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Items: 1 to 50 of 77

1.

Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.

Huang A, Jayaraman L, Fura A, Vite GD, Trainor GL, Gottardis MM, Spires TE, Spires VM, Rizzo CA, Obermeier MT, Elzinga PA, Todderud G, Fan Y, Newitt JA, Beyer SM, Zhu Y, Warrack BM, Goodenough AK, Tebben AJ, Doweyko AM, Gold DL, Balog A.

ACS Med Chem Lett. 2015 Dec 2;7(1):40-5. doi: 10.1021/acsmedchemlett.5b00310. eCollection 2016 Jan 14.

2.

9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.

Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Liu Q, Batt D, Lombardo LJ, Vyas D, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Lippy J, Khan J, Sack JS, Purandare AV.

Bioorg Med Chem Lett. 2015 Jul 15;25(14):2809-12. doi: 10.1016/j.bmcl.2015.04.101. Epub 2015 May 11.

PMID:
25987372
3.

Combined Inhibition of IGF-1R/IR and Src family kinases enhances antitumor effects in prostate cancer by decreasing activated survival pathways.

Dayyani F, Parikh NU, Varkaris AS, Song JH, Moorthy S, Chatterji T, Maity SN, Wolfe AR, Carboni JM, Gottardis MM, Logothetis CJ, Gallick GE.

PLoS One. 2012;7(12):e51189. doi: 10.1371/journal.pone.0051189. Epub 2012 Dec 26.

4.

IGF signaling contributes to malignant transformation of hematopoietic progenitors by the MLL-AF9 oncoprotein.

Jenkins CR, Shevchuk OO, Giambra V, Lam SH, Carboni JM, Gottardis MM, Holzenberger M, Pollak M, Humphries RK, Weng AP.

Exp Hematol. 2012 Sep;40(9):715-723.e6. doi: 10.1016/j.exphem.2012.05.003. Epub 2012 May 18.

PMID:
22613471
5.

IGFBP ratio confers resistance to IGF targeting and correlates with increased invasion and poor outcome in breast tumors.

Becker MA, Hou X, Harrington SC, Weroha SJ, Gonzalez SE, Jacob KA, Carboni JM, Gottardis MM, Haluska P.

Clin Cancer Res. 2012 Mar 15;18(6):1808-17. doi: 10.1158/1078-0432.CCR-11-1806. Epub 2012 Jan 27.

6.

Dual IGF-1R/InsR inhibitor BMS-754807 synergizes with hormonal agents in treatment of estrogen-dependent breast cancer.

Hou X, Huang F, Macedo LF, Harrington SC, Reeves KA, Greer A, Finckenstein FG, Brodie A, Gottardis MM, Carboni JM, Haluska P.

Cancer Res. 2011 Dec 15;71(24):7597-607. doi: 10.1158/0008-5472.CAN-11-1080. Epub 2011 Oct 31.

7.

Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2.

Purandare AV, McDevitt TM, Wan H, You D, Penhallow B, Han X, Vuppugalla R, Zhang Y, Ruepp SU, Trainor GL, Lombardo L, Pedicord D, Gottardis MM, Ross-Macdonald P, de Silva H, Hosbach J, Emanuel SL, Blat Y, Fitzpatrick E, Taylor TL, McIntyre KW, Michaud E, Mulligan C, Lee FY, Woolfson A, Lasho TL, Pardanani A, Tefferi A, Lorenzi MV.

Leukemia. 2012 Feb;26(2):280-8. doi: 10.1038/leu.2011.292. Epub 2011 Oct 21.

PMID:
22015772
8.

A tripartite complex composed of ETV6-NTRK3, IRS1 and IGF1R is required for ETV6-NTRK3-mediated membrane localization and transformation.

Tognon CE, Martin MJ, Moradian A, Trigo G, Rotblat B, Cheng SW, Pollard M, Uy E, Chow C, Carboni JM, Gottardis MM, Pollak M, Morin GB, Sorensen PH.

Oncogene. 2012 Mar 8;31(10):1334-40. doi: 10.1038/onc.2011.323. Epub 2011 Aug 1.

PMID:
21804605
9.

Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.

