Kyle A. Emmitte, Ph.D. - Publications

Affiliations: 
2001 University of North Carolina, Chapel Hill, Chapel Hill, NC 
Area:
total synthesis of biologically active and structurally novel natural products

40 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2016 Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, ... ... Emmitte KA, et al. 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. Bioorganic & Medicinal Chemistry Letters. PMID 27185330 DOI: 10.1016/j.bmcl.2016.05.010  1
2016 Felts AS, Rodriguez AL, Morrison RD, Venable DF, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. 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. Bioorganic & Medicinal Chemistry Letters. PMID 26988308 DOI: 10.1016/j.bmcl.2016.03.026  1
2016 Lindsley CW, Emmitte KA, Hopkins CR, Bridges TM, Gregory KJ, Niswender CM, Conn PJ. Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors. Chemical Reviews. PMID 26882314 DOI: 10.1021/acs.chemrev.5b00656  1
2016 Huang F, Goyal N, Sullivan K, Hanamshet K, Patel M, Mazina OM, Wang CX, An WF, Spoonamore J, Metkar S, Emmitte KA, Cocklin S, Skorski T, Mazin AV. Targeting BRCA1- and BRCA2-deficient cells with RAD52 small molecule inhibitors. Nucleic Acids Research. PMID 26873923 DOI: 10.1093/nar/gkw087  1
2015 Felts AS, Rodriguez AL, Smith KA, Engers JL, Morrison RD, Byers FW, Blobaum AL, Locuson CW, Chang S, Venable DF, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Emmitte KA. Design of 4-oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as selective negative allosteric modulators of metabotropic glutamate receptor subtype 2. Journal of Medicinal Chemistry. PMID 26524606 DOI: 10.1021/acs.jmedchem.5b01371  1
2015 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, et al. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. Journal of Medicinal Chemistry. 58: 7485-500. PMID 26335039 DOI: 10.1021/acs.jmedchem.5b01005  1
2015 Gould RW, Amato RJ, Bubser M, Joffe ME, Nedelcovych MT, Thompson AD, Nickols HH, Yuh JP, Zhan X, Felts AS, Rodriguez AL, Morrison RD, Byers FW, Rook JM, Daniels JS, ... ... Emmitte KA, et al. Partial mGlu5 Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. PMID 26315507 DOI: 10.1038/npp.2015.265  1
2015 Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, ... ... Emmitte KA, et al. Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes. Cell. 161: 1252-1265. PMID 26046436 DOI: 10.1016/j.cell.2015.05.023  1
2015 Walker AG, Wenthur CJ, Xiang Z, Rook JM, Emmitte KA, Niswender CM, Lindsley CW, Conn PJ. Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction. Proceedings of the National Academy of Sciences of the United States of America. 112: 1196-201. PMID 25583490 DOI: 10.1073/pnas.1416196112  1
2015 Rook JM, Tantawy MN, Ansari MS, Felts AS, Stauffer SR, Emmitte KA, Kessler RM, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ. Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 40: 755-65. PMID 25241804 DOI: 10.1038/npp.2014.245  1
2014 Bates BS, Rodriguez AL, Felts AS, Morrison RD, Venable DF, Blobaum AL, Byers FW, Lawson KP, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorganic & Medicinal Chemistry Letters. 24: 3307-14. PMID 24969015 DOI: 10.1016/j.bmcl.2014.06.003  1
2014 Cho HP, Engers DW, Venable DF, Niswender CM, Lindsley CW, Conn PJ, Emmitte KA, Rodriguez AL. A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors. Acs Chemical Neuroscience. 5: 597-610. PMID 24798819 DOI: 10.1021/cn5000343  1
2014 Gregory KJ, Nguyen ED, Malosh C, Mendenhall JL, Zic JZ, Bates BS, Noetzel MJ, Squire EF, Turner EM, Rook JM, Emmitte KA, Stauffer SR, Lindsley CW, Meiler J, Conn PJ. Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site. Acs Chemical Neuroscience. 5: 282-95. PMID 24528109 DOI: 10.1021/cn400225x  1
