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Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo.
Sebolt-Leopold JS, Dudley DT, Herrera R, Van Becelaere K, Wiland A, Gowan RC, Tecle H, Barrett SD, Bridges A, Przybranowski S, Leopold WR, Saltiel AR. Sebolt-Leopold JS, et al. Nat Med. 1999 Jul;5(7):810-6. doi: 10.1038/10533. Nat Med. 1999. PMID: 10395327
Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition.
Ohren JF, Chen H, Pavlovsky A, Whitehead C, Zhang E, Kuffa P, Yan C, McConnell P, Spessard C, Banotai C, Mueller WT, Delaney A, Omer C, Sebolt-Leopold J, Dudley DT, Leung IK, Flamme C, Warmus J, Kaufman M, Barrett S, Tecle H, Hasemann CA. Ohren JF, et al. Nat Struct Mol Biol. 2004 Dec;11(12):1192-7. doi: 10.1038/nsmb859. Epub 2004 Nov 14. Nat Struct Mol Biol. 2004. PMID: 15543157
2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase).
Warmus JS, Flamme C, Zhang LY, Barrett S, Bridges A, Chen H, Gowan R, Kaufman M, Sebolt-Leopold J, Leopold W, Merriman R, Ohren J, Pavlovsky A, Przybranowski S, Tecle H, Valik H, Whitehead C, Zhang E. Warmus JS, et al. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6171-4. doi: 10.1016/j.bmcl.2008.10.015. Epub 2008 Oct 7. Bioorg Med Chem Lett. 2008. PMID: 18951019
The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
Barrett SD, Bridges AJ, Dudley DT, Saltiel AR, Fergus JH, Flamme CM, Delaney AM, Kaufman M, LePage S, Leopold WR, Przybranowski SA, Sebolt-Leopold J, Van Becelaere K, Doherty AM, Kennedy RM, Marston D, Howard WA Jr, Smith Y, Warmus JS, Tecle H. Barrett SD, et al. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4. doi: 10.1016/j.bmcl.2008.10.054. Epub 2008 Oct 15. Bioorg Med Chem Lett. 2008. PMID: 18952427
Central role of the MEK/ERK MAP kinase pathway in a mouse model of rheumatoid arthritis: potential proinflammatory mechanisms.
Thiel MJ, Schaefer CJ, Lesch ME, Mobley JL, Dudley DT, Tecle H, Barrett SD, Schrier DJ, Flory CM. Thiel MJ, et al. Arthritis Rheum. 2007 Oct;56(10):3347-57. doi: 10.1002/art.22869. Arthritis Rheum. 2007. PMID: 17907188
In vitro and in vivo evaluation of the subtype-selective muscarinic agonist PD 151832.
Jaen J, Barrett S, Brann M, Callahan M, Davis R, Doyle P, Eubanks D, Lauffer D, Lauffer L, Lipinski W, et al. Jaen J, et al. Life Sci. 1995;56(11-12):845-52. doi: 10.1016/0024-3205(95)00019-3. Life Sci. 1995. PMID: 10188784
Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.
Tecle H, Barrett SD, Lauffer DJ, Augelli-Szafran C, Brann MR, Callahan MJ, Caprathe BW, Davis RE, Doyle PD, Eubanks D, Lipiniski W, Mirzadegan T, Moos WH, Moreland DW, Nelson CB, Pavia MR, Raby C, Schwarz RD, Spencer CJ, Thomas AJ, Jaen JC. Tecle H, et al. J Med Chem. 1998 Jul 2;41(14):2524-36. doi: 10.1021/jm960683m. J Med Chem. 1998. PMID: 9651157
CI-1017, a functionally M1-selective muscarinic agonist: design, synthesis, and preclinical pharmacology.
Tecle H, Schwarz RD, Barrett SD, Callahan MJ, Caprathe BW, Davis RE, Doyle P, Emmerling M, Lauffer DJ, Mirzadegan T, Moreland DW, Lipiniski W, Nelson C, Raby C, Spencer C, Spiegel K, Thomas AJ, Jaen JC. Tecle H, et al. Pharm Acta Helv. 2000 Mar;74(2-3):141-8. doi: 10.1016/s0031-6865(99)00027-8. Pharm Acta Helv. 2000. PMID: 10812951
Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring.
Boys ML, Bian F, Kramer JB, Chio CL, Ren XD, Chen H, Barrett SD, Sexton KE, Iula DM, Filzen GF, Nguyen MN, Angell P, Downs VL, Wang Z, Raheja N, Ellsworth EL, Fakhoury S, Bratton LD, Keller PR, Gowan R, Drummond EM, Maiti SN, Hena MA, Lu L, McConnell P, Knafels JD, Thanabal V, Sun F, Alessi D, McCarthy A, Zhang E, Finzel BC, Patel S, Ciotti SM, Eisma R, Payne NA, Gilbertsen RB, Kostlan CR, Pocalyko DJ, Lala DS. Boys ML, et al. Bioorg Med Chem Lett. 2012 May 15;22(10):3392-7. doi: 10.1016/j.bmcl.2012.04.013. Epub 2012 Apr 10. Bioorg Med Chem Lett. 2012. PMID: 22542194
Pantolactams as androgen receptor antagonists for the topical suppression of sebum production.
Sexton KE, Barrett S, Bridgwood K, Carroll M, Dettling D, Du D, Fakhoury S, Fedij V, Hu LY, Kostlan C, Pocalyko D, Raheja N, Smith Y, Shanmugasundaram V, Wade K. Sexton KE, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5230-3. doi: 10.1016/j.bmcl.2011.07.048. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21831636
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