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54. “Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1”, Wen, W.; Wang, Y.; McManus, O. B.; Wu, M.; Li, M.; Lindsley, C. W.; Dong, X.*; Hopkins, C. R.*Chem. Med. Chem.2015, 10, 57-61. DOI: 10.1002/cmdc.201402277. PMID: 25209672.
53. “Discovery and characterization of a potent and selective inhibitor of Aedes aegypti inward rectifier potassium channels”, Raphemot, R.; Rouhier, M. F.; Swale, D. R.; Days, E.; Weaver, C. D.; Lovell, K. M.; Konkel, L. C.; Engers, D. W.; Bollinger, S. R.; Hopkins, C. R.; Piermarini, P. M.; Denton, J. S. PLoS One2014, 9, e110772. DOI: 10.1371/journal.pone.0110772.
52. “Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7”, Jalan-Sakrikar, N.; Field, J. R.; Klar, R.; Mattmann, M. E.; Gregory, K. J.; Zamorano, R.; Engers, D. W.; Bollinger, S. R.; Weaver, C. D.; Days, E. L.; Utley, T. J.; Hurtado, M.; Rigault, D.; Acher, F.; Walker, A. G.; Melancon, B. J.; Wood, M. R.; Lindsley, C. W.; Conn, P. J.; Xiang, X.; Hopkins, C. R.; Niswender, C. M.* ACS Chem. Neurosci.2014, 5, 1221-1237. DOI: 10.1021/cn5000153z. PMID: 25225882.
51. “Inhibition of BMP Signaling Suppresses Metastasis in Mammary Cancer”, Owens, P.; Pickup, M. W.; Novitskiy, S. V.; Giltnane, J. M.; Gorska, A. E.; Hopkins, C. R.; Hong, C. C.*; Moses, H. L.* Oncogene2014, Advance online publication, 7 July 2014; DOI: 10.1038/onc.2014.189. PMID: 24998846.
50. “Specific Activin Receptor-Like Kinase 3 Inhibitors Enhance Liver Regeneration”, Tsugawa, D.; Oya, Y.; Masuzaki, R.; Ray, K.; Engers, D. W.; Dib, M.; Ho, K.; Do, N.; Kuramitsu, K.; Yu, P.; Bloch, K.; Lindsley, C. W.; Hopkins, C. R.; Hong, C. C.; Karp, S.* J. Pharmacol. Exper. Ther.2014, 351, 549-558. DOI: 10.1124/jpet.114.216903. PMID: 25271257.
49. “Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics: development of novel mGlu1 PAMs via ‘double molecular switch’ of an mGlu4 PAM chemotype”, Cho, H. P.; Garcia-Barrantes, P. M.; Brogan, J. T.; Hopkins, C. R.; Niswender, C. M.; Morrison, R. D.; Bubser, M.; Daniels, J. S.; Jones, C. K.; Conn, P. J.; Lindsley, C. W.* ACS Chem. Biol.2014, 9, 2334-2346. DOI: 10.1021/cb5000560h. PMID: 25137254
For a highlight see: from the SCENEs, “Small Molecules Reactive Receptor Linked With Schizophrenia” Chem. & Eng. News2014, 92 (39), 32.
48. “Discovery and characterization of ML398, a potent and selective chiral morpholine-based antagonist of the dopamine 4 (D4) receptor with in vivo activity in a cocaine-induced hyperlocomotion assay”, Berry, C. B.; Bubser, M.; Jones, C. K.; Hayes, J. P.; Wepy, J. A.; Locuson, C. W.; Daniels, J. S.; Lindsley, C. W.; Hopkins, C. R.*ACS Med. Chem. Lett.2014, 5, 1060-1064. DOI: 10.1021/ml500267c. PMID: 25221667.
