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Items: 1 to 50 of 104

1.

MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.

Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H, Jewell JP, Kariv I, Katz JD, Kunii K, Lu W, Lutterbach BA, Paweletz CP, Qu X, Reilly JF, Szewczak AA, Zeng Q, Kohl NE, Dinsmore CJ.

Cancer Res. 2010 Feb 15;70(4):1524-33. doi: 10.1158/0008-5472.CAN-09-2541. Epub 2010 Feb 9.

2.

Proceedings from the 2009 genetic syndromes of the Ras/MAPK pathway: From bedside to bench and back.

Rauen KA, Schoyer L, McCormick F, Lin AE, Allanson JE, Stevenson DA, Gripp KW, Neri G, Carey JC, Legius E, Tartaglia M, Schubbert S, Roberts AE, Gelb BD, Shannon K, Gutmann DH, McMahon M, Guerra C, Fagin JA, Yu B, Aoki Y, Neel BG, Balmain A, Drake RR, Nolan GP, Zenker M, Bollag G, Sebolt-Leopold J, Gibbs JB, Silva AJ, Patton EE, Viskochil DH, Kieran MW, Korf BR, Hagerman RJ, Packer RJ, Melese T.

Am J Med Genet A. 2010 Jan;152A(1):4-24. doi: 10.1002/ajmg.a.33183.

3.

Lung cancer cell lines harboring MET gene amplification are dependent on Met for growth and survival.

Lutterbach B, Zeng Q, Davis LJ, Hatch H, Hang G, Kohl NE, Gibbs JB, Pan BS.

Cancer Res. 2007 Mar 1;67(5):2081-8. Erratum in: Cancer Res. 2007 Apr 15;67(8):3987.

4.

Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.

Sisko JT, Tucker TJ, Bilodeau MT, Buser CA, Ciecko PA, Coll KE, Fernandes C, Gibbs JB, Koester TJ, Kohl N, Lynch JJ, Mao X, McLoughlin D, Miller-Stein CM, Rodman LD, Rickert KW, Sepp-Lorenzino L, Shipman JM, Thomas KA, Wong BK, Hartman GD.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1146-50. Epub 2005 Dec 20.

PMID:
16368234
5.

Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.

Bilodeau MT, Balitza AE, Koester TJ, Manley PJ, Rodman LD, Buser-Doepner C, Coll KE, Fernandes C, Gibbs JB, Heimbrook DC, Huckle WR, Kohl N, Lynch JJ, Mao X, McFall RC, McLoughlin D, Miller-Stein CM, Rickert KW, Sepp-Lorenzino L, Shipman JM, Subramanian R, Thomas KA, Wong BK, Yu S, Hartman GD.

J Med Chem. 2004 Dec 2;47(25):6363-72.

PMID:
15566305
6.

Farnesyl:protein transferase inhibitors as potential agents for the management of human prostate cancer.

Sepp-Lorenzino L, Tjaden G, Moasser MM, Timaul N, Ma Z, Kohl NE, Gibbs JB, Oliff A, Rosen N, Scher HI.

Prostate Cancer Prostatic Dis. 2001;4(1):33-43.

7.

Medical laser safety hazard evaluation.

Edwards BE, Barnes LK, Gibbs JB, Nguyen GB.

Health Phys. 2002 Aug;83(8 Suppl):S36-44.

PMID:
12132727
8.

The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.

Tucker TJ, Abrams MT, Buser CA, Davide JP, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hartman GD, Huber HE, Liu D, Lobell RB, Lumma WC, Robinson RG, Sisko JT, Smith AM.

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2027-30.

PMID:
12113834
9.

3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.

Bell IM, Gallicchio SN, Abrams M, Beese LS, Beshore DC, Bhimnathwala H, Bogusky MJ, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hamilton KA, Hartman GD, Heimbrook DC, Homnick CF, Huber HE, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Robinson R, Rodrigues AD, Taylor JS, Walsh ES, Williams TM, Zartman CB.

J Med Chem. 2002 Jun 6;45(12):2388-409.

PMID:
12036349
10.

Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.

Bell IM, Gallicchio SN, Abrams M, Beshore DC, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hartman GD, Heimbrook DC, Homnick CF, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Miller PA, Omer CA, Rodrigues AD, Walsh ES, Williams TM.

