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Page 1
Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.
Horne DB, Biswas K, Brown J, Bartberger MD, Clarine J, Davis CD, Gore VK, Harried S, Horner M, Kaller MR, Lehto SG, Liu Q, Ma VV, Monenschein H, Nguyen TT, Yuan CC, Youngblood BD, Zhang M, Zhong W, Allen JR, Chen JJ, Gavva NR. Horne DB, et al. Among authors: clarine j. J Med Chem. 2018 Sep 27;61(18):8186-8201. doi: 10.1021/acs.jmedchem.8b00518. Epub 2018 Sep 10. J Med Chem. 2018. PMID: 30148953
Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.
Horne DB, Tamayo NA, Bartberger MD, Bo Y, Clarine J, Davis CD, Gore VK, Kaller MR, Lehto SG, Ma VV, Nishimura N, Nguyen TT, Tang P, Wang W, Youngblood BD, Zhang M, Gavva NR, Monenschein H, Norman MH. Horne DB, et al. Among authors: clarine j. J Med Chem. 2014 Apr 10;57(7):2989-3004. doi: 10.1021/jm401955h. Epub 2014 Mar 19. J Med Chem. 2014. PMID: 24597733
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
Rzasa RM, Frohn MJ, Andrews KL, Chmait S, Chen N, Clarine JG, Davis C, Eastwood HA, Horne DB, Hu E, Jones AD, Kaller MR, Kunz RK, Miller S, Monenschein H, Nguyen T, Pickrell AJ, Porter A, Reichelt A, Zhao X, Treanor JJS, Allen JR. Rzasa RM, et al. Among authors: clarine jg. Bioorg Med Chem. 2014 Dec 1;22(23):6570-6585. doi: 10.1016/j.bmc.2014.10.013. Bioorg Med Chem. 2014. PMID: 25456383
The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core.
Harrington PE, St Jean DJ Jr, Clarine J, Coulter TS, Croghan M, Davenport A, Davis J, Ghiron C, Hutchinson J, Kelly MG, Lott F, Lu JY, Martin D, Morony S, Poon SF, Portero-Larragueta E, Reagan JD, Regal KA, Tasker A, Wang M, Yang Y, Yao G, Zeng Q, Henley C 3rd, Fotsch C. Harrington PE, et al. Among authors: clarine j. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5544-7. doi: 10.1016/j.bmcl.2010.07.060. Epub 2010 Aug 12. Bioorg Med Chem Lett. 2010. PMID: 20708930
Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition.
Reich SH, Sprengeler PA, Chiang GG, Appleman JR, Chen J, Clarine J, Eam B, Ernst JT, Han Q, Goel VK, Han EZR, Huang V, Hung INJ, Jemison A, Jessen KA, Molter J, Murphy D, Neal M, Parker GS, Shaghafi M, Sperry S, Staunton J, Stumpf CR, Thompson PA, Tran C, Webber SE, Wegerski CJ, Zheng H, Webster KR. Reich SH, et al. Among authors: clarine j. J Med Chem. 2018 Apr 26;61(8):3516-3540. doi: 10.1021/acs.jmedchem.7b01795. Epub 2018 Mar 29. J Med Chem. 2018. PMID: 29526098
Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers.
Smith CR, Aranda R, Bobinski TP, Briere DM, Burns AC, Christensen JG, Clarine J, Engstrom LD, Gunn RJ, Ivetac A, Jean-Baptiste R, Ketcham JM, Kobayashi M, Kuehler J, Kulyk S, Lawson JD, Moya K, Olson P, Rahbaek L, Thomas NC, Wang X, Waters LM, Marx MA. Smith CR, et al. Among authors: clarine j. J Med Chem. 2022 Feb 10;65(3):1749-1766. doi: 10.1021/acs.jmedchem.1c01900. Epub 2022 Jan 18. J Med Chem. 2022. PMID: 35041419 Free article.
Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase.
Ernst JT, Thompson PA, Nilewski C, Sprengeler PA, Sperry S, Packard G, Michels T, Xiang A, Tran C, Wegerski CJ, Eam B, Young NP, Fish S, Chen J, Howard H, Staunton J, Molter J, Clarine J, Nevarez A, Chiang GG, Appleman JR, Webster KR, Reich SH. Ernst JT, et al. Among authors: clarine j. J Med Chem. 2020 Jun 11;63(11):5879-5955. doi: 10.1021/acs.jmedchem.0c00182. Epub 2020 May 29. J Med Chem. 2020. PMID: 32470302
1-Aminomethyl SAR in a novel series of flavagline-inspired eIF4A inhibitors: Effects of amine substitution on cell potency and in vitro PK properties.
Nilewski C, Michels TD, Packard GK, Xiang AX, Sprengeler PA, Eam B, Fish S, Thompson PA, Wegerski CJ, Nevarez A, Clarine J, Sperry S, Ernst JT, Reich SH. Nilewski C, et al. Among authors: clarine j. Bioorg Med Chem Lett. 2021 Sep 1;47:128111. doi: 10.1016/j.bmcl.2021.128111. Epub 2021 Aug 2. Bioorg Med Chem Lett. 2021. PMID: 34353608
Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A.
Thompson PA, Eam B, Young NP, Fish S, Chen J, Barrera M, Howard H, Sung E, Parra A, Staunton J, Chiang GG, Gerson-Gurwitz A, Wegerski CJ, Nevarez A, Clarine J, Sperry S, Xiang A, Nilewski C, Packard GK, Michels T, Tran C, Sprengeler PA, Ernst JT, Reich SH, Webster KR. Thompson PA, et al. Among authors: clarine j. Mol Cancer Ther. 2021 Jan;20(1):26-36. doi: 10.1158/1535-7163.MCT-19-0973. Epub 2020 Oct 9. Mol Cancer Ther. 2021. PMID: 33037136
The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading.
Sudhakar N, Yan L, Qiryaqos F, Engstrom LD, Laguer J, Calinisan A, Hebbert A, Waters L, Moya K, Bowcut V, Vegar L, Ketcham JM, Ivetac A, Smith CR, Lawson JD, Rahbaek L, Clarine J, Nguyen N, Saechao B, Parker C, Elliott AJ, Vanderpool D, He L, Hover LD, Fernandez-Banet J, Coma S, Pachter JA, Hallin J, Marx MA, Briere DM, Christensen JG, Olson P, Haling J, Khare S. Sudhakar N, et al. Among authors: clarine j. Mol Cancer Ther. 2024 Apr 19. doi: 10.1158/1535-7163.MCT-23-0870. Online ahead of print. Mol Cancer Ther. 2024. PMID: 38641404
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