Harikrishnan LS, Kamau MG, Wan H, Inghrim JA, Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Lombardo LJ, Poss MA, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Baldwin KF, Lippy J, Nirschl DS, Qiu R, Miller AV, Khan J, Sack JS, Purandare AV.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1425-8. doi: 10.1016/j.bmcl.2011.01.022. Epub 2011 Jan 11.

PMID:
21282055
10.

Drug efflux by breast cancer resistance protein is a mechanism of resistance to the benzimidazole insulin-like growth factor receptor/insulin receptor inhibitor, BMS-536924.

Hou X, Huang F, Carboni JM, Flatten K, Asmann YW, Ten Eyck C, Nakanishi T, Tibodeau JD, Ross DD, Gottardis MM, Erlichman C, Kaufmann SH, Haluska P.

Mol Cancer Ther. 2011 Jan;10(1):117-25. doi: 10.1158/1535-7163.MCT-10-0438.

11.

High IGF-IR activity in triple-negative breast cancer cell lines and tumorgrafts correlates with sensitivity to anti-IGF-IR therapy.

Litzenburger BC, Creighton CJ, Tsimelzon A, Chan BT, Hilsenbeck SG, Wang T, Carboni JM, Gottardis MM, Huang F, Chang JC, Lewis MT, Rimawi MF, Lee AV.

Clin Cancer Res. 2011 Apr 15;17(8):2314-27. doi: 10.1158/1078-0432.CCR-10-1903. Epub 2010 Dec 22.

12.

ETV6-NTRK3-mediated breast epithelial cell transformation is blocked by targeting the IGF1R signaling pathway.

Tognon CE, Somasiri AM, Evdokimova VE, Trigo G, Uy EE, Melnyk N, Carboni JM, Gottardis MM, Roskelley CD, Pollak M, Sorensen PH.

Cancer Res. 2011 Feb 1;71(3):1060-70. doi: 10.1158/0008-5472.CAN-10-3096. Epub 2010 Dec 9.

13.

A fibronectin scaffold approach to bispecific inhibitors of epidermal growth factor receptor and insulin-like growth factor-I receptor.

Emanuel SL, Engle LJ, Chao G, Zhu RR, Cao C, Lin Z, Yamniuk AP, Hosbach J, Brown J, Fitzpatrick E, Gokemeijer J, Morin P, Morse BA, Carvajal IM, Fabrizio D, Wright MC, Das Gupta R, Gosselin M, Cataldo D, Ryseck RP, Doyle ML, Wong TW, Camphausen RT, Cload ST, Marsh HN, Gottardis MM, Furfine ES.

MAbs. 2011 Jan-Feb;3(1):38-48. Epub 2011 Jan 1.

14.

Synthetic lethality screens reveal RPS6 and MST1R as modifiers of insulin-like growth factor-1 receptor inhibitor activity in childhood sarcomas.

Potratz JC, Saunders DN, Wai DH, Ng TL, McKinney SE, Carboni JM, Gottardis MM, Triche TJ, Jürgens H, Pollak MN, Aparicio SA, Sorensen PH.

Cancer Res. 2010 Nov 1;70(21):8770-81. doi: 10.1158/0008-5472.CAN-10-1093. Epub 2010 Oct 19.

15.

Drug safety is a barrier to the discovery and development of new androgen receptor antagonists.

Foster WR, Car BD, Shi H, Levesque PC, Obermeier MT, Gan J, Arezzo JC, Powlin SS, Dinchuk JE, Balog A, Salvati ME, Attar RM, Gottardis MM.

Prostate. 2011 Apr;71(5):480-8. doi: 10.1002/pros.21263. Epub 2010 Sep 28.

PMID:
20878947
16.

Differential mechanisms of acquired resistance to insulin-like growth factor-i receptor antibody therapy or to a small-molecule inhibitor, BMS-754807, in a human rhabdomyosarcoma model.

Huang F, Hurlburt W, Greer A, Reeves KA, Hillerman S, Chang H, Fargnoli J, Graf Finckenstein F, Gottardis MM, Carboni JM.

Cancer Res. 2010 Sep 15;70(18):7221-31. doi: 10.1158/0008-5472.CAN-10-0391. Epub 2010 Aug 31.

17.

Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.

