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Items: 14

1.

Target Deconvolution of a Multikinase Inhibitor with Antimetastatic Properties Identifies TAOK3 as a Key Contributor to a Cancer Stem Cell-Like Phenotype.

Bian Y, Teper Y, Mathews Griner LA, Aiken TJ, Shukla V, Guha R, Shinn P, Xin HW, Pflicke H, Powers AS, Li D, Jiang JK, Patel P, Rogers SA, Aubé J, Ferrer M, Thomas CJ, Rudloff U.

Mol Cancer Ther. 2019 Nov;18(11):2097-2110. doi: 10.1158/1535-7163.MCT-18-1011. Epub 2019 Aug 8.

PMID:
31395684
2.

Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.

Ramurthy S, Taft BR, Aversa RJ, Barsanti PA, Burger MT, Lou Y, Nishiguchi GA, Rico A, Setti L, Smith A, Subramanian S, Tamez V, Tanner H, Wan L, Hu C, Appleton BA, Mamo M, Tandeske L, Tellew JE, Huang S, Yue Q, Chaudhary A, Tian H, Iyer R, Hassan AQ, Mathews Griner LA, La Bonte LR, Cooke VG, Van Abbema A, Merritt H, Gampa K, Feng F, Yuan J, Mishina Y, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Sellers WR, Lees E, Shao W, Dillon MP, Stuart DD.

J Med Chem. 2020 Mar 12;63(5):2013-2027. doi: 10.1021/acs.jmedchem.9b00161. Epub 2019 May 16.

PMID:
31059256
3.

Mutation Profiles in Glioblastoma 3D Oncospheres Modulate Drug Efficacy.

Wilson KM, Mathews-Griner LA, Williamson T, Guha R, Chen L, Shinn P, McKnight C, Michael S, Klumpp-Thomas C, Binder ZA, Ferrer M, Gallia GL, Thomas CJ, Riggins GJ.

SLAS Technol. 2019 Feb;24(1):28-40. doi: 10.1177/2472630318803749. Epub 2018 Oct 5.

4.

Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF.

Shao W, Mishina YM, Feng Y, Caponigro G, Cooke VG, Rivera S, Wang Y, Shen F, Korn JM, Mathews Griner LA, Nishiguchi G, Rico A, Tellew J, Haling JR, Aversa R, Polyakov V, Zang R, Hekmat-Nejad M, Amiri P, Singh M, Keen N, Dillon MP, Lees E, Ramurthy S, Sellers WR, Stuart DD.

Cancer Res. 2018 Mar 15;78(6):1537-1548. doi: 10.1158/0008-5472.CAN-17-2033. Epub 2018 Jan 17.

5.

Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.

Nishiguchi GA, Rico A, Tanner H, Aversa RJ, Taft BR, Subramanian S, Setti L, Burger MT, Wan L, Tamez V, Smith A, Lou Y, Barsanti PA, Appleton BA, Mamo M, Tandeske L, Dix I, Tellew JE, Huang S, Mathews Griner LA, Cooke VG, Van Abbema A, Merritt H, Ma S, Gampa K, Feng F, Yuan J, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Jansen JM, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Lees E, Shao W, Stuart DD, Dillon MP, Ramurthy S.

J Med Chem. 2017 Jun 22;60(12):4869-4881. doi: 10.1021/acs.jmedchem.6b01862. Epub 2017 Jun 8.

PMID:
28557458
6.

SU9516 Increases α7β1 Integrin and Ameliorates Disease Progression in the mdx Mouse Model of Duchenne Muscular Dystrophy.

Sarathy A, Wuebbles RD, Fontelonga TM, Tarchione AR, Mathews Griner LA, Heredia DJ, Nunes AM, Duan S, Brewer PD, Van Ry T, Hennig GW, Gould TW, Dulcey AE, Wang A, Xu X, Chen CZ, Hu X, Zheng W, Southall N, Ferrer M, Marugan J, Burkin DJ.

Mol Ther. 2017 Jun 7;25(6):1395-1407. doi: 10.1016/j.ymthe.2017.03.022. Epub 2017 Apr 5.

7.

Large-scale pharmacological profiling of 3D tumor models of cancer cells.

