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Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors.

Moschos SJ, Sullivan RJ, Hwu WJ, Ramanathan RK, Adjei AA, Fong PC, Shapira-Frommer R, Tawbi HA, Rubino J, Rush TS 3rd, Zhang D, Miselis NR, Samatar AA, Chun P, Rubin EH, Schiller J, Long BJ, Dayananth P, Carr D, Kirschmeier P, Bishop WR, Deng Y, Cooper A, Shipps GW, Moreno BH, Robert L, Ribas A, Flaherty KT.

JCI Insight. 2018 Feb 22;3(4). pii: 92352. doi: 10.1172/jci.insight.92352. eCollection 2018 Feb 22.


Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.

Bogen SL, Pan W, Gibeau CR, Lahue BR, Ma Y, Nair LG, Seigel E, Shipps GW Jr, Tian Y, Wang Y, Lin Y, Liu M, Liu S, Mirza A, Wang X, Lipari P, Seidel-Dugan C, Hicklin DJ, Bishop WR, Rindgen D, Nomeir A, Prosise W, Reichert P, Scapin G, Strickland C, Doll RJ.

ACS Med Chem Lett. 2016 Jan 20;7(3):324-9. doi: 10.1021/acsmedchemlett.5b00472. eCollection 2016 Mar 10.


Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.

Morris EJ, Jha S, Restaino CR, Dayananth P, Zhu H, Cooper A, Carr D, Deng Y, Jin W, Black S, Long B, Liu J, Dinunzio E, Windsor W, Zhang R, Zhao S, Angagaw MH, Pinheiro EM, Desai J, Xiao L, Shipps G, Hruza A, Wang J, Kelly J, Paliwal S, Gao X, Babu BS, Zhu L, Daublain P, Zhang L, Lutterbach BA, Pelletier MR, Philippar U, Siliphaivanh P, Witter D, Kirschmeier P, Bishop WR, Hicklin D, Gilliland DG, Jayaraman L, Zawel L, Fawell S, Samatar AA.

Cancer Discov. 2013 Jul;3(7):742-50. doi: 10.1158/2159-8290.CD-13-0070. Epub 2013 Apr 24.


Clinical trial of a farnesyltransferase inhibitor in children with Hutchinson-Gilford progeria syndrome.

Gordon LB, Kleinman ME, Miller DT, Neuberg DS, Giobbie-Hurder A, Gerhard-Herman M, Smoot LB, Gordon CM, Cleveland R, Snyder BD, Fligor B, Bishop WR, Statkevich P, Regen A, Sonis A, Riley S, Ploski C, Correia A, Quinn N, Ullrich NJ, Nazarian A, Liang MG, Huh SY, Schwartzman A, Kieran MW.

Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16666-71. doi: 10.1073/pnas.1202529109. Epub 2012 Sep 24.


Costello and cardio-facio-cutaneous syndromes: Moving toward clinical trials in RASopathies.

Rauen KA, Banerjee A, Bishop WR, Lauchle JO, McCormick F, McMahon M, Melese T, Munster PN, Nadaf S, Packer RJ, Sebolt-Leopold J, Viskochil DH.

Am J Med Genet C Semin Med Genet. 2011 May 15;157C(2):136-46. doi: 10.1002/ajmg.c.30294. Epub 2011 Apr 14.


A fully human insulin-like growth factor-I receptor antibody SCH 717454 (Robatumumab) has antitumor activity as a single agent and in combination with cytotoxics in pediatric tumor xenografts.

Wang Y, Lipari P, Wang X, Hailey J, Liang L, Ramos R, Liu M, Pachter JA, Bishop WR, Wang Y.

Mol Cancer Ther. 2010 Feb;9(2):410-8. doi: 10.1158/1535-7163.MCT-09-0555. Epub 2010 Feb 2.


SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53.

Demma M, Maxwell E, Ramos R, Liang L, Li C, Hesk D, Rossman R, Mallams A, Doll R, Liu M, Seidel-Dugan C, Bishop WR, Dasmahapatra B.

J Biol Chem. 2010 Apr 2;285(14):10198-212. doi: 10.1074/jbc.M109.083469. Epub 2010 Feb 2.


Discovery of C-imidazole azaheptapyridine FPT inhibitors.

Zhu HY, Cooper AB, Desai J, Njoroge G, Kirschmeier P, Bishop WR, Strickland C, Hruza A, Doll RJ, Girijavallabhan VM.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1134-6. doi: 10.1016/j.bmcl.2009.12.013. Epub 2009 Dec 6.


Continuous and intermittent dosing of lonafarnib potentiates the therapeutic efficacy of docetaxel on preclinical human prostate cancer models.

Liu G, Taylor SA, Marrinan CH, Hsieh Y, Bishop WR, Kirschmeier P, Long BJ.