47. “TRPC5 inhibition protects against kidney filter damage”, Schaldecker, T.; Kim, S.; Tarabanis, C.; Tian, D.; Hakroush, S.; Castonguay, P.; Ahn, W.; Wallentin, H.; Heid, H.; Hopkins, C. R.; Lindsley, C. W.; Riccio, A.; Buvall, L.; Weins, A.; Greka, A.* J. Clin. Invest.2013, 123, 5298-5309. DOI: 10.1172/JCI71165. PMID: 24231357.
Highlighted in Science Daily: “Blocking signal-transmitting cellular pores may prevent kidney damage”, Nov. 15, 2013.
Manuscript highlighted in Nature Reviews Drug Discovery: Flemming, A. “Targeting a Faulty Filter”2014, 13, 101. DOI: 10.1038/nrd4234.
46. “Reversible Inhibitors of Regulators of G-protein Signaling Identified in a High-throughput Cell-based Calcium Signaling Assay”, Storaska, A. J.; Mei, J. P.; Wu, M.; Wade, S. M.; Blazer, L. L.; Sjorgen, B.; Lindsley, C. W.; Hopkins, C. R.; McManus, O.; Neubig, R. R.* Cell. Signaling2013, 25, 2848-2855. DOI: 10.1016/j.cellsig.2013.09.007. PMID: 24041654.
45. “Eliciting renal failure in mosquitoes with a small-molecule inhibitor of inward-rectifying potassium channels”, Raphemot, R.; Rouhier, M. F.; Hopkins, C. R.; Gogliotti, R. D.; Lovell, K.; Hine, R. M.; Beyenbach, K. W.; Denton, J. S.*; Piermarini, P. M.* PLoS ONE2013, 8(5), e64905. DOI: 10.1371/journal.pone.0064905.
44. “Dynamic Subunit Stoichiometry Confers a Progressive Continuum of Pharmacological Sensitivity by KCNQ Channels”, Yu, H.; Lin, Z.; Mattmann, M. E.; Zou, B.; Terrenoire, C.; Wu, M.; McManus, O. B.; Kass, R. S.; Lindsley, C. W.; Hopkins, C. R.*; Li, M.* Proc. Nat. Acad. Sci.2013, 110, 8732-8737. DOI: 10.1073/pnas.1300684110.
43. “Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1,5-a]pyrimidine scaffold of Dorsomorphin: The discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe”, Engers, D. W.; Frist, A. Y.; Lindsley, C. W.; Hong, C. C.; Hopkins, C. R.*Bioorg. Med. Chem. Lett.2013, 23(11), 3248-3252. DOI: 10.1016/j.bmcl.2013.03.113.
42. “Further exploration of M1 allosteric agonists: Subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism”, Sheffler, D. J.; Sevel, C.; Le, U.; Lovell, K. M.; Tarr, J. C.; Carrington, S. J. S.; Cho, H. P.; Digby, G. J.; Niswender, C. M.; Conn, P. J.; Hopkins, C. R.; Wood, M. R.; Lindsley, C. W.* Bioorg. Med. Chem. Lett.2013, 23, 223-227. DOI: 10.1016/j.bmcl.2012.10.132.
41. “Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: Development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia”, Le, U.; Melancon, B. J.; Bridges, T. M.; Vinson, P. N.; Utley, T. J.; Lamsal, A.; Rodriguez, A. L.; Venable, D.; Sheffler, D. J.; Jones, C. K.; Blobaum, A. L.; Wood, M. R.; Daniels, J. S.; Conn, P. J.; Niswender, C. M.; Lindsley, C. W.; Hopkins, C. R.* Bioorg. Med. Chem. Lett.2013, 23, 346-350. DOI: 10.1016/j.bmcl.2012.10.073
40. “Identification and Characterization of a Compound that Protects Cardiac Tissue From Human Ether-à-go-go-Related Gene (hERG)-Related, Drug-Induced Arrhythmias”, Potet, F.; Lorinc, A. N.; Chaigne, S.; Hopkins, C. R.; Venkataraman, R.; Stepanovic, S. Z.; Lewis, L. M.; Days, E.; Sidorov, V. Y.; Engers, D. W.; Zou, B.; Afshartous, D.; Balser, J. R.; Li, M.; Baudenbacher, F. J.; Lindsley, C. W.; Weaver, C. D.; Kuperschmidt, S.* J. Biol. Chem.2012, 287, 39613-39625. DOI: 10.1074/jbc.M112.380162.