J Med Chem. 2001 Aug 30;44(18):2933-49.

PMID:
11520202
11.

Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.

Dinsmore CJ, Bergman JM, Wei DD, Zartman CB, Davide JP, Greenberg IB, Liu D, O'Neill TJ, Gibbs JB, Koblan KS, Kohl NE, Lobell RB, Chen IW, McLoughlin DA, Olah TV, Graham SL, Hartman GD, Williams TM.

Bioorg Med Chem Lett. 2001 Feb 26;11(4):537-40.

PMID:
11229765
12.

Farnesyltransferase inhibitors potentiate the antitumor effect of radiation on a human tumor xenograft expressing activated HRAS.

Cohen-Jonathan E, Muschel RJ, Gillies McKenna W, Evans SM, Cerniglia G, Mick R, Kusewitt D, Sebti SM, Hamilton AD, Oliff A, Kohl N, Gibbs JB, Bernhard EJ.

Radiat Res. 2000 Aug;154(2):125-32.

PMID:
10931682
13.

Mouse mammary tumor virus-Ki-rasB transgenic mice develop mammary carcinomas that can be growth-inhibited by a farnesyl:protein transferase inhibitor.

Omer CA, Chen Z, Diehl RE, Conner MW, Chen HY, Trumbauer ME, Gopal-Truter S, Seeburger G, Bhimnathwala H, Abrams MT, Davide JP, Ellis MS, Gibbs JB, Greenberg I, Koblan KS, Kral AM, Liu D, Lobell RB, Miller PJ, Mosser SD, O'Neill TJ, Rands E, Schaber MD, Senderak ET, Oliff A, Kohl NE.

Cancer Res. 2000 May 15;60(10):2680-8.

14.

Mechanism-based target identification and drug discovery in cancer research.

Gibbs JB.

Science. 2000 Mar 17;287(5460):1969-73. Review.

PMID:
10720316
15.

Anticancer drug targets: growth factors and growth factor signaling.

Gibbs JB.

J Clin Invest. 2000 Jan;105(1):9-13. Review. No abstract available.

16.

Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.

Dinsmore CJ, Williams TM, O'Neill TJ, Liu D, Rands E, Culberson JC, Lobell RB, Koblan KS, Kohl NE, Gibbs JB, Oliff AI, Graham SL, Hartman GD.

Bioorg Med Chem Lett. 1999 Dec 6;9(23):3301-6.

PMID:
10612589
17.

In vitro and in vivo effects of a farnesyltransferase inhibitor on Nf1-deficient hematopoietic cells.

Mahgoub N, Taylor BR, Gratiot M, Kohl NE, Gibbs JB, Jacks T, Shannon KM.

Blood. 1999 Oct 1;94(7):2469-76.

18.

Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.

Anthony NJ, Gomez RP, Schaber MD, Mosser SD, Hamilton KA, O'Neil TJ, Koblan KS, Graham SL, Hartman GD, Shah D, Rands E, Kohl NE, Gibbs JB, Oliff AI.

J Med Chem. 1999 Aug 26;42(17):3356-68.

PMID:
10464022
19.

Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.

Ciccarone TM, MacTough SC, Williams TM, Dinsmore CJ, O'Neill TJ, Shah D, Culberson JC, Koblan KS, Kohl NE, Gibbs JB, Oliff AI, Graham SL, Hartman GD.

Bioorg Med Chem Lett. 1999 Jul 19;9(14):1991-6.

PMID:
10450968
20.

Clavaric acid and steroidal analogues as Ras- and FPP-directed inhibitors of human farnesyl-protein transferase.

Lingham RB, Silverman KC, Jayasuriya H, Kim BM, Amo SE, Wilson FR, Rew DJ, Schaber MD, Bergstrom JD, Koblan KS, Graham SL, Kohl NE, Gibbs JB, Singh SB.

J Med Chem. 1998 Nov 5;41(23):4492-501.

PMID:
9804689
21.

Biochemical and biological analyses of farnesyl-protein transferase inhibitors.

Kohl NE, Koblan KS, Omer CA, Oliff A, Gibbs JB.

Methods Mol Biol. 1998;84:283-91.

PMID:
9666457
22.