Int J Cancer. 2009 Dec 1;125(11):2711-20. doi: 10.1002/ijc.24644.


Combining the farnesyltransferase inhibitor lonafarnib with paclitaxel results in enhanced growth inhibitory effects on human ovarian cancer models in vitro and in vivo.

Taylor SA, Marrinan CH, Liu G, Nale L, Bishop WR, Kirschmeier P, Liu M, Long BJ.

Gynecol Oncol. 2008 Apr;109(1):97-106. doi: 10.1016/j.ygyno.2007.12.013. Epub 2008 Jan 31.


Enhanced FTase activity achieved via piperazine interaction with catalytic zinc.

Njoroge FG, Vibulbhan B, Pinto P, Strickland C, Bishop WR, Nomeir A, Girijavallabhan V.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):984-8. Epub 2005 Nov 16. Erratum in: Bioorg Med Chem Lett. 2006 Apr 15;16(8):2312.


Lipid posttranslational modifications. Farnesyl transferase inhibitors.

Basso AD, Kirschmeier P, Bishop WR.

J Lipid Res. 2006 Jan;47(1):15-31. Epub 2005 Nov 8. Review.


Inhibition of insulin-like growth factor-I receptor (IGF-IR) signaling and tumor cell growth by a fully human neutralizing anti-IGF-IR antibody.

Wang Y, Hailey J, Williams D, Wang Y, Lipari P, Malkowski M, Wang X, Xie L, Li G, Saha D, Ling WL, Cannon-Carlson S, Greenberg R, Ramos RA, Shields R, Presta L, Brams P, Bishop WR, Pachter JA.

Mol Cancer Ther. 2005 Aug;4(8):1214-21.


Integrative genomics revealed RAI3 is a cell growth-promoting gene and a novel P53 transcriptional target.

Wu Q, Ding W, Mirza A, Van Arsdale T, Wei I, Bishop WR, Basso A, McClanahan T, Luo L, Kirschmeier P, Gustafson E, Hernandez M, Liu S.

J Biol Chem. 2005 Apr 1;280(13):12935-43. Epub 2005 Jan 18.


Farnesyl protein transferase inhibitors targeting the catalytic zinc for enhanced binding.

Njoroge FG, Vibulbhan B, Pinto P, Strickland C, Kirschmeier P, Bishop WR, Girijavallabhan V.

Bioorg Med Chem Lett. 2004 Dec 6;14(23):5877-80.


Farnesyltransferase inhibitors as anticancer agents: critical crossroads.

Doll RJ, Kirschmeier P, Bishop WR.

Curr Opin Drug Discov Devel. 2004 Jul;7(4):478-86. Review.


Phase I study of the farnesyltransferase inhibitor lonafarnib with paclitaxel in solid tumors.

Khuri FR, Glisson BS, Kim ES, Statkevich P, Thall PF, Meyers ML, Herbst RS, Munden RF, Tendler C, Zhu Y, Bangert S, Thompson E, Lu C, Wang XM, Shin DM, Kies MS, Papadimitrakopoulou V, Fossella FV, Kirschmeier P, Bishop WR, Hong WK.

Clin Cancer Res. 2004 May 1;10(9):2968-76.


Farnesyl transferase inhibitors: mechanism of action, translational studies and clinical evaluation.

Bishop WR, Kirschmeier P, Baum C.

Cancer Biol Ther. 2003 Jul-Aug;2(4 Suppl 1):S96-104. Review. No abstract available.


Global transcriptional program of p53 target genes during the process of apoptosis and cell cycle progression.

Mirza A, Wu Q, Wang L, McClanahan T, Bishop WR, Gheyas F, Ding W, Hutchins B, Hockenberry T, Kirschmeier P, Greene JR, Liu S.

Oncogene. 2003 Jun 5;22(23):3645-54.


Efficacy of SCH66336, a farnesyl transferase inhibitor, in conjunction with imatinib against BCR-ABL-positive cells.

Nakajima A, Tauchi T, Sumi M, Bishop WR, Ohyashiki K.

Mol Cancer Ther. 2003 Mar;2(3):219-24.


Neutralizing anti-insulin-like growth factor receptor 1 antibodies inhibit receptor function and induce receptor degradation in tumor cells.

Hailey J, Maxwell E, Koukouras K, Bishop WR, Pachter JA, Wang Y.

Mol Cancer Ther. 2002 Dec;1(14):1349-53.


Trihalobenzocycloheptapyridine analogues of Sch 66336 as potent inhibitors of farnesyl protein transferase.

Njoroge FG, Vibulbhan B, Pinto P, Strickland CL, Bishop WR, Kirschmeir P, Girijavallabhan V, Ganguly AK.