39. “The hereditary spastic paraplegia proteins spartin and maspardin interact in a pathway that regulates BMP signaling”, Clowes, V. E.; Edwards, T. L.; Angus, K. L.; Warren, J.; Harbour, M. E.; Hopkins, C. R.; Hong, C. C.; Blackstone, C.; Hanna, M.; Reid, E.* J. Med. Genet., 2012, 49, S94.
38. “DMH1, a novel BMP small molecule inhibitor, increases cardiomyocyte progenitors and promotes cardiac differentiation in mouse embryonic stem cells”, Ao, A.*; Hao, J.; Hopkins, C. R.; Hong, C. C. PLoS ONE2012, 7, e41627. DOI: 10.1371/journal.pone.0041627. PMID: 22848549.
37. “Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective Kv7.1 (KCNQ1) potassium channel activator”, Mattmann, M. E.; Yu, H.; Lin, Z.; Xu, K.; Huang, X.; Long, S.; Wu, M.; McManus, O. B.; Engers, D. W.; Le, U. M.; Li, M.*; Lindsley, C. W.; Hopkins, C. R.*Bioorg. Med. Chem. Lett.2012, 22, 5936-5941. DOI: 10.1016/j.bmcl.2012.07.060.
36. “Discovery of a Series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as Novel Molecular Switches that Modulate Modes of Kv7.2 (KCNQ2) Channel Pharmacology: Identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a Potent, Brain Penetrant Kv7.2 Channel Inhibitor”, Cheung, Y.-Y.; Yu, H.; Xu, K.; Zou, B.; Wu, M.; McManus, O. B.; Li, M.*; Lindsley, C. W.; Hopkins, C. R.*J. Med. Chem.2012, 55, 6975-6979. DOI: 10.1021/jm300700v. PMID: 22793372.
35. “Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators”, Mueller, R.; Dawson, E. S.; Niswender, C. M.; Butkiewicz, M.; Hopkins, C. R.; Weaver, C. D.; Lindsley, C. W.; Conn, P. J.; Meiler, J.* J. Mol. Model.2012, 18, 4437-4446. DOI: 10.1007/s00894-012-1441-0. PMID: 22592386.
34. “Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor”, Salovich, J. M.; Vinson, P. N.; Sheffler, D. J.; Lamsal, A.; Utley, T. J.; Blobaum, A. L.; Bridges, T. M.; Le, U.; Jones, C. K.; Wood, M. R.; Daniels, J. S.; Conn, P. J.; Niswender, C. M.; Lindsley, C. W.; Hopkins, C. R.*Bioorg. Med. Chem. Lett.2012, 22(15), 5084-5088. DOI: 10.1016/j.bmcl.2012.05.109. PMID: 22738637.
33. “DMH1, a highly selective small molecule BMP inhibitor promotes neurogenesis of hiPSCs: Comparison of PAX6 and SOX1 expression during neural induction”, Neely, M. D.*; Litt, M. J.; Tidball, A. M.; Li, G. G.; Aboud, A. A.; Hopkins, C. R.; Chamberlin, R.; Hong, C. C.; Ess, K. C.; Bowman, A. B. ACS Chem. Neursci.2012, 3, 482-491. DOI: 10.1021/cn300029t. PMID: 22860217.