N-Arylalkyl pseudopeptide inhibitors of farnesyltransferase.

deSolms SJ, Giuliani EA, Graham SL, Koblan KS, Kohl NE, Mosser SD, Oliff AI, Pompliano DL, Rands E, Scholz TH, Wiscount CM, Gibbs JB, Smith RL.

J Med Chem. 1998 Jul 2;41(14):2651-6.

PMID:
9651171
23.

Antitumor effect of a farnesyl protein transferase inhibitor in mammary and lymphoid tumors overexpressing N-ras in transgenic mice.

Mangues R, Corral T, Kohl NE, Symmans WF, Lu S, Malumbres M, Gibbs JB, Oliff A, Pellicer A.

Cancer Res. 1998 Mar 15;58(6):1253-9.

24.

A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis.

Barrington RE, Subler MA, Rands E, Omer CA, Miller PJ, Hundley JE, Koester SK, Troyer DA, Bearss DJ, Conner MW, Gibbs JB, Hamilton K, Koblan KS, Mosser SD, O'Neill TJ, Schaber MD, Senderak ET, Windle JJ, Oliff A, Kohl NE.

Mol Cell Biol. 1998 Jan;18(1):85-92.

25.

Farnesyltransferase inhibitors versus Ras inhibitors.

Gibbs JB, Graham SL, Hartman GD, Koblan KS, Kohl NE, Omer CA, Oliff A.

Curr Opin Chem Biol. 1997 Aug;1(2):197-203. Review.

PMID:
9667853
26.

Kinase-deficient Pak1 mutants inhibit Ras transformation of Rat-1 fibroblasts.

Tang Y, Chen Z, Ambrose D, Liu J, Gibbs JB, Chernoff J, Field J.

Mol Cell Biol. 1997 Aug;17(8):4454-64.

27.

Farnesyl: proteintransferase inhibitors as agents to inhibit tumor growth.

Omer CA, Anthony NJ, Buser-Doepner CA, Burkhardt AL, deSolms SJ, Dinsmore CJ, Gibbs JB, Hartman GD, Koblan KS, Lobell RB, Oliff A, Williams TM, Kohl NE.

Biofactors. 1997;6(3):359-66. Review.

PMID:
9288406
28.

The potential of farnesyltransferase inhibitors as cancer chemotherapeutics.

Gibbs JB, Oliff A.

Annu Rev Pharmacol Toxicol. 1997;37:143-66. Review.

PMID:
9131250
29.

Selection of potent inhibitors of farnesyl-protein transferase from a synthetic tetrapeptide combinatorial library.

Wallace A, Koblan KS, Hamilton K, Marquis-Omer DJ, Miller PJ, Mosser SD, Omer CA, Schaber MD, Cortese R, Oliff A, Gibbs JB, Pessi A.

J Biol Chem. 1996 Dec 6;271(49):31306-11.

30.

Chemistry and Biology of Cylindrols: Novel Inhibitors of Ras Farnesyl-Protein Transferase from Cylindrocarpon lucidum.

Singh SB, Ball RG, Bills GF, Cascales C, Gibbs JB, Goetz MA, Hoogsteen K, Jenkins RG, Liesch JM, Lingham RB, Silverman KC, Zink DL.

J Org Chem. 1996 Nov 1;61(22):7727-7737.

PMID:
11667727
31.

New molecular targets for cancer therapy.

Oliff A, Gibbs JB, McCormick F.

Sci Am. 1996 Sep;275(3):144-9. Review. No abstract available.

PMID:
8701284
32.

Farnesyltransferase inhibitors: a new class of cancer chemotherapeutics.

Koblan KS, Kohl NE, Omer CA, Anthony NJ, Conner MW, deSolms SJ, Williams TM, Graham SL, Hartman GD, Oliff A, Gibbs JB.

Biochem Soc Trans. 1996 Aug;24(3):688-92. Review. No abstract available.

PMID:
8878827
33.

2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.

Williams TM, Ciccarone TM, MacTough SC, Bock RL, Conner MW, Davide JP, Hamilton K, Koblan KS, Kohl NE, Kral AM, Mosser SD, Omer CA, Pompliano DL, Rands E, Schaber MD, Shah D, Wilson FR, Gibbs JB, Graham SL, Hartman GD, Oliff AI, Smith RL.

J Med Chem. 1996 Mar 29;39(7):1345-8. No abstract available.

PMID:
8691462
34.