Bioorg Med Chem. 2003 Jan 2;11(1):139-43.


Human survivin is negatively regulated by wild-type p53 and participates in p53-dependent apoptotic pathway.

Mirza A, McGuirk M, Hockenberry TN, Wu Q, Ashar H, Black S, Wen SF, Wang L, Kirschmeier P, Bishop WR, Nielsen LL, Pickett CB, Liu S.

Oncogene. 2002 Apr 18;21(17):2613-22.


Synthesis of 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase.

Cooper AB, Strickland CL, Wang J, Desai J, Kirschmeier P, Patton R, Bishop WR, Weber PC, Girijavallabhan V.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):601-5.


Inhibitors of farnesyl protein transferase and MEK1,2 induce apoptosis in fibroblasts transformed with farnesylated but not geranylgeranylated H-Ras.

Brassard DL, English JM, Malkowski M, Kirschmeier P, Nagabhushan TL, Bishop WR.

Exp Cell Res. 2002 Feb 15;273(2):138-46.


Orally bioavailable farnesyltransferase inhibitors as anticancer agents in transgenic and xenograft models.

Liu M, Bishop WR, Nielsen LL, Bryant MS, Kirschmeier P.

Methods Enzymol. 2001;333:306-18.


Protein farnesyltransferase assays.

Zhang FL, Bishop WR.

Curr Protoc Pharmacol. 2001 May;Chapter 3:Unit3.4. doi: 10.1002/0471141755.ph0304s00. No abstract available.


In vivo prenylation analysis of Ras and Rho proteins.

Kirschmeier PT, Whyte D, Wilson O, Bishop WR, Pai JK.

Methods Enzymol. 2001;332:115-27. No abstract available.


Activity of the farnesyl protein transferase inhibitor SCH66336 against BCR/ABL-induced murine leukemia and primary cells from patients with chronic myeloid leukemia.

Peters DG, Hoover RR, Gerlach MJ, Koh EY, Zhang H, Choe K, Kirschmeier P, Bishop WR, Daley GQ.

Blood. 2001 Mar 1;97(5):1404-12.


The farnesyl protein transferase inhibitor SCH66336 synergizes with taxanes in vitro and enhances their antitumor activity in vivo.

Shi B, Yaremko B, Hajian G, Terracina G, Bishop WR, Liu M, Nielsen LL.

Cancer Chemother Pharmacol. 2000;46(5):387-93.


The farnesyl transferase inhibitor SCH 66336 induces a G(2) --> M or G(1) pause in sensitive human tumor cell lines.

Ashar HR, James L, Gray K, Carr D, McGuirk M, Maxwell E, Black S, Armstrong L, Doll RJ, Taveras AG, Bishop WR, Kirschmeier P.

Exp Cell Res. 2001 Jan 1;262(1):17-27.


Biological effects and mechanism of action of farnesyl transferase inhibitors.

Ashar HR, Armstrong L, James LJ, Carr DM, Gray K, Taveras A, Doll RJ, Bishop WR, Kirschmeier PT.

Chem Res Toxicol. 2000 Oct;13(10):949-52. Review. No abstract available.


Farnesyl transferase inhibitors block the farnesylation of CENP-E and CENP-F and alter the association of CENP-E with the microtubules.

Ashar HR, James L, Gray K, Carr D, Black S, Armstrong L, Bishop WR, Kirschmeier P.

J Biol Chem. 2000 Sep 29;275(39):30451-7.


A Phase I trial of the farnesyl transferase inhibitor SCH66336: evidence for biological and clinical activity.

Adjei AA, Erlichman C, Davis JN, Cutler DL, Sloan JA, Marks RS, Hanson LJ, Svingen PA, Atherton P, Bishop WR, Kirschmeier P, Kaufmann SH.

Cancer Res. 2000 Apr 1;60(7):1871-7.


A farnesyl transferase inhibitor suppresses TPA-mediated skin tumor development without altering hyperplasia in the ras transgenic Tg.AC mouse.

Trempus CS, Bishop WR, Njoroge FG, Doll RJ, Battalora MS, Mahler JF, Haseman JK, Tennant RW.

Mol Carcinog. 2000 Jan;27(1):24-33.


Combination therapy with the farnesyl protein transferase inhibitor SCH66336 and SCH58500 (p53 adenovirus) in preclinical cancer models.

Nielsen LL, Shi B, Hajian G, Yaremko B, Lipari P, Ferrari E, Gurnani M, Malkowski M, Chen J, Bishop WR, Liu M.

Cancer Res. 1999 Dec 1;59(23):5896-901.


Analogues of 1-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo-[5,6]-cyclohepta [1,2-b]pyridin-11-yl)piperidine as inhibitors of farnesyl protein transferase.