32. “The mGlu4 positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine A2A antagonist in preclinical rodent models of Parkinson’s disease”, Jones, C. K.; Bubser, M.; Thompson, A. D.; Dickerson, J. W.; Turle-Lorenzo, N.; Amalric, M.; Blobaum, A. L.; Bridges, T. M.; Morrison, R. D.; Jadhav, S.; Engers, D. W.; Italiano, K.; Bode, J.; Daniels, J. S.; Lindsley, C. W.; Hopkins, C. R.; Conn, J. P.; Niswender, C. M.* J. Pharmacol. Exper. Ther.2012, 340, 404-421. DOI: 10.1124/jpet.111.187443. PMID: 22088953.
For a highlight, see: SciBx 2011, 4(46), doi: 10.1038/scibx.2011.1301. This week in therapeutics, Neurology.
Most-Read articles J. Pharmacol. Exper. Ther. for month of November 2011.
31. “Discovery, characterization and structure-activity relationships of an inhibitor of inward rectifying potassium (Kir) channels with preference for Kir2.3, Kir3.X and Kir7.1”, Raphemot, R.*; Lonergan, D. L.; Nguyen, T. T.; Utley, T.; Lewis, L. M.; Kadakia, R.; Weaver, C. D.; Gogliotti, R.; Hopkins, C. R.; Lindsley, C.; Denton, J. S. Frontiers in Pharmacology: Pharmacology of Ion Channels and Channelopathis2011, 2, Article 75. DOI: 10.3389/fphar.2011.00075.
30. “The Discovery and Characterization of ML218: A novel, centrally active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson’s Disease”, Zixiu, X.; Thompson, A. D.; Brogan, J. T.; Schulte, M. L.; Melancon, B. J.; Mi, D.; Lewis, L. M.; Zou, B.; Yang, L.; Morrison, R.; Santomango, T.; Byers, F.; Brewer, K.; Aldrich, J. S.; Yu, H.; Dawson, E. S.; Li, M.; McManus, O.; Jones, C. K.; Daniels, J. S.; Hopkins, C. R.; Xie, X. S.; Conn, P. J.; Weaver, C. D.; Lindsley, C. W.* ACS Chem. Neurosci. 2011, 2, 730-742. DOI: 10.1021/cn200085z. PMID: 22368764.
29. “Discovery, Synthesis, SAR Development of a Series of N-4-(2,5-dioxopyrrolidin-1-yl)-phenylpicolinamides: Characterization of VU0400195 (ML182) as a Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 (mGlu4) with Oral Efficacy in an anti-Parkinsonian Animal Model”, Jones, C. K.; Engers, D. W.; Thompson, A. D.; Field, J. R.; Blobaum, A. L.; Lindsley, S. R.; Zhou, Y.; Gogliotti, R. D.; Jadhav, S.; Zamorano, R.; Bogenpohl, J.; Smith, Y.; Daniels, J. S.; Morrison, R.; Weaver, C. D.; Conn, P. J.; Lindsley, C. W.; Niswender, C. M.*; Hopkins, C. R.*J. Med. Chem. 2011, 54, 7639-7647. DOI: 10.1021/jm200956q. PMID: 21966889.
28. “Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: Unexpected ‘molecular switch’ from a closely related mGlu4 positive allosteric modulator”, Utley, T.; Haddenham, D.; Salovich, J. M.; Zamorano, R.; Vinson, P. N.; Lindsley, C. W.; Hopkins, C. R.*; Niswender, C. M.* Bioorg. Med. Chem. Lett. 2011, 21, 6955-6959. DOI: 10.1016/j.bmcl.2011.09.131. PMID: 22030026.
27. “Identification of ML204 – a novel, potent antagonist that selectively modulates TRPC4 currents”, Miller, M.; Shi, J.; Zhu, Y.; Kustov, M.; Tian, J.-b.; Stevens, A.; Wu, M.; Long, S.; Yang, P.; Zholos, A. V.; Salovich, J. M.; Weaver, C. D.; Hopkins, C.*; Lindsley, C. W.; McManus, O.; Li, M.*; Zhu, M. X. J. Biol. Chem.2011, 286, 33436-33446. DOI: 10.1074/jbc.M111.274167. PMID: 21795696.
