : Neuropsychopharmacology. 42, 13, p. 2553-2566 14 p.

Research output: Contribution to journalArticle

7 Scopus citations

Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core

Bollinger, K. A., Felts, A. S., Brassard, C. J., Engers, J. L., Rodriguez, A. L., Weiner, R. L., Cho, H. P., Chang, S., Bubser, M., Jones, C. K., Blobaum, A. L., Niswender, C. M., Conn, P. J., Emmitte, K. A. & Lindsley, C. W., 1 Jan 2017, In : ACS Medicinal Chemistry Letters. 8, 9, p. 919-924 6 p.

Research output: Contribution to journalArticle

13 Scopus citations

Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs

Engers, J. L., Bollinger, K. A., Weiner, R. L., Rodriguez, A. L., Long, M. F., Breiner, M. M., Chang, S., Bollinger, S. R., Bubser, M., Jones, C. K., Morrison, R. D., Bridges, T. M., Blobaum, A. L., Niswender, C. M., Conn, P. J., Emmitte, K. A. & Lindsley, C. W., 1 Jan 2017, In : ACS Medicinal Chemistry Letters. 8, 9, p. 925-930 6 p.

Research output: Contribution to journalArticle

12 Scopus citations

Development and kilogram-scale synthesis of mGlu5 negative allosteric modulator VU0424238 (auglurant)

David, T. K., Prashanth, N. K., Rajendraswami, M., Pallalu, D., Castelhano, A. L., Kates, M. J., Blobaum, A. L., Jones, C. K., Emmitte, K. A., Conn, P. J. & Lindsley, C. W., 6 Sep 2017, In : Tetrahedron Letters. 58, 36, p. 3554-3558 5 p.

Research output: Contribution to journalArticle

1 Scopus citations

Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

Felts, A. S., Rodriguez, A. L., Morrison, R. D., Bollinger, K. A., Venable, D. F., Blobaum, A. L., Byers, F. W., Thompson Gray, A., Daniels, J. S., Niswender, C. M., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 1 Nov 2017, In : Bioorganic and Medicinal Chemistry Letters. 27, 21, p. 4858-4866 9 p.

Research output: Contribution to journalArticle

5 Scopus citations

Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation

Felts, A. S., Rodriguez, A. L., Blobaum, A. L., Morrison, R. D., Bates, B. S., Thompson Gray, A., Rook, J. M., Tantawy, M. N., Byers, F. W., Chang, S., Venable, D. F., Luscombe, V. B., Tamagnan, G. D., Niswender, C. M., Daniels, J. S., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 22 Jun 2017, In : Journal of Medicinal Chemistry. 60, 12, p. 5072-5085 14 p.

Research output: Contribution to journalArticle

14 Scopus citations

mGlu5 negative allosteric modulators: a patent review (2013 - 2016)

Emmitte, K. A., 3 Jun 2017, In : Expert Opinion on Therapeutic Patents. 27, 6, p. 691-706 16 p.

Research output: Contribution to journalReview article

14 Scopus citations
2016

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, M. R., Noetzel, M. J., Engers, J. L., Bollinger, K. A., Melancon, B. J., Tarr, J. C., Han, C., West, M., Gregro, A. R., Lamsal, A., Chang, S., Ajmera, S., Smith, E., Chase, P., Hodder, P. S., Bubser, M., Jones, C. K., Hopkins, C. R., Emmitte, K. A., Niswender, C. M. & 5 others, Wood, M. W., Duggan, M. E., Conn, P. J., Bridges, T. M. & Lindsley, C. W., 1 Jul 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 13, p. 3029-3033 5 p.

Research output: Contribution to journalArticle

17 Scopus citations

Evaluating the disposition of a mixed aldehyde oxidase/cytochrome P450 substrate in rats with attenuated P450 activity

Crouch, R. D., Morrison, R. D., Byers, F. W., Lindsley, C. W., Emmitte, K. A. & Daniels, J. S., Aug 2016, In : Drug Metabolism and Disposition. 44, 8, p. 1296-1303 8 p.

Research output: Contribution to journalArticle

8 Scopus citations

N-Alkylpyrido[1′,2′:1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents

Felts, A. S., Rodriguez, A. L., Morrison, R. D., Venable, D. F., Blobaum, A. L., Byers, F. W., Daniels, J. S., Niswender, C. M., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 15 Apr 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 8, p. 1894-1900 7 p.

Research output: Contribution to journalArticle

5 Scopus citations

Partial mGlu 5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects

Gould, R. W., Amato, R. J., Bubser, M., Joffe, M. E., Nedelcovych, M. T., Thompson, A. D., Nickols, H. H., Yuh, J. P., Zhan, X., Felts, A. S., Rodriguez, A. L., Morrison, R. D., Byers, F. W., Rook, J. M., Daniels, J. S., Niswender, C. M., Conn, P. J., Emmitte, K. A., Lindsley, C. W. & Jones, C. K., 1 Mar 2016, In : Neuropsychopharmacology. 41, 4, p. 1166-1178 13 p.