Afonso A, Weinstein J, Kelly J, Wolin R, Rosenblum SB, Connolly M, Guzi T, James L, Carr D, Patton R, Bishop WR, Kirshmeier P, Liu M, Heimark L, Chen KJ, Nomeir AA.

Bioorg Med Chem. 1999 Sep;7(9):1845-55.


Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.

Taveras AG, Deskus J, Chao J, Vaccaro CJ, Njoroge FG, Vibulbhan B, Pinto P, Remiszewski S, del Rosario J, Doll RJ, Alvarez C, Lalwani T, Mallams AK, Rossman RR, Afonso A, Girijavallabhan VM, Ganguly AK, Pramanik B, Heimark L, Bishop WR, Wang L, Kirschmeier P, James L, Carr D, Liu M, et al.

J Med Chem. 1999 Jul 15;42(14):2651-61.


Atropisomeric trihalobenzocycloheptapyridine analogues provide stereoselective FPT inhibitors with antitumor activity.

Njoroge FG, Vibulbhan B, Bishop WR, Kirschmeier P, Bryant MS, Nomeir AA, Liu M, Doll RJ, Girijavallabhan VM, Ganguly AK.

Bioorg Med Chem. 1999 May;7(5):861-7.


Activity of SCH 66336, a tricyclic farnesyltransferase inhibitor, against human tumor colony-forming units.

Petit T, Izbicka E, Lawrence RA, Bishop WR, Weitman S, Von Hoff DD.

Ann Oncol. 1999 Apr;10(4):449-53.


Treatment of neoplastic meningitis with intrathecal temozolomide.

Sampson JH, Archer GE, Villavicencio AT, McLendon RE, Friedman AH, Bishop WR, Bigner DD, Friedman HS.

Clin Cancer Res. 1999 May;5(5):1183-8.


Effects of SCH 59228, an orally bioavailable farnesyl protein transferase inhibitor, on the growth of oncogene-transformed fibroblasts and a human colon carcinoma xenograft in nude mice.

Liu M, Bryant MS, Chen J, Lee S, Yaremko B, Li Z, Dell J, Lipari P, Malkowski M, Prioli N, Rossman RR, Korfmacher WA, Nomeir AA, Lin CC, Mallams AK, Doll RJ, Catino JJ, Girijavallabhan VM, Kirschmeier P, Bishop WR.

Cancer Chemother Pharmacol. 1999;43(1):50-8.


Inhibitors of farnesyl protein transferase. Synthesis and biological activity of amide and cyanoguanidine derivatives containing a 5,11-dihydro[1]benzthiepin, benzoxepin, and benzazepin [4,3-b]pyridine ring system.

Wolin R, Connolly M, Kelly J, Weinstein J, Rosenblum S, Afonso A, James L, Kirschmeier P, Bishop WR.

Bioorg Med Chem Lett. 1998 Sep 22;8(18):2521-6.


(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.

Njoroge FG, Taveras AG, Kelly J, Remiszewski S, Mallams AK, Wolin R, Afonso A, Cooper AB, Rane DF, Liu YT, Wong J, Vibulbhan B, Pinto P, Deskus J, Alvarez CS, del Rosario J, Connolly M, Wang J, Desai J, Rossman RR, Bishop WR, Patton R, Wang L, Kirschmeier P, Ganguly AK, et al.

J Med Chem. 1998 Nov 19;41(24):4890-902.


Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice.

Liu M, Bryant MS, Chen J, Lee S, Yaremko B, Lipari P, Malkowski M, Ferrari E, Nielsen L, Prioli N, Dell J, Sinha D, Syed J, Korfmacher WA, Nomeir AA, Lin CC, Wang L, Taveras AG, Doll RJ, Njoroge FG, Mallams AK, Remiszewski S, Catino JJ, Girijavallabhan VM, Bishop WR, et al.

Cancer Res. 1998 Nov 1;58(21):4947-56.


Synthesis of isomeric 3-piperidinyl and 3-pyrrolidinyl benzo[5,6]cyclohepta[1,2-b]pyridines: sulfonamido derivatives as inhibitors of Ras prenylation.

Kelly J, Wolin R, Connolly M, Afonso A, James L, Kirshmeier P, Bishop WR, McPhail AT.

Bioorg Med Chem. 1998 Jun;6(6):673-86.


Potent, selective, and orally bioavailable tricyclic pyridyl acetamide N-oxide inhibitors of farnesyl protein transferase with enhanced in vivo antitumor activity.

Njoroge FG, Vibulbhan B, Pinto P, Bishop WR, Bryant MS, Nomeir AA, Lin C, Liu M, Doll RJ, Girijavallabhan V, Ganguly AK.

J Med Chem. 1998 May 7;41(10):1561-7.


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