Xiao HY, Balog A, Attar RM, Fairfax D, Fleming LB, Holst CL, Martin GS, Rossiter LM, Chen J, Cvjic ME, Dell-John J, Geng J, Gottardis MM, Han WC, Nation A, Obermeier M, Rizzo CA, Schweizer L, Spires T Jr, Shan W, Gavai A, Salvati ME, Vite G.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4491-5. doi: 10.1016/j.bmcl.2010.06.034. Epub 2010 Jun 10.

PMID:
20584610
18.

Molecular markers for novel therapies in neuroendocrine (carcinoid) tumors.

Gilbert JA, Adhikari LJ, Lloyd RV, Rubin J, Haluska P, Carboni JM, Gottardis MM, Ames MM.

Endocr Relat Cancer. 2010 Jun 25;17(3):623-36. doi: 10.1677/ERC-09-0318. Print 2010 Sep.

19.

Insulin-mediated acceleration of breast cancer development and progression in a nonobese model of type 2 diabetes.

Novosyadlyy R, Lann DE, Vijayakumar A, Rowzee A, Lazzarino DA, Fierz Y, Carboni JM, Gottardis MM, Pennisi PA, Molinolo AA, Kurshan N, Mejia W, Santopietro S, Yakar S, Wood TL, LeRoith D.

Cancer Res. 2010 Jan 15;70(2):741-51. doi: 10.1158/0008-5472.CAN-09-2141. Epub 2010 Jan 12.

20.

BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR.

Carboni JM, Wittman M, Yang Z, Lee F, Greer A, Hurlburt W, Hillerman S, Cao C, Cantor GH, Dell-John J, Chen C, Discenza L, Menard K, Li A, Trainor G, Vyas D, Kramer R, Attar RM, Gottardis MM.

Mol Cancer Ther. 2009 Dec;8(12):3341-9. doi: 10.1158/1535-7163.MCT-09-0499.

21.

Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.

Wittman MD, Carboni JM, Yang Z, Lee FY, Antman M, Attar R, Balimane P, Chang C, Chen C, Discenza L, Frennesson D, Gottardis MM, Greer A, Hurlburt W, Johnson W, Langley DR, Li A, Li J, Liu P, Mastalerz H, Mathur A, Menard K, Patel K, Sack J, Sang X, Saulnier M, Smith D, Stefanski K, Trainor G, Velaparthi U, Zhang G, Zimmermann K, Vyas DM.

J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r.

PMID:
19778024
22.

BMS-536924 sensitizes human epithelial ovarian cancer cells to the PARP inhibitor, 3-aminobenzamide.

Beauchamp MC, Knafo A, Yasmeen A, Carboni JM, Gottardis MM, Pollak MN, Gotlieb WH.

Gynecol Oncol. 2009 Nov;115(2):193-8. doi: 10.1016/j.ygyno.2009.07.009. Epub 2009 Aug 21.

PMID:
19699512
23.

Discovery of BMS-641988, a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer.

Attar RM, Jure-Kunkel M, Balog A, Cvijic ME, Dell-John J, Rizzo CA, Schweizer L, Spires TE, Platero JS, Obermeier M, Shan W, Salvati ME, Foster WR, Dinchuk J, Chen SJ, Vite G, Kramer R, Gottardis MM.

Cancer Res. 2009 Aug 15;69(16):6522-30. doi: 10.1158/0008-5472.CAN-09-1111. Epub 2009 Aug 4.

24.

Castration-resistant prostate cancer: locking up the molecular escape routes.

Attar RM, Takimoto CH, Gottardis MM.

Clin Cancer Res. 2009 May 15;15(10):3251-5. doi: 10.1158/1078-0432.CCR-08-1171. Epub 2009 May 15. Review.

25.

BMS-536924 reverses IGF-IR-induced transformation of mammary epithelial cells and causes growth inhibition and polarization of MCF7 cells.

Litzenburger BC, Kim HJ, Kuiatse I, Carboni JM, Attar RM, Gottardis MM, Fairchild CR, Lee AV.

Clin Cancer Res. 2009 Jan 1;15(1):226-37. doi: 10.1158/1078-0432.CCR-08-0801.

26.

The mechanisms of differential sensitivity to an insulin-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors.