2013 Felts AS, Rodriguez AL, Morrison RD, Venable DF, Manka JT, Bates BS, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA. Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorganic & Medicinal Chemistry Letters. 23: 5779-85. PMID 24074843 DOI: 10.1016/j.bmcl.2013.09.001  1
2013 Manka JT, Rodriguez AL, Morrison RD, Venable DF, Cho HP, Blobaum AL, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1. Bioorganic & Medicinal Chemistry Letters. 23: 5091-6. PMID 23932792 DOI: 10.1016/j.bmcl.2013.07.029  1
2013 Lovell KM, Felts AS, Rodriguez AL, Venable DF, Cho HP, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorganic & Medicinal Chemistry Letters. 23: 3713-8. PMID 23727046 DOI: 10.1016/j.bmcl.2013.05.020  1
2013 Wenthur CJ, Morrison R, Felts AS, Smith KA, Engers JL, Byers FW, Daniels JS, Emmitte KA, Conn PJ, Lindsley CW. Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM). Journal of Medicinal Chemistry. 56: 5208-12. PMID 23718281 DOI: 10.1021/jm400439t  1
2013 Amato RJ, Felts AS, Rodriguez AL, Venable DF, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Jones CK, Emmitte KA. Substituted 1-Phenyl-3-(pyridin-2-yl)urea negative allosteric modulators of mGlu5: discovery of a new tool compound VU0463841 with activity in rat models of cocaine addiction. Acs Chemical Neuroscience. 4: 1217-28. PMID 23682684 DOI: 10.1021/cn400070k  1
2012 Gregory KJ, Noetzel MJ, Rook JM, Vinson PN, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM, Conn PJ. Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships. Molecular Pharmacology. 82: 860-75. PMID 22863693 DOI: 10.1124/mol.112.080531  1
2012 Morrison RD, Blobaum AL, Byers FW, Santomango TS, Bridges TM, Stec D, Brewer KA, Sanchez-Ponce R, Corlew MM, Rush R, Felts AS, Manka J, Bates BS, Venable DF, Rodriguez AL, ... ... Emmitte KA, et al. The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5. Drug Metabolism and Disposition: the Biological Fate of Chemicals. 40: 1834-45. PMID 22711749 DOI: 10.1124/dmd.112.046136  1
2012 Mueller R, Dawson ES, Meiler J, Rodriguez AL, Chauder BA, Bates BS, Felts AS, Lamb JP, Menon UN, Jadhav SB, Kane AS, Jones CK, Gregory KJ, Niswender CM, Conn PJ, ... ... Emmitte KA, et al. Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGluâ‚…): from an artificial neural network virtual screen to an in vivo tool compound. Chemmedchem. 7: 406-14. PMID 22267125 DOI: 10.1002/cmdc.201100510  1
2012 Theriault JR, Felts AS, Bates BS, Perez JR, Palmer M, Gilbert SR, Dawson ES, Engers JL, Lindsley CW, Emmitte KA. Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway. Bioorganic & Medicinal Chemistry Letters. 22: 76-81. PMID 22172704 DOI: 10.1016/j.bmcl.2011.11.077  1
2012 Melancon BJ, Hopkins CR, Wood MR, Emmitte KA, Niswender CM, Christopoulos A, Conn PJ, Lindsley CW. Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. Journal of Medicinal Chemistry. 55: 1445-64. PMID 22148748 DOI: 10.1021/jm201139r  1
2011 Lindsley CW, Bates BS, Menon UN, Jadhav SB, Kane AS, Jones CK, Rodriguez AL, Conn PJ, Olsen CM, Winder DG, Emmitte KA. (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction. Acs Chemical Neuroscience. 2: 471-482. PMID 21927650 DOI: 10.1021/cn100099n  1
2009 Crimmins MT, Ellis JM, Emmitte KA, Haile PA, McDougall PJ, Parrish JD, Zuccarello JL. Enantioselective total synthesis of brevetoxin A: unified strategy for the B, E, G, and J subunits. Chemistry (Weinheim An Der Bergstrasse, Germany). 15: 9223-34. PMID 19650091 DOI: 10.1002/chem.200900776  1
