Skip to main page content
Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation

Search Page

My NCBI Filters
Text availability
Article attribute
Article type
Publication date

Search Results

440 results
Filters applied: . Clear all Results are displayed in a computed author sort order. Results by year timeline is unavailable
Page 1
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
Efficacy was achieved with a wide range of doses with no signs of toxicity, and correlated with a reduction in the levels of activated mitogen-activated protein kinase in excised tumors. These data indicate that MEK inhibitors represent a promising, noncytoto …
Efficacy was achieved with a wide range of doses with no signs of toxicity, and correlated with a reduction in the levels of a …
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
This paper reports a second generation MEK inhibitor. The previously reported potent and efficacious MEK inhibitor, PD-184352 (CI-1040), contains an integral hydroxamate moiety. ...An oxadiazole moiety behaves as a bioisostere for the hydroxamate group, leading to …
This paper reports a second generation MEK inhibitor. The previously reported potent and efficacious MEK inhibitor, PD-184352 (CI-104 …
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. 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
Signaling through the erbB receptor family of tyrosine kinases contributes to the proliferation, differentiation, migration, and survival of a variety of cell types. ...PF-00299804 is a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor curre …
Signaling through the erbB receptor family of tyrosine kinases contributes to the proliferation, differentiation, migration, and survival of …
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
A novel series of benzhydroxamate esters derived from their precursor anthranilic acids have been prepared and have been identified as potent MEK inhibitors. 2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-benzamide, CI-1040, was the first MEK inhibitor t
A novel series of benzhydroxamate esters derived from their precursor anthranilic acids have been prepared and have been identified a
Therapeutic challenges of kinase and phosphatase inhibition and use in anti-diabetic strategy.
Bridges AJ. Bridges AJ. Biochem Soc Trans. 2005 Apr;33(Pt 2):343-5. doi: 10.1042/BST0330343. Biochem Soc Trans. 2005. PMID: 15787602 Review.
Because of this, we know a great deal about which processes signalling inhibitors interfere with, but little about the overall consequences. ...
Because of this, we know a great deal about which processes signalling inhibitors interfere with, but little about the overall conseq …
Chemical inhibitors of protein kinases.
Bridges AJ. Bridges AJ. Chem Rev. 2001 Aug;101(8):2541-72. doi: 10.1021/cr000250y. Chem Rev. 2001. PMID: 11749388 Review. No abstract available.
Anticancer efficacy of the irreversible EGFr tyrosine kinase inhibitor PD 0169414 against human tumor xenografts.
Vincent PW, Bridges AJ, Dykes DJ, Fry DW, Leopold WR, Patmore SJ, Roberts BJ, Rose S, Sherwood V, Zhou H, Elliott WL. Vincent PW, et al. Cancer Chemother Pharmacol. 2000;45(3):231-8. doi: 10.1007/s002800050034. Cancer Chemother Pharmacol. 2000. PMID: 10663641
PURPOSE: The involvement of the EGF receptor (EGFr) family of receptors in cancers suggests that a selective inhibitor of the tyrosine kinase activity of the EGFr family could have a therapeutic effect. ...CONCLUSION: PD 0169414 is a specific, irreversible in …
PURPOSE: The involvement of the EGF receptor (EGFr) family of receptors in cancers suggests that a selective inhibitor of the tyrosin …
Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor.
Fry DW, Bridges AJ, Denny WA, Doherty A, Greis KD, Hicks JL, Hook KE, Keller PR, Leopold WR, Loo JA, McNamara DJ, Nelson JM, Sherwood V, Smaill JB, Trumpp-Kallmeyer S, Dobrusin EM. Fry DW, et al. Proc Natl Acad Sci U S A. 1998 Sep 29;95(20):12022-7. doi: 10.1073/pnas.95.20.12022. Proc Natl Acad Sci U S A. 1998. PMID: 9751783 Free PMC article.
A class of high-affinity inhibitors is disclosed that selectively target and irreversibly inactivate the epidermal growth factor receptor tyrosine kinase through specific, covalent modification of a cysteine residue present in the ATP binding pocket. A series
A class of high-affinity inhibitors is disclosed that selectively target and irreversibly inactivate the epidermal growth factor rece
Biochemical and antiproliferative properties of 4-[ar(alk)ylamino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor.
Fry DW, Nelson JM, Slintak V, Keller PR, Rewcastle GW, Denny WA, Zhou H, Bridges AJ. Fry DW, et al. Biochem Pharmacol. 1997 Oct 15;54(8):877-87. doi: 10.1016/s0006-2952(97)00242-6. Biochem Pharmacol. 1997. PMID: 9354588
Inhibitors of protein tyrosine kinases.
Fry DW, Bridges AJ. Fry DW, et al. Curr Opin Biotechnol. 1995 Dec;6(6):662-7. doi: 10.1016/0958-1669(95)80109-x. Curr Opin Biotechnol. 1995. PMID: 8527837 Review.
The description in the past year of several novel protein tyrosine kinase inhibitors, which exhibit dramatic improvements in potency and specificity over earlier agents, will be considered a major turning point in the field. ...
The description in the past year of several novel protein tyrosine kinase inhibitors, which exhibit dramatic improvements in potency and spe …
440 results
Jump to page
Feedback