Huang F, Greer A, Hurlburt W, Han X, Hafezi R, Wittenberg GM, Reeves K, Chen J, Robinson D, Li A, Lee FY, Gottardis MM, Clark E, Helman L, Attar RM, Dongre A, Carboni JM.

Cancer Res. 2009 Jan 1;69(1):161-70. doi: 10.1158/0008-5472.CAN-08-0835.

27.

HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924.

Haluska P, Carboni JM, TenEyck C, Attar RM, Hou X, Yu C, Sagar M, Wong TW, Gottardis MM, Erlichman C.

Mol Cancer Ther. 2008 Sep;7(9):2589-98. doi: 10.1158/1535-7163.MCT-08-0493. Epub 2008 Sep 2.

28.

Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.

Salvati ME, Balog A, Shan W, Rampulla R, Giese S, Mitt T, Furch JA, Vite GD, Attar RM, Jure-Kunkel M, Geng J, Rizzo CA, Gottardis MM, Krystek SR, Gougoutas J, Galella MA, Obermeier M, Fura A, Chandrasena G.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1910-5. doi: 10.1016/j.bmcl.2008.02.006. Epub 2008 Feb 8.

PMID:
18291644
29.

The androgen receptor can signal through Wnt/beta-Catenin in prostate cancer cells as an adaptation mechanism to castration levels of androgens.

Schweizer L, Rizzo CA, Spires TE, Platero JS, Wu Q, Lin TA, Gottardis MM, Attar RM.

BMC Cell Biol. 2008 Jan 24;9:4. doi: 10.1186/1471-2121-9-4.

30.

Phase I trial of weekly paclitaxel and BMS-214662 in patients with advanced solid tumors.

Bailey HH, Alberti DB, Thomas JP, Mulkerin DL, Binger KA, Gottardis MM, Martell RE, Wilding G.

Clin Cancer Res. 2007 Jun 15;13(12):3623-9. Epub 2007 May 17.

31.

Constitutively active type I insulin-like growth factor receptor causes transformation and xenograft growth of immortalized mammary epithelial cells and is accompanied by an epithelial-to-mesenchymal transition mediated by NF-kappaB and snail.

Kim HJ, Litzenburger BC, Cui X, Delgado DA, Grabiner BC, Lin X, Lewis MT, Gottardis MM, Wong TW, Attar RM, Carboni JM, Lee AV.

Mol Cell Biol. 2007 Apr;27(8):3165-75. Epub 2007 Feb 12.

32.

GREB1 is a novel androgen-regulated gene required for prostate cancer growth.

Rae JM, Johnson MD, Cordero KE, Scheys JO, Larios JM, Gottardis MM, Pienta KJ, Lippman ME.

Prostate. 2006 Jun 1;66(8):886-94.

PMID:
16496412
33.

Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3.

Fink BE, Gavai AV, Tokarski JS, Goyal B, Misra R, Xiao HY, Kimball SD, Han WC, Norris D, Spires TE, You D, Gottardis MM, Lorenzi MV, Vite GD.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1532-6. Epub 2006 Jan 4.

PMID:
16386902
34.

Identification of novel functional inhibitors of 17beta-hydroxysteroid dehydrogenase type III (17beta-HSD3).

Spires TE, Fink BE, Kick EK, You D, Rizzo CA, Takenaka I, Lawrence RM, Ruan Z, Salvati ME, Vite GD, Weinmann R, Attar RM, Gottardis MM, Lorenzi MV.

Prostate. 2005 Oct 1;65(2):159-70.

PMID:
15924334
35.

Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.

Salvati ME, Balog A, Wei DD, Pickering D, Attar RM, Geng J, Rizzo CA, Hunt JT, Gottardis MM, Weinmann R, Martinez R.

Bioorg Med Chem Lett. 2005 Jan 17;15(2):389-93.

PMID:
15603960
36.

Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.

Salvati ME, Balog A, Shan W, Wei DD, Pickering D, Attar RM, Geng J, Rizzo CA, Gottardis MM, Weinmann R, Krystek SR, Sack J, An Y, Kish K.

Bioorg Med Chem Lett. 2005 Jan 17;15(2):271-6.

PMID:
15603938
37.

Inhibition of proliferation and estrogen receptor signaling by peroxisome proliferator-activated receptor gamma ligands in uterine leiomyoma.

