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Critical role of ASCT2-mediated amino acid metabolism in promoting leukaemia development and progression.

Ni F, Yu WM, Li Z, Graham DK, Jin L, Kang S, Rossi MR, Li S, Broxmeyer HE, Qu CK.

Nat Metab. 2019 Mar;1(3):390-403. doi: 10.1038/s42255-019-0039-6. Epub 2019 Mar 11.


Data-Driven Construction of Antitumor Agents with Controlled Polypharmacology.

Da C, Zhang D, Stashko M, Vasileiadi E, Parker RE, Minson KA, Huey MG, Huelse JM, Hunter D, Gilbert TSK, Norris-Drouin J, Miley M, Herring LE, Graves LM, DeRyckere D, Earp HS, Graham DK, Frye SV, Wang X, Kireev D.

J Am Chem Soc. 2019 Oct 2;141(39):15700-15709. doi: 10.1021/jacs.9b08660. Epub 2019 Sep 20.


TAM Family Receptor Kinase Inhibition Reverses MDSC-Mediated Suppression and Augments Anti-PD-1 Therapy in Melanoma.

Holtzhausen A, Harris W, Ubil E, Hunter DM, Zhao J, Zhang Y, Zhang D, Liu Q, Wang X, Graham DK, Frye SV, Earp HS.

Cancer Immunol Res. 2019 Oct;7(10):1672-1686. doi: 10.1158/2326-6066.CIR-19-0008. Epub 2019 Aug 26.


The Emerging Role of TYRO3 as a Therapeutic Target in Cancer.

Smart SK, Vasileiadi E, Wang X, DeRyckere D, Graham DK.

Cancers (Basel). 2018 Nov 29;10(12). pii: E474. doi: 10.3390/cancers10120474. Review.


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.


MERTK inhibition alters the PD-1 axis and promotes anti-leukemia immunity.

Lee-Sherick AB, Jacobsen KM, Henry CJ, Huey MG, Parker RE, Page LS, Hill AA, Wang X, Frye SV, Earp HS, Jordan CT, DeRyckere D, Graham DK.

JCI Insight. 2018 Nov 2;3(21). pii: 97941. doi: 10.1172/jci.insight.97941.


Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.

Zhao J, Zhang D, Zhang W, Stashko MA, DeRyckere D, Vasileiadi E, Parker RE, Hunter D, Liu Q, Zhang Y, Norris-Drouin J, Li B, Drewry DH, Kireev D, Graham DK, Earp HS, Frye SV, Wang X.

J Med Chem. 2018 Nov 21;61(22):10242-10254. doi: 10.1021/acs.jmedchem.8b01229. Epub 2018 Nov 5.


MERTK Promotes Resistance to Irreversible EGFR Tyrosine Kinase Inhibitors in Non-small Cell Lung Cancers Expressing Wild-type EGFR Family Members.

Yan D, Parker RE, Wang X, Frye SV, Earp HS 3rd, DeRyckere D, Graham DK.

Clin Cancer Res. 2018 Dec 15;24(24):6523-6535. doi: 10.1158/1078-0432.CCR-18-0040. Epub 2018 Sep 7.


MERTK Mediates Intrinsic and Adaptive Resistance to AXL-targeting Agents.

McDaniel NK, Cummings CT, Iida M, Hülse J, Pearson HE, Vasileiadi E, Parker RE, Orbuch RA, Ondracek OJ, Welke NB, Kang GH, Davies KD, Wang X, Frye SV, Earp HS, Harari PM, Kimple RJ, DeRyckere D, Graham DK, Wheeler DL.

Mol Cancer Ther. 2018 Nov;17(11):2297-2308. doi: 10.1158/1535-7163.MCT-17-1239. Epub 2018 Aug 9.


GAS6/TAM Pathway Signaling in Hemostasis and Thrombosis.

Law LA, Graham DK, Di Paola J, Branchford BR.

Front Med (Lausanne). 2018 May 9;5:137. doi: 10.3389/fmed.2018.00137. eCollection 2018. Review.


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.


Animals can assign novel odours to a known category.

Wright HF, Wilkinson A, Croxton RS, Graham DK, Harding RC, Hodkinson HL, Keep B, Cracknell NR, Zulch HE.

Sci Rep. 2017 Aug 21;7(1):9019. doi: 10.1038/s41598-017-09454-0.


The Current State of FLT3 Inhibition in Acute Myeloid Leukemia - Pitfalls and Promises.

Minson KA, DeRyckere D, Graham DK.

J Cell Signal