Research output: Contribution to journalArticle

21 Scopus citations

Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors

Lindsley, C. W., Emmitte, K. A., Hopkins, C. R., Bridges, T. M., Gregory, K. J., Niswender, C. M. & Conn, P. J., 8 Jun 2016, In : Chemical Reviews. 116, 11, p. 6707-6741 35 p.

Research output: Contribution to journalReview article

95 Scopus citations

Targeting BRCA1-and BRCA2-deficient cells with RAD52 small molecule inhibitors

Huang, F., Goyal, N., Sullivan, K., Hanamshet, K., Patel, M., Mazina, O. M., Wang, C. X., An, W. F., Spoonamore, J., Metkar, S., Emmitte, K. A., Cocklin, S., Skorski, T. & Mazin, A. V., 19 May 2016, In : Nucleic Acids Research. 44, 9, p. 4189-4199 11 p.

Research output: Contribution to journalArticle

35 Scopus citations

VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy

Nickols, H. H., Yuh, J. P., Gregory, K. J., Morrison, R. D., Bates, B. S., Stauffer, S. R., Emmitte, K. A., Bubser, M., Peng, W., Nedelcovych, M. T., Thompson, A., Lv, X., Xiang, Z., Daniels, J. S., Niswender, C. M., Lindsley, C. W., Jones, C. K. & Conn, P. J., 1 Jan 2016, In : The Journal of pharmacology and experimental therapeutics. 356, 1, p. 123-136 14 p.

Research output: Contribution to journalArticle

25 Scopus citations
2015

Advancing biological understanding and therapeutics discovery with small-molecule probes

Schreiber, S. L., Kotz, J. D., Li, M., Aubé, J., Austin, C. P., Reed, J. C., Rosen, H., White, E. L., Sklar, L. A., Lindsley, C. W., Alexander, B. R., Bittker, J. A., Clemons, P. A., De Souza, A., Foley, M. A., Palmer, M., Shamji, A. F., Wawer, M. J., McManus, O., Wu, M. & 26 others, Zou, B., Yu, H., Golden, J. E., Schoenen, F. J., Simeonov, A., Jadhav, A., Jackson, M. R., Pinkerton, A. B., Chung, T. D. Y., Griffin, P. R., Cravatt, B. F., Hodder, P. S., Roush, W. R., Roberts, E., Chung, D. H., Jonsson, C. B., Noah, J. W., Severson, W. E., Ananthan, S., Edwards, B., Oprea, T. I., Conn, P. J., Hopkins, C. R., Wood, M. R., Stauffer, S. R. & Emmitte, K. A., 1 Jan 2015, In : Cell. 161, 6, p. 1252-1265 14 p.

Research output: Contribution to journalReview article

78 Scopus citations

Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2

Felts, A. S., Rodriguez, A. L., Smith, K. A., Engers, J. L., Morrison, R. D., Byers, F. W., Blobaum, A. L., Locuson, C. W., Chang, S., Venable, D. F., Niswender, C. M., Daniels, J. S., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 25 Nov 2015, In : Journal of Medicinal Chemistry. 58, 22, p. 9027-9040 14 p.

Research output: Contribution to journalArticle

20 Scopus citations

Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents

Engers, J. L., Rodriguez, A. L., Konkol, L. C., Morrison, R. D., Thompson, A. D., Byers, F. W., Blobaum, A. L., Chang, S., Venable, D. F., Loch, M. T., Niswender, C. M., Daniels, J. S., Jones, C. K., Conn, P. J., Lindsley, C. W. & Emmitte, K. A., 24 Sep 2015, In : Journal of Medicinal Chemistry. 58, 18, p. 7485-7500 16 p.

Research output: Contribution to journalArticle

30 Scopus citations

Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction

Walker, A. G., Wenthur, C. J., Xiang, Z., Rook, J. M., Emmitte, K. A., Niswender, C. M., Lindsley, C. W. & Conn, P. J., 27 Jan 2015, In : Proceedings of the National Academy of Sciences of the United States of America. 112, 4, p. 1196-1201 6 p.

Research output: Contribution to journalArticle

56 Scopus citations

Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles

Rook, J. M., Tantawy, M. N., Ansari, M. S., Felts, A. S., Stauffer, S. R., Emmitte, K. A., Kessler, R. M., Niswender, C. M., Daniels, J. S., Jones, C. K., Lindsley, C. W. & Conn, P. J., Feb 2015, In : Neuropsychopharmacology. 40, 3, p. 755-765 11 p.

Research output: Contribution to journalArticle

22 Scopus citations