26. “Application of Small Organic Molecules Reveals Cooperative TGFb and BMP Regulation of Mesothelial Cell Behaviors”, Cross, E. E.; Thomason, R. T.; Martinez, M.; Hopkins, C. R.; Hong, C. C.; Bader, D.* ACS Chem. Biol.2011, 6, 952-961. DOI: 10.1021/cb200205z. PMID: 21740033.
25. “Discovery, Synthesis, and Structure–Activity Relationship of a Series of N-Aryl-bicyclo[2.2.1]heptane-2-carboxamides: Characterization of ML213 as a Novel KCNQ2 and KCNQ4 Potassium Channel Opener”, Yu, H.; Wu, M.; Townsend, S. D.; Zou, B.; Long, S.; Daniels, J. S.; McManus, O. B.; Li, M.*; Lindsley, C. W.; Hopkins, C. R.*ACS Chem. Neurosci.2011, 572-577. DOI: 10.1021/cn200065b. PMID: 22125664.
24. “Selective inhibition of the Kir2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR and pharmacological characterization of ML133”, Wang, H.-R.; Wu, M.; Yu, H.; Long, S.; Stevens, A.; Engers, D. W.; Sackin, H.; Daniels, J. S.; Dawson, E. S.; Hopkins, C. R.; Lindsley, C. W.*; Li, M.*; McManus, O. B. ACS Chem. Biol. 2011, 6, 845-856. DOI: 10.1021/cb200146a. PMID: 21615117.
23. “Solution-Phase Parallel Synthesis and SAR of Homopiperazinyl Analogs as Positive Allosteric Modulators of mGlu4”, Cheung, Y.-Y.; Zamorano, R.; Blobaum, A. L.; Weaver, C. D.; Conn, P. J.; Lindsley, C. W.; Niswender, C. M.; Hopkins, C. R.*ACS Comb. Sci.2011, 13, 159-165. DOI: 10.1021/co1000508. PMID: 21338051.
22. “Discovery, Synthesis, and Structure–Activity Relationship Development of a Series of N-(4-Acetamido)phenylpicolinamides as Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4 (mGlu4) with CNS Exposure in Rats”, Engers, D. W.; Field, J. R.; Le, U.; Zhou, Y.; Bolinger, J. D.; Zamorano, Z.; Blobaum, A. L.; Jones, C. K.; Jadhav, S.; Weaver, C. D.; Conn, P. J.; Lindsley, C. W.; Niswender, C. M.*; Hopkins, C. R.*J. Med. Chem.2011, 54, 1106-1110. DOI: 10.1021/jm101271s. PMID: 21247167.
21. “Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators”, Bridges, T. M.; Kennedy, J. P.; Hopkins, C. R.; Conn, P. J.; Lindsley, C. W.* Bioorg. Med. Chem. Lett.2010, 20, 5617-5622. DOI:10.1016/j.bmcl.2010.08.042. PMID: 20801651.
20. “Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)”, Engers, D. W.; Gentry, P. R.; Williams, R.; Bolinger, J. D.; Weaver, C. D.; Menon, U. N.; Conn, P. J.; Lindsley, C. W.; Niswender, C. M.*; Hopkins, C. R.*Bioorg. Med. Chem. Lett.2010, 20, 5175-5178. DOI: 10.1016/j.bmcl.2010.07.007. PMID: 20667732.
19. “Synthesis of 1,3-disubstituted indazoles utilizing a Suzuki cross-coupling/deprotection/N-arylation sequence”, Salovich, J. M.; Lindsley, C. W.; Hopkins, C. R.*Tetrahedron Lett.2010, 51, 3796-3799. DOI: 10.1016/j.tetlet.2010.05.060. PMID: 20606711.
