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Items: 11

1.

The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients.

Hallin J, Engstrom LD, Hargis L, Calinisan A, Aranda R, Briere DM, Sudhakar N, Bowcut V, Baer BR, Ballard JA, Burkard MR, Fell JB, Fischer JP, Vigers GP, Xue JY, Gatto S, Fernandez-Banet J, Pavlicek A, Velastegui K, Chao RC, Barton J, Pierobon M, Baldelli E, Patricoin EF, Cassidy DP, Marx MA, Rybkin II, Johnson ML, Ou SI, Lito P, Papadopoulos KP, Janne PA, Olson P, Christensen JG.

Cancer Discov. 2019 Oct 28. pii: CD-19-1167. doi: 10.1158/2159-8290.CD-19-1167. [Epub ahead of print]

PMID:
31658955
2.

The class I/IV HDAC inhibitor mocetinostat increases tumor antigen presentation, decreases immune suppressive cell types and augments checkpoint inhibitor therapy.

Briere D, Sudhakar N, Woods DM, Hallin J, Engstrom LD, Aranda R, Chiang H, Sodré AL, Olson P, Weber JS, Christensen JG.

Cancer Immunol Immunother. 2018 Mar;67(3):381-392. doi: 10.1007/s00262-017-2091-y. Epub 2017 Nov 9.

PMID:
29124315
3.

Glesatinib Exhibits Antitumor Activity in Lung Cancer Models and Patients Harboring MET Exon 14 Mutations and Overcomes Mutation-mediated Resistance to Type I MET Inhibitors in Nonclinical Models.

Engstrom LD, Aranda R, Lee M, Tovar EA, Essenburg CJ, Madaj Z, Chiang H, Briere D, Hallin J, Lopez-Casas PP, Baños N, Menendez C, Hidalgo M, Tassell V, Chao R, Chudova DI, Lanman RB, Olson P, Bazhenova L, Patel SP, Graveel C, Nishino M, Shapiro GI, Peled N, Awad MM, Jänne PA, Christensen JG.

Clin Cancer Res. 2017 Nov 1;23(21):6661-6672. doi: 10.1158/1078-0432.CCR-17-1192. Epub 2017 Aug 1.

4.

PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models.

Zou HY, Friboulet L, Kodack DP, Engstrom LD, Li Q, West M, Tang RW, Wang H, Tsaparikos K, Wang J, Timofeevski S, Katayama R, Dinh DM, Lam H, Lam JL, Yamazaki S, Hu W, Patel B, Bezwada D, Frias RL, Lifshits E, Mahmood S, Gainor JF, Affolter T, Lappin PB, Gukasyan H, Lee N, Deng S, Jain RK, Johnson TW, Shaw AT, Fantin VR, Smeal T.

Cancer Cell. 2015 Jul 13;28(1):70-81. doi: 10.1016/j.ccell.2015.05.010. Epub 2015 Jul 2.

5.

PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.

Zou HY, Li Q, Engstrom LD, West M, Appleman V, Wong KA, McTigue M, Deng YL, Liu W, Brooun A, Timofeevski S, McDonnell SR, Jiang P, Falk MD, Lappin PB, Affolter T, Nichols T, Hu W, Lam J, Johnson TW, Smeal T, Charest A, Fantin VR.

Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8. doi: 10.1073/pnas.1420785112. Epub 2015 Mar 2.

6.

Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.

Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP.

J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q. Epub 2014 Jun 3.

PMID:
24819116
7.

Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.

Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Johnson PS, Kania RS, Lam H, Lam JL, Le PT, Li Q, Lingardo L, Liu W, Lu MW, McTigue M, Palmer CL, Richardson PF, Sach NW, Shen H, Smeal T, Smith GL, Stewart AE, Timofeevski S, Tsaparikos K, Wang H, Zhu H, Zhu J, Zou HY, Edwards MP.

J Med Chem. 2014 Feb 27;57(4):1170-87. doi: 10.1021/jm401805h. Epub 2014 Feb 6.

8.

Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor.

Zou HY, Li Q, Lee JH, Arango ME, Burgess K, Qiu M, Engstrom LD, Yamazaki S, Parker M, Timofeevski S, Cui JJ, McTigue M, Los G, Bender SL, Smeal T, Christensen JG.

Mol Cancer Ther. 2012 Apr;11(4):1036-47. doi: 10.1158/1535-7163.MCT-11-0839. Epub 2012 Mar 2.

9.

Mxi1-0, an alternatively transcribed Mxi1 isoform, is overexpressed in glioblastomas.

Engstrom LD, Youkilis AS, Gorelick JL, Zheng D, Ackley V, Petroff CA, Benson LQ, Coon MR, Zhu X, Hanash SM, Wechsler DS.

Neoplasia. 2004 Sep-Oct;6(5):660-73.

10.

A novel chromosomal inversion at 11q23 in infant acute myeloid leukemia fuses MLL to CALM, a gene that encodes a clathrin assembly protein.

Wechsler DS, Engstrom LD, Alexander BM, Motto DG, Roulston D.

Genes Chromosomes Cancer. 2003 Jan;36(1):26-36.

11.

Mxi1, a Myc antagonist, suppresses proliferation of DU145 human prostate cells.

Taj MM, Tawil RJ, Engstrom LD, Zeng Z, Hwang C, Sanda MG, Wechsler DS.

Prostate. 2001 May 15;47(3):194-204.

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