2009 Sabbatini P, Rowand JL, Groy A, Korenchuk S, Liu Q, Atkins C, Dumble M, Yang J, Anderson K, Wilson BJ, Emmitte KA, Rabindran SK, Kumar R. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 15: 3058-67. PMID 19383820 DOI: 10.1158/1078-0432.CCR-08-2530  1
2009 Emmitte KA, Adjabeng GM, Adjebang GM, Andrews CW, Alberti JG, Bambal R, Chamberlain SD, Davis-Ward RG, Dickson HD, Hassler DF, Hornberger KR, Jackson JR, Kuntz KW, Lansing TJ, Mook RA, et al. Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorganic & Medicinal Chemistry Letters. 19: 1694-7. PMID 19237286 DOI: 10.1016/j.bmcl.2009.01.094  1
2009 Emmitte KA, Wilson BJ, Baum EW, Emerson HK, Kuntz KW, Nailor KE, Salovich JM, Smith SC, Cheung M, Gerding RM, Stevens KL, Uehling DE, Mook RA, Moorthy GS, Dickerson SH, et al. Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R). Bioorganic & Medicinal Chemistry Letters. 19: 1004-8. PMID 19101143 DOI: 10.1016/j.bmcl.2008.11.058  1
2009 Crimmins MT, Zuccarello JL, Ellis JM, McDougall PJ, Haile PA, Parrish JD, Emmitte KA. Total synthesis of brevetoxin A. Organic Letters. 11: 489-92. PMID 19099481 DOI: 10.1021/ol802710u  1
2009 Emmitte KA, Andrews CW, Badiang JG, Davis-Ward RG, Dickson HD, Drewry DH, Emerson HK, Epperly AH, Hassler DF, Knick VB, Kuntz KW, Lansing TJ, Linn JA, Mook RA, Nailor KE, et al. Discovery of thiophene inhibitors of polo-like kinase. Bioorganic & Medicinal Chemistry Letters. 19: 1018-21. PMID 19097784 DOI: 10.1016/j.bmcl.2008.11.041  1
2009 Emmitte KA, Adjabeng GM, Webb Andrews C, Badiang Alberti JG, Bambal R, Chamberlain SD, Davis-Ward RG, Dickson HD, Hassler DF, Hornberger KR, Jackson JR, Kuntz KW, Lansing TJ, Mook RA, Nailor KE, et al. Corrigendum to "Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding" [Bioorg. Med. Chem. Lett. 19 (2009) 1694] (DOI:10.1016/j.bmcl.2009.01.094) Bioorganic and Medicinal Chemistry Letters. 19: 2604. DOI: 10.1016/j.bmcl.2009.01.114  1
2009 Kuntz KW, Emmitte KA. Discovery of GSK461364: A Polo-Like Kinase 1 Inhibitor for the Treatment of Cancer Kinase Inhibitor Drugs. 351-364. DOI: 10.1002/9780470524961.ch14  1
2008 Hornberger KR, Badiang JG, Salovich JM, Kuntz KW, Emmitte KA, Cheung M. Regioselective synthesis of benzimidazole thiophene inhibitors of polo-like kinase 1 Tetrahedron Letters. 49: 6348-6351. DOI: 10.1016/j.tetlet.2008.08.077  1
2005 Crimmins MT, McDougall PJ, Emmitte KA. A convergent coupling strategy for the formation of polycyclic ethers: stereoselective synthesis of the BCDE fragment of brevetoxin A. Organic Letters. 7: 4033-6. PMID 16119960 DOI: 10.1021/ol051543m  1
2004 Crimmins MT, Diaz CJ, Emmitte KA. A unified approach to the enantioselective synthesis of 2,6-cis and trans disubstituted tetrahydropyranones Heterocycles. 62: 179-183.  1
2002 Crimmins MT, Emmitte KA, Choy AL. Ring closing metathesis for the formation of medium ring ethers: The total synthesis of (-)-isolaurallene Tetrahedron. 58: 1817-1834. DOI: 10.1016/S0040-4020(02)00040-6  1
2001 Crimmins MT, Emmitte KA. Asymmetric total synthesis of (-)-isolaurallene. Journal of the American Chemical Society. 123: 1533-4. PMID 11456742 DOI: 10.1021/ja005892h  1
2000 Crimmins MT, Emmitte KA, Katz JD. Diastereoselective alkylations of oxazolidinone glycolates: a useful extension of the Evans asymmetric alkylation. Organic Letters. 2: 2165-7. PMID 10891257  1
2000 Crimmins MT, Emmitte KA. An efficient strategy for the synthesis of α,α'-cis and trans- disubstituted medium ring ethers Synthesis. 899-903.  1
1999 Crimmins MT, Emmitte KA. Total synthesis of (+)-laurencin: an asymmetric alkylation-ring-closing metathesis approach to medium ring ethers. Organic Letters. 1: 2029-32. PMID 10836060  1
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