18. “Re-exploration of the PHCCC Scaffold: Discovery of Improved Positive Allosteric Modulators of mGluR4”, Williams, R.; Zhou, Y.; Niswender, C. M.; Luo, Q.; Conn, P. J.; Lindsley, C. W.; Hopkins, C. R.*ACS Chemical Neurosci.2010, 1, 411-419. DOI: 10.1021/cn9000318. PMID: 20582156.
2nd Most Cited Article Published in ACS Chemical Neuroscience in Last 3 Years.
17. “In Vivo Structure Activity Relationship Study of Dorsomorphin Analogs Identifies Selective VEGF and BMP Inhibitors”, Hao, J.; Ho, J. N.; Lewis, J. A.; Karim, K. A. Daniels, R. N.; Gentry, P. R.; Hopkins, C. R.; Lindsley, C. W.; Hong, C. C.* ACS Chem. Biol.2010, 5, 245-253. DOI: 10.1021/cb9002865. PMID: 20020776.
For a highlight see: Science & Technology Concentrates, Sophie L. Rovner: “Zebrafish Aid Drug Development.” Chem. & Eng. News2010, 88 (4), 29.
Bowman, T. V. and Zon, L. I.: “Swimming into the Future of Drug Discovery: In Vivo Chemical Screens in Zebrafish.” ACS Chem. Biol.2010, 5, 159-161.
MacMillan, L.: “Zebrafish Swim into Drug Development.” ScienceDaily, 25 Jan. 2010.
Top 20 Most Cited Articles Published in ACS Chemical Biology the Last 3 Years.
16. “Chemical Lead Optimization of a pan Gq mAChR M1, M3, M5 Positive Allosteric Modulator (PAM) Lead. Part I. Development of the first highly selective M5 PAM”, Bridges, T. M.; Kennedy, J. P.; Cho, H. P.; Breininger, M. L.; Gentry, P. R.; Hopkins, C. R.; Conn, J. P.; Lindsley, C. W.* Bioorg. Med. Chem. Lett. 2010, 20, 558-562. DOI: 10.1016/j.bmcl.2009.11.089. PMID: 20004578.
15. “Identification of selective small molecule inhibitors of vascular endothelial growth factor (VEGF) and bone morphogenetic protein (BMP) signaling using zebrafish-based in vivo structure activity relationship studies”, Hao, J.; Ho, J. N.; Daniels, R. N.; Karim, K. A.; Murphy, C. K.; Hopkins, C. R.; Lindsley, C.; Hong, C. C.* Circulation2009, 120, S1090.
14. “Synthesis and SAR of a Novel Positive Allosteric Modulator (PAM) of the Metabotropic Glutamate Receptor 4 (mGluR4)”, Williams, R.; Johnson, K. A.; Gentry, P. R.; Niswender, C. M.; Weaver, C. D.; Conn, P. J.; Lindsley, C. W.; Hopkins, C. R.* Bioorg. Med. Chem. Lett.2009, 19, 4967-4970. DOI: 10.1016/j.bmcl.2009.07.072. PMID: 19640716.
12. “Is 2009 the year that Prasugel (Effient®), Eli Lilly/Daiichi Sankyo’s antiplatelet agent gets approved?”, Hopkins, C. R.* Curr. Top. Med. Chem.2008, 8, 1710-1711.
11. “Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-g binding agents with potential application to the treatment of osteoporosis”, Hopkins, C. R.*; O’Neil, S. V.; Laufersweiler, M. C.; Wang, Y.; Soper, D. L.; Ellis, C. D.; Kontoyianni, M.; Pokross, M.; Petrey, M. E.; Roesgen, J. T.; Obringer, D. M.; Richardson, E. C.; DeMuth, T. P., Jr. Bioorg. Med. Chem. Lett.2006, 16, 5659-5663. DOI: 10.1016/j.bmcl.2006.08.003. PMID: 16919947.
