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Items: 1 to 20 of 132

1.

UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with Methotrexate in Leukemia Models.

DeRyckere D, Lee-Sherick AB, Huey MG, Hill AA, Tyner JW, Jacobsen KM, Page LS, Kirkpatrick GG, Eryildiz F, Montgomery SA, Zhang W, Wang X, Frye SV, Earp HS, Graham DK.

Clin Cancer Res. 2017 Mar 15;23(6):1481-1492. doi: 10.1158/1078-0432.CCR-16-1330. Epub 2016 Sep 20. Erratum in: Clin Cancer Res. 2017 Jul 15;23 (14 ):3971-3972.

2.

The small-molecule MERTK inhibitor UNC2025 decreases platelet activation and prevents thrombosis.

Branchford BR, Stalker TJ, Law L, Acevedo G, Sather S, Brzezinski C, Wilson KM, Minson K, Lee-Sherick AB, Davizon-Castillo P, Ng C, Zhang W, Neeves KB, Lentz SR, Wang X, Frye SV, Shelton Earp H 3rd, DeRyckere D, Brass LF, Graham DK, Di Paola JA.

J Thromb Haemost. 2018 Feb;16(2):352-363. doi: 10.1111/jth.13875. Epub 2018 Jan 12.

3.

MerTK as a therapeutic target in glioblastoma.

Wu J, Frady LN, Bash RE, Cohen SM, Schorzman AN, Su YT, Irvin DM, Zamboni WC, Wang X, Frye SV, Ewend MG, Sulman EP, Gilbert MR, Earp HS, Miller CR.

Neuro Oncol. 2018 Jan 10;20(1):92-102. doi: 10.1093/neuonc/nox111.

4.

Small Molecule Inhibition of MERTK Is Efficacious in Non-Small Cell Lung Cancer Models Independent of Driver Oncogene Status.

Cummings CT, Zhang W, Davies KD, Kirkpatrick GD, Zhang D, DeRyckere D, Wang X, Frye SV, Earp HS, Graham DK.

Mol Cancer Ther. 2015 Sep;14(9):2014-22. doi: 10.1158/1535-7163.MCT-15-0116. Epub 2015 Jul 10.

5.

MERTK Inhibition Induces Polyploidy and Promotes Cell Death and Cellular Senescence in Glioblastoma Multiforme.

Sufit A, Lee-Sherick AB, DeRyckere D, Rupji M, Dwivedi B, Varella-Garcia M, Pierce AM, Kowalski J, Wang X, Frye SV, Earp HS, Keating AK, Graham DK.

PLoS One. 2016 Oct 26;11(10):e0165107. doi: 10.1371/journal.pone.0165107. eCollection 2016.

6.

Effects of MERTK Inhibitors UNC569 and UNC1062 on the Growth of Acute Myeloid Leukaemia Cells.

Koda Y, Itoh M, Tohda S.

Anticancer Res. 2018 Jan;38(1):199-204.

PMID:
29277773
7.

Inhibition of MERTK Promotes Suppression of Tumor Growth in BRAF Mutant and BRAF Wild-Type Melanoma.

Sinik L, Minson KA, Tentler JJ, Carrico J, Bagby SM, Robinson WA, Kami R, Burstyn-Cohen T, Eckhardt SG, Wang X, Frye SV, Earp HS, DeRyckere D, Graham DK.

Mol Cancer Ther. 2019 Feb;18(2):278-288. doi: 10.1158/1535-7163.MCT-18-0456. Epub 2018 Nov 27.

PMID:
30482852
8.

Activity of the multikinase inhibitor sorafenib in combination with cytarabine in acute myeloid leukemia.

Hu S, Niu H, Inaba H, Orwick S, Rose C, Panetta JC, Yang S, Pounds S, Fan Y, Calabrese C, Rehg JE, Campana D, Rubnitz JE, Baker SD.

J Natl Cancer Inst. 2011 Jun 8;103(11):893-905. doi: 10.1093/jnci/djr107. Epub 2011 Apr 12.

9.

UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.

Zhang W, DeRyckere D, Hunter D, Liu J, Stashko MA, Minson KA, Cummings CT, Lee M, Glaros TG, Newton DL, Sather S, Zhang D, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X.

J Med Chem. 2014 Aug 28;57(16):7031-41. doi: 10.1021/jm500749d. Epub 2014 Aug 6.

10.

Antileukemic Activity of 2-Deoxy-d-Glucose through Inhibition of N-Linked Glycosylation in Acute Myeloid Leukemia with FLT3-ITD or c-KIT Mutations.

Larrue C, Saland E, Vergez F, Serhan N, Delabesse E, Mansat-De Mas V, Hospital MA, Tamburini J, Manenti S, Sarry JE, Récher C.

Mol Cancer Ther. 2015 Oct;14(10):2364-73. doi: 10.1158/1535-7163.MCT-15-0163. Epub 2015 Jul 23.

11.