Houston KD, Copland JA, Broaddus RR, Gottardis MM, Fischer SM, Walker CL.

Cancer Res. 2003 Mar 15;63(6):1221-7.

38.

Quality indicators increase the reliability of microarray data.

Raffelsberger W, Dembélé D, Neubauer MG, Gottardis MM, Gronemeyer H.

Genomics. 2002 Oct;80(4):385-94.

PMID:
12376092
39.

Synergistic cytotoxicity exhibited by combination treatment of selective retinoid ligands with taxol (Paclitaxel).

Vivat-Hannah V, You D, Rizzo C, Daris JP, Lapointe P, Zusi FC, Marinier A, Lorenzi MV, Gottardis MM.

Cancer Res. 2001 Dec 15;61(24):8703-11.

40.

Circumventing tamoxifen resistance in breast cancers using antiestrogens that induce unique conformational changes in the estrogen receptor.

Connor CE, Norris JD, Broadwater G, Willson TM, Gottardis MM, Dewhirst MW, McDonnell DP.

Cancer Res. 2001 Apr 1;61(7):2917-22.

41.

Efficacy of LGD1069 (Targretin), a retinoid X receptor-selective ligand, for treatment of uterine leiomyoma.

Gamage SD, Bischoff ED, Burroughs KD, Lamph WW, Gottardis MM, Walker CL, Fuchs-Young R.

J Pharmacol Exp Ther. 2000 Nov;295(2):677-81.

42.

9-cis-Retinoic acid suppresses mammary tumorigenesis in C3(1)-simian virus 40 T antigen-transgenic mice.

Wu K, Kim HT, Rodriquez JL, Munoz-Medellin D, Mohsin SK, Hilsenbeck SG, Lamph WW, Gottardis MM, Shirley MA, Kuhn JG, Green JE, Brown PH.

Clin Cancer Res. 2000 Sep;6(9):3696-704.

43.

Estrogen receptor activation via activation function 2 predicts agonism of xenoestrogens in normal and neoplastic cells of the uterine myometrium.

Hunter DS, Hodges LC, Vonier PM, Fuchs-Young R, Gottardis MM, Walker CL.

Cancer Res. 1999 Jul 1;59(13):3090-9.

44.

5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.

Zhi L, Tegley CM, Edwards JP, West SJ, Marschke KB, Gottardis MM, Mais DE, Jones TK.

Bioorg Med Chem Lett. 1998 Dec 1;8(23):3365-70.

PMID:
9873735
45.

5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.

Tegley CM, Zhi L, Marschke KB, Gottardis MM, Yang Q, Jones TK.

J Med Chem. 1998 Oct 22;41(22):4354-9.

PMID:
9784110
46.

Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists.

Edwards JP, Zhi L, Pooley CL, Tegley CM, West SJ, Wang MW, Gottardis MM, Pathirana C, Schrader WT, Jones TK.

J Med Chem. 1998 Jul 16;41(15):2779-85.

PMID:
9667968
47.

5-Aryl-1,2-dihydro-5H-chromeno[3,4-f]quinolines as potent, orally active, nonsteroidal progesterone receptor agonists: the effect of D-ring substituents.

Edwards JP, West SJ, Marschke KB, Mais DE, Gottardis MM, Jones TK.

J Med Chem. 1998 Jan 29;41(3):303-10.

PMID:
9464361
48.

5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.

Zhi L, Tegley CM, Kallel EA, Marschke KB, Mais DE, Gottardis MM, Jones TK.

J Med Chem. 1998 Jan 29;41(3):291-302.

PMID:
9464360
49.

Beyond tamoxifen: the retinoid X receptor-selective ligand LGD1069 (TARGRETIN) causes complete regression of mammary carcinoma.

Bischoff ED, Gottardis MM, Moon TE, Heyman RA, Lamph WW.

Cancer Res. 1998 Feb 1;58(3):479-84.

50.

Decreased Egr-1 expression in human, mouse and rat mammary cells and tissues correlates with tumor formation.

Huang RP, Fan Y, de Belle I, Niemeyer C, Gottardis MM, Mercola D, Adamson ED.

Int J Cancer. 1997 Jul 3;72(1):102-9.

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