10. “Development of N-4,6-pyrimidine-N-alkyl-N’-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase”, Maier, J. A.; Brugel, T. A.*; Sabat, M.; Golebiowski, A.; Laufersweiler, M. J.; VanRens, J. C.; Hopkins, C. R.; De, B.; Hsieh, L. C.; Brown, K. K.; Easwaran, V.; Janusz, M. J. Bioorg. Med. Chem. Lett.2006, 16, 3646-3650. DOI: 10.1016/j.bmcl.2006.04.072. PMID: 16682201.
9. “Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase”, Hopkins, C. R.*; Czekaj, M.; Kaye, S. S.; Gao, Z.; Pribish, J.; Pauls, H.; Liang, G.; Sides, K.; Cramer, D.; Cairns, J.; Luo, Y.; Lim, H.-K.; Vaz, R.; Rebello, S.; Maignan, S.; Dupuy, A.; Mathieu, M.; Levell, J.* Bioorg. Med. Chem. Lett.2005, 15, 2734-2737. DOI: 10.1016/j.bmcl.2005.04.002. PMID: 15911249.
8. “Synthesis of 6,7-disubstituted-5H-pyrrolo[2,3-b]pyrazines via palladium-catalyzed heteroannulation”, Hopkins, C. R.* and Collar, N. Tetrahedron Lett.2005, 46, 1845-1848. DOI: 10.1016/j.tetlet.2005.01.105.
7. “An improved method for the synthesis of 6-substituted-5H-pyrrolo[2,3-b]pyrazines via palladium-catalyzed heteroannulation using microwave heating”, Hopkins, C. R.* and Collar, N. Tetrahedron Lett.2004, 45, 8631-8633. DOI: 10.1016/j.tetlet.2004.09.152.
6. “Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation”, Hopkins, C. R.*; Neuenschwander, K.; Scotese, A.; Jackson, S.; Nieduzak, T.; Pauls, H.; Liang, G.; Sides, K.; Cramer, D.; Cairns, J.; Maignan, S.; Mathieu, M. Bioorg. Med. Chem. Lett.2004, 14, 4819-4823. DOI: 10.1016/j.bmcl.2004.07.051.
5. “6-Substituted-5H-pyrrolo[2,3-b]pyrazines via palladium-catalyzed heteroannulation from N-(3-chloropyrazin-2-yl)-methanesulfonamide and alkynes”, Hopkins, C. R.* and Collar, N. Tetrahedron Lett.2004, 45, 8087-8090. DOI: 10.1016/j.tetlet.2004.08.155.
4. “Convenient synthesis of 4-amino-3,5-disubstituted pyrazoles in one-step from the corresponding diketo oximes”, Majid, T.; Hopkins, C. R.*; Pedgrift, B.; Collar, N. Tetrahedron Lett.2004, 45, 2137-2139. DOI: 10.1016/j.tetlet.2004.01.045.
3. “Separation of Cdc25 dual specificity phosphatase inhibition and DNA cleaving activities in a focused library of analogs of the antitumor antibiotic Dnacin”, Wipf, P.*; Hopkins, C. R.; Phillips, E. O.; Lazo, J. S. Tetrahedron2002, 58, 6367-6372. DOI: 10.1016/s0040-4020(02)00636-1.
2. “Enantioselective synthesis of the AB-ring system of the antitumor antibiotic tetrazomine”, Wipf, P.* and Hopkins, C. R.J. Org. Chem.2001, 66, 3133-3139. DOI: 10.1021/jo015512q. PMID: 11325279.
1. “Efficient synthesis of 1,4-dihydro-2H-isoquinoline-3,5,8-triones via cyclobutene ring expansion”, Wipf, P.* and Hopkins, C. R.J. Org. Chem.1999, 64, 6881-6887. DOI: 10.1021/jo990089v. PMID: 11674700.