Efficacy of a Mer and Flt3 tyrosine kinase small molecule inhibitor, UNC1666, in acute myeloid leukemia.

Lee-Sherick AB, Zhang W, Menachof KK, Hill AA, Rinella S, Kirkpatrick G, Page LS, Stashko MA, Jordan CT, Wei Q, Liu J, Zhang D, DeRyckere D, Wang X, Frye S, Earp HS, Graham DK.

Oncotarget. 2015 Mar 30;6(9):6722-36.

12.

Targeting sphingosine kinase 1 induces MCL1-dependent cell death in acute myeloid leukemia.

Powell JA, Lewis AC, Zhu W, Toubia J, Pitman MR, Wallington-Beddoe CT, Moretti PA, Iarossi D, Samaraweera SE, Cummings N, Ramshaw HS, Thomas D, Wei AH, Lopez AF, D'Andrea RJ, Lewis ID, Pitson SM.

Blood. 2017 Feb 9;129(6):771-782. doi: 10.1182/blood-2016-06-720433. Epub 2016 Dec 12.

13.

Inhibition of Wild-Type p53-Expressing AML by the Novel Small Molecule HDM2 Inhibitor CGM097.

Weisberg E, Halilovic E, Cooke VG, Nonami A, Ren T, Sanda T, Simkin I, Yuan J, Antonakos B, Barys L, Ito M, Stone R, Galinsky I, Cowens K, Nelson E, Sattler M, Jeay S, Wuerthner JU, McDonough SM, Wiesmann M, Griffin JD.

Mol Cancer Ther. 2015 Oct;14(10):2249-59. doi: 10.1158/1535-7163.MCT-15-0429. Epub 2015 Jul 23.

14.

Selective Inhibitors of Histone Deacetylases 1 and 2 Synergize with Azacitidine in Acute Myeloid Leukemia.

Min C, Moore N, Shearstone JR, Quayle SN, Huang P, van Duzer JH, Jarpe MB, Jones SS, Yang M.

PLoS One. 2017 Jan 6;12(1):e0169128. doi: 10.1371/journal.pone.0169128. eCollection 2017.

15.

Inhibition of MerTK increases chemosensitivity and decreases oncogenic potential in T-cell acute lymphoblastic leukemia.

Brandao LN, Winges A, Christoph S, Sather S, Migdall-Wilson J, Schlegel J, McGranahan A, Gao D, Liang X, Deryckere D, Graham DK.

Blood Cancer J. 2013 Jan 25;3:e101. doi: 10.1038/bcj.2012.46.

16.

Silvestrol exhibits significant in vivo and in vitro antileukemic activities and inhibits FLT3 and miR-155 expressions in acute myeloid leukemia.

Alachkar H, Santhanam R, Harb JG, Lucas DM, Oaks JJ, Hickey CJ, Pan L, Kinghorn AD, Caligiuri MA, Perrotti D, Byrd JC, Garzon R, Grever MR, Marcucci G.

J Hematol Oncol. 2013 Mar 16;6:21. doi: 10.1186/1756-8722-6-21.

17.

Aberrant Mer receptor tyrosine kinase expression contributes to leukemogenesis in acute myeloid leukemia.

Lee-Sherick AB, Eisenman KM, Sather S, McGranahan A, Armistead PM, McGary CS, Hunsucker SA, Schlegel J, Martinson H, Cannon C, Keating AK, Earp HS, Liang X, DeRyckere D, Graham DK.

Oncogene. 2013 Nov 14;32(46):5359-68. doi: 10.1038/onc.2013.40. Epub 2013 Mar 11. Erratum in: Oncogene. 2016 Dec 1;35(48):6270.

18.

Activity of the hypoxia-activated prodrug, TH-302, in preclinical human acute myeloid leukemia models.

Portwood S, Lal D, Hsu YC, Vargas R, Johnson MK, Wetzler M, Hart CP, Wang ES.

Clin Cancer Res. 2013 Dec 1;19(23):6506-19. doi: 10.1158/1078-0432.CCR-13-0674. Epub 2013 Oct 2.

19.

Mutant FLT3: a direct target of sorafenib in acute myelogenous leukemia.

Zhang W, Konopleva M, Shi YX, McQueen T, Harris D, Ling X, Estrov Z, Quintás-Cardama A, Small D, Cortes J, Andreeff M.

J Natl Cancer Inst. 2008 Feb 6;100(3):184-98. doi: 10.1093/jnci/djm328. Epub 2008 Jan 29.

PMID:
18230792
20.

Targeting the leukemia microenvironment by CXCR4 inhibition overcomes resistance to kinase inhibitors and chemotherapy in AML.

Zeng Z, Shi YX, Samudio IJ, Wang RY, Ling X, Frolova O, Levis M, Rubin JB, Negrin RR, Estey EH, Konoplev S, Andreeff M, Konopleva M.

Blood. 2009 Jun 11;113(24):6215-24. doi: 10.1182/blood-2008-05-158311. Epub 2008 Oct 27.

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