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89 results

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Page 1
Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.
Yingling JM, McMillen WT, Yan L, Huang H, Sawyer JS, Graff J, Clawson DK, Britt KS, Anderson BD, Beight DW, Desaiah D, Lahn MM, Benhadji KA, Lallena MJ, Holmgaard RB, Xu X, Zhang F, Manro JR, Iversen PW, Iyer CV, Brekken RA, Kalos MD, Driscoll KE. Yingling JM, et al. Among authors: clawson dk. Oncotarget. 2017 Dec 31;9(6):6659-6677. doi: 10.18632/oncotarget.23795. eCollection 2018 Jan 23. Oncotarget. 2017. PMID: 29467918 Free PMC article.
Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
Li HY, Wang Y, Heap CR, King CH, Mundla SR, Voss M, Clawson DK, Yan L, Campbell RM, Anderson BD, Wagner JR, Britt K, Lu KX, McMillen WT, Yingling JM. Li HY, et al. Among authors: clawson dk. J Med Chem. 2006 Mar 23;49(6):2138-42. doi: 10.1021/jm058209g. J Med Chem. 2006. PMID: 16539403
Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.
Li HY, McMillen WT, Heap CR, McCann DJ, Yan L, Campbell RM, Mundla SR, King CH, Dierks EA, Anderson BD, Britt KS, Huss KL, Voss MD, Wang Y, Clawson DK, Yingling JM, Sawyer JS. Li HY, et al. Among authors: clawson dk. J Med Chem. 2008 Apr 10;51(7):2302-6. doi: 10.1021/jm701199p. Epub 2008 Mar 4. J Med Chem. 2008. PMID: 18314943
Discovery of LY2457546: a multi-targeted anti-angiogenic kinase inhibitor with a novel spectrum of activity and exquisite potency in the acute myelogenous leukemia-Flt-3-internal tandem duplication mutant human tumor xenograft model.
Burkholder TP, Clayton JR, Rempala ME, Henry JR, Knobeloch JM, Mendel D, McLean JA, Hao Y, Barda DA, Considine EL, Uhlik MT, Chen Y, Ma L, Bloem LJ, Akunda JK, McCann DJ, Sanchez-Felix M, Clawson DK, Lahn MM, Starling JJ. Burkholder TP, et al. Among authors: clawson dk. Invest New Drugs. 2012 Jun;30(3):936-49. doi: 10.1007/s10637-011-9640-6. Epub 2011 Mar 1. Invest New Drugs. 2012. PMID: 21360050
Crystal structure of human parathyroid hormone 1-34 at 0.9-A resolution.
Jin L, Briggs SL, Chandrasekhar S, Chirgadze NY, Clawson DK, Schevitz RW, Smiley DL, Tashjian AH, Zhang F. Jin L, et al. Among authors: clawson dk. J Biol Chem. 2000 Sep 1;275(35):27238-44. doi: 10.1074/jbc.M001134200. J Biol Chem. 2000. PMID: 10837469 Free article.
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.
Henry JR, Kaufman MD, Peng SB, Ahn YM, Caldwell TM, Vogeti L, Telikepalli H, Lu WP, Hood MM, Rutkoski TJ, Smith BD, Vogeti S, Miller D, Wise SC, Chun L, Zhang X, Zhang Y, Kays L, Hipskind PA, Wrobleski AD, Lobb KL, Clay JM, Cohen JD, Walgren JL, McCann D, Patel P, Clawson DK, Guo S, Manglicmot D, Groshong C, Logan C, Starling JJ, Flynn DL. Henry JR, et al. Among authors: clawson dk. J Med Chem. 2015 May 28;58(10):4165-79. doi: 10.1021/acs.jmedchem.5b00067. Epub 2015 May 12. J Med Chem. 2015. PMID: 25965804
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.
Carson MW, Luz JG, Suen C, Montrose C, Zink R, Ruan X, Cheng C, Cole H, Adrian MD, Kohlman DT, Mabry T, Snyder N, Condon B, Maletic M, Clawson D, Pustilnik A, Coghlan MJ. Carson MW, et al. J Med Chem. 2014 Feb 13;57(3):849-60. doi: 10.1021/jm401616g. Epub 2014 Feb 4. J Med Chem. 2014. PMID: 24446728
Crystal structure of the obese protein leptin-E100.
Zhang F, Basinski MB, Beals JM, Briggs SL, Churgay LM, Clawson DK, DiMarchi RD, Furman TC, Hale JE, Hsiung HM, Schoner BE, Smith DP, Zhang XY, Wery JP, Schevitz RW. Zhang F, et al. Among authors: clawson dk. Nature. 1997 May 8;387(6629):206-9. doi: 10.1038/387206a0. Nature. 1997. PMID: 9144295
Defining Target Engagement Required for Efficacy In Vivo at the Retinoic Acid Receptor-Related Orphan Receptor C2 (RORγt).
Lugar CW, Clarke CA, Morphy R, Rudyk H, Sapmaz S, Stites RE, Vaught GM, Furness K, Broughton HB, Durst GL, Clawson DK, Stout SL, Guo SY, Durbin JD, Stayrook KR, Edmondson DD, Kikly K, New NE, Bina HA, Chambers MG, Shetler P, Chang WY, Chang VC, Barr R, Gough WH, Steele JP, Getman B, Patel N, Mathes BM, Richardson TI. Lugar CW, et al. Among authors: clawson dk. J Med Chem. 2021 May 13;64(9):5470-5484. doi: 10.1021/acs.jmedchem.0c01918. Epub 2021 Apr 14. J Med Chem. 2021. PMID: 33852312
89 results