Invited Reviews
9. “Inhibitors of the bone morphogenetic protein (BMP) signaling pathway: a patent review (2008-2015)”, Hopkins, C. R.*Expert Opin. Ther. Patents2016, Accepted for Publication. DOI: 10.1080/13543776.2016.1217330.
8. “Practical strategies and concepts in GPCR allosteric modulator discovery: recent advances with metabotropic glutamate receptors”, Emmitte, K. A.; Hopkins, C. R.; Bridges, T. M.; Gregory, K. J.; Niswender, C. M.; Conn, P. J.*; Lindsley, C. W.* Chem. Rev.2016, 116, 6707-6741. DOI: 10.1021/acs.chemrev.5b00656.
7. “Metabotropic glutamate receptor 4 (mGlu4) positive allosteric modulators for the treatment of Parkinson’s disease: Historical perspective and review of the patent literature”, Lindsley, C. W.; Hopkins, C. R.*Expert Opin. Ther. Patents2012, 461-481. DOI: 10.1517/13543776.2012.679437. PMID: 22506633.
6. “Allosteric Modulation of 7 Transmembrane Spanning Receptors: Theory, Practice and Opportunities for CNS Drug Discovery”, Melancon, B. J.; Hopkins, C. R.; Wood, M. R.; Emmitte, K. A.; Niswender, C. M.; Christopolous, A.; Conn, P. J.; Lindsley, C. W.* J. Med. Chem. (Perspective)2012, 55, 1445-1464. DOI: 10.1021/jm201139r. PMID: 22148748.
Top Ten Most Most Read Article of 2012.
5. “Recent Progress on the Identification of Metabotropic Glutamate 4 Receptor Ligands and Their Potential Utility as CNS Therapeutics”, Robichaud, A. J.*; Engers, D. W.; Lindsley, C. W.; Hopkins, C. R.*ACS Chem. Neurosci.2011, 2, 433-449. DOI: 10.1021/cn200043e. PMID: 22860170.
4. “”Molecular Switches” on mGluR Allosteric Ligands that Modulate Modes of Pharmacology”, Wood, M. R.; Hopkins, C. R.; Brogan, J. T.; Conn, P. J.; Lindsley, C. W.* Biochemistry2010, 50, 2403-2410. DOI: 10.1021/bi200129s. PMID: 21341760.
3. “The antipsychotic potential of muscarinic allosteric modulation”, Bridges, T. M.; LeBois, E. P.; Hopkins, C. R.; Wood, M. R.; Jones, C. K.; Conn, J. P.; Lindsley, C. W.* Drug News Perspect.2010, 23, 229-240. DOI: 10.1358/dnp.2010.23.4.1416977. PMID: 20520852.
2. “Recent Progress in the Development of mGluR4 Positive Allosteric Modulators for the Treatment of Parkinson’s Disease”, Lindsley, C. W.; Engers, D. W.; Niswender, C. M.; Hopkins, C. R.* Curr. Top. Med. Chem.2009, 9, 949-963. PMID: 19754407.
1. “mGluR4-positive allosteric modulation as potential treatment for Parkinson’s disease”, Hopkins, C. R.*; Lindsley, C. W.; Niswender, C. M. Future Med. Chem.2009, 1, 501-513. DOI: 10.4155/fmc.09.38. PMID: 20161443.
Book Chapters
2. Melancon, B. J.; Hopkins, C. R.* ‘Muscarinic receptors allosteric modulation’ in Allosterism in Drug Discovery, Doller, D. Ed. Royal Society of Chemistry, 2016. (Invited)
1. Lindsley, C. W.; Hopkins, C. R.; Sulikowski, G. A. ‘Biomimetic Synthesis of Lignans’ in Biomimetic Organic Synthesis, Poupon, E.; Nay, B., Eds. Wiley-VCH Verlag GmbH & Co. KGaA, 2011, pp 677-693. (Invited)