Farnesyltransferase inhibitors and anti-Ras therapy.

Gibbs JB, Kohl NE, Koblan KS, Omer CA, Sepp-Lorenzino L, Rosen N, Anthony NJ, Conner MW, deSolms SJ, Williams TM, Graham SL, Hartman GD, Oliff A.

Breast Cancer Res Treat. 1996;38(1):75-83. Review.

PMID:
8825125
35.

A peptidomimetic inhibitor of farnesyl:protein transferase blocks the anchorage-dependent and -independent growth of human tumor cell lines.

Sepp-Lorenzino L, Ma Z, Rands E, Kohl NE, Gibbs JB, Oliff A, Rosen N.

Cancer Res. 1995 Nov 15;55(22):5302-9.

36.
37.

Development of inhibitors of protein farnesylation as potential chemotherapeutic agents.

Kohl NE, Conner MW, Gibbs JB, Graham SL, Hartman GD, Oliff A.

J Cell Biochem Suppl. 1995;22:145-50. Review.

PMID:
8538192
38.

Inhibition of Ras function in vitro and in vivo using inhibitors of farnesyl-protein transferase.

Kohl NE, Wilson FR, Thomas TJ, Bock RL, Mosser SD, Oliff A, Gibbs JB.

Methods Enzymol. 1995;255:378-86. No abstract available.

PMID:
8524123
39.

Determination of Ras and GTPase-activating protein interactions by kinetic competition assay.

Schaber MD, Gibbs JB.

Methods Enzymol. 1995;255:171-8. No abstract available.

PMID:
8524101
40.

Determination of guanine nucleotides bound to Ras in mammalian cells.

Gibbs JB.

Methods Enzymol. 1995;255:118-25. No abstract available.

PMID:
8524093
41.

Pharmaceutical research in molecular oncology.

Gibbs JB, Oliff A.

Cell. 1994 Oct 21;79(2):193-8. Review. No abstract available.

PMID:
7954788
42.

Synthesis and biological activity of ras farnesyl protein transferase inhibitors. Tetrapeptide analogs with amino methyl and carbon linkages.

Wai JS, Bamberger DL, Fisher TE, Graham SL, Smith RL, Gibbs JB, Mosser SD, Oliff AI, Pompliano DL, Rands E, et al.

Bioorg Med Chem. 1994 Sep;2(9):939-47.

PMID:
7712129
43.

Farnesyltransferase inhibition causes morphological reversion of ras-transformed cells by a complex mechanism that involves regulation of the actin cytoskeleton.

Prendergast GC, Davide JP, deSolms SJ, Giuliani EA, Graham SL, Gibbs JB, Oliff A, Kohl NE.

Mol Cell Biol. 1994 Jun;14(6):4193-202.

44.

Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic.

Gibbs JB, Oliff A, Kohl NE.

Cell. 1994 Apr 22;77(2):175-8. Review. No abstract available.

PMID:
8168127
45.

Ras regulatory interactions: novel targets for anti-cancer intervention?

Prendergast GC, Gibbs JB.

Bioessays. 1994 Mar;16(3):187-91. Review.

PMID:
8166672
46.

cDNA cloning and expression of rat and human protein geranylgeranyltransferase type-I.

Zhang FL, Diehl RE, Kohl NE, Gibbs JB, Giros B, Casey PJ, Omer CA.

J Biol Chem. 1994 Feb 4;269(5):3175-80.

47.

Protein prenylation in eukaryotic microorganisms: genetics, biology and biochemistry.

Omer CA, Gibbs JB.

Mol Microbiol. 1994 Jan;11(2):219-25. Review.

PMID:
8170384
48.
49.

Negative growth selection against rodent fibroblasts targeted for genetic inhibition of farnesyl transferase.

Prendergast GC, Davide JP, Kral A, Diehl R, Gibbs JB, Omer CA, Kohl NE.

Cell Growth Differ. 1993 Sep;4(9):707-13.

50.

Isoprenoid diphosphate utilization by recombinant human farnesyl:protein transferase: interactive binding between substrates and a preferred kinetic pathway.

Pompliano DL, Schaber MD, Mosser SD, Omer CA, Shafer JA, Gibbs JB.

Biochemistry. 1993 Aug 17;32(32):8341-7.

PMID:
8347630

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