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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
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. Among authors: tecle h. Arthritis Rheum. 2007 Oct;56(10):3347-57. doi: 10.1002/art.22869. Arthritis Rheum. 2007. PMID: 17907188 Free article.
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. Among authors: tecle h. 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
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
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. Among authors: tecle h. 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
Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor.
Gonzales AJ, Hook KE, Althaus IW, Ellis PA, Trachet E, Delaney AM, Harvey PJ, Ellis TA, Amato DM, Nelson JM, Fry DW, Zhu T, Loi CM, Fakhoury SA, Schlosser KM, Sexton KE, Winters RT, Reed JE, Bridges AJ, Lettiere DJ, Baker DA, Yang J, Lee HT, Tecle H, Vincent PW. Gonzales AJ, et al. Among authors: tecle h. Mol Cancer Ther. 2008 Jul;7(7):1880-9. doi: 10.1158/1535-7163.MCT-07-2232. Epub 2008 Jul 7. Mol Cancer Ther. 2008. PMID: 18606718 Free article.
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
4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase.
Spicer JA, Rewcastle GW, Kaufman MD, Black SL, Plummer MS, Denny WA, Quin J 3rd, Shahripour AB, Barrett SD, Whitehead CE, Milbank JB, Ohren JF, Gowan RC, Omer C, Camp HS, Esmaeil N, Moore K, Sebolt-Leopold JS, Pryzbranowski S, Merriman RL, Ortwine DF, Warmus JS, Flamme CM, Pavlovsky AG, Tecle H. Spicer JA, et al. Among authors: tecle h. J Med Chem. 2007 Oct 18;50(21):5090-102. doi: 10.1021/jm0704548. Epub 2007 Sep 19. J Med Chem. 2007. PMID: 17880056
4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties.
Jaen JC, Wise LD, Caprathe BW, Tecle H, Bergmeier S, Humblet CC, Heffner TG, Meltzer LT, Pugsley TA. Jaen JC, et al. J Med Chem. 1990 Jan;33(1):311-7. doi: 10.1021/jm00163a051. J Med Chem. 1990. PMID: 1967314
Examination of a series of 8-[3-[bis(4-fluorophenyl)amino]propyl]-1-aryl-1,3,8- triazaspiro[4.5]decan-4-ones as potential antipsychotic agents.
Wise LD, Pattison IC, Butler DE, DeWald HA, Lewis EP, Lobbestael SJ, Tecle H, Coughenour LL, Downs DA, Poschel BP. Wise LD, et al. J Med Chem. 1985 Dec;28(12):1811-7. doi: 10.1021/jm00150a011. J Med Chem. 1985. PMID: 2866248
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