Mathews Griner LA, Zhang X, Guha R, McKnight C, Goldlust IS, Lal-Nag M, Wilson K, Michael S, Titus S, Shinn P, Thomas CJ, Ferrer M.

Cell Death Dis. 2016 Dec 1;7(12):e2492. doi: 10.1038/cddis.2016.360.

8.

Ranking Differential Drug Activities from Dose-Response Synthetic Lethality Screens.

Guha R, Mathews Griner LA, Keller JM, Zhang X, Fitzgerald D, Antignani A, Pastan I, Thomas CJ, Ferrer M.

J Biomol Screen. 2016 Oct;21(9):942-55. doi: 10.1177/1087057116644890. Epub 2016 Apr 25.

PMID:
27112173
9.

Aurora B kinase is a potent and selective target in MYCN-driven neuroblastoma.

Bogen D, Wei JS, Azorsa DO, Ormanoglu P, Buehler E, Guha R, Keller JM, Mathews Griner LA, Ferrer M, Song YK, Liao H, Mendoza A, Gryder BE, Sindri S, He J, Wen X, Zhang S, Shern JF, Yohe ME, Taschner-Mandl S, Shohet JM, Thomas CJ, Martin SE, Ambros PF, Khan J.

Oncotarget. 2015 Nov 3;6(34):35247-62. doi: 10.18632/oncotarget.6208.

10.

High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations.

Mott BT, Eastman RT, Guha R, Sherlach KS, Siriwardana A, Shinn P, McKnight C, Michael S, Lacerda-Queiroz N, Patel PR, Khine P, Sun H, Kasbekar M, Aghdam N, Fontaine SD, Liu D, Mierzwa T, Mathews-Griner LA, Ferrer M, Renslo AR, Inglese J, Yuan J, Roepe PD, Su XZ, Thomas CJ.

Sci Rep. 2015 Sep 25;5:13891. doi: 10.1038/srep13891.

11.

Selective targeting of JAK/STAT signaling is potentiated by Bcl-xL blockade in IL-2-dependent adult T-cell leukemia.

Zhang M, Mathews Griner LA, Ju W, Duveau DY, Guha R, Petrus MN, Wen B, Maeda M, Shinn P, Ferrer M, Conlon KD, Bamford RN, O'Shea JJ, Thomas CJ, Waldmann TA.

Proc Natl Acad Sci U S A. 2015 Oct 6;112(40):12480-5. doi: 10.1073/pnas.1516208112. Epub 2015 Sep 22.

12.

Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors.

Ceribelli M, Kelly PN, Shaffer AL, Wright GW, Xiao W, Yang Y, Mathews Griner LA, Guha R, Shinn P, Keller JM, Liu D, Patel PR, Ferrer M, Joshi S, Nerle S, Sandy P, Normant E, Thomas CJ, Staudt LM.

Proc Natl Acad Sci U S A. 2014 Aug 5;111(31):11365-70. doi: 10.1073/pnas.1411701111. Epub 2014 Jul 21.

13.

A high throughput screening assay system for the identification of small molecule inhibitors of gsp.

Bhattacharyya N, Hu X, Chen CZ, Mathews Griner LA, Zheng W, Inglese J, Austin CP, Marugan JJ, Southall N, Neumann S, Northup JK, Ferrer M, Collins MT.

PLoS One. 2014 Mar 25;9(3):e90766. doi: 10.1371/journal.pone.0090766. eCollection 2014.

14.

High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells.

Mathews Griner LA, Guha R, Shinn P, Young RM, Keller JM, Liu D, Goldlust IS, Yasgar A, McKnight C, Boxer MB, Duveau DY, Jiang JK, Michael S, Mierzwa T, Huang W, Walsh MJ, Mott BT, Patel P, Leister W, Maloney DJ, Leclair CA, Rai G, Jadhav A, Peyser BD, Austin CP, Martin SE, Simeonov A, Ferrer M, Staudt LM, Thomas CJ.

Proc Natl Acad Sci U S A. 2014 Feb 11;111(6):2349-54. doi: 10.1073/pnas.1311846111. Epub 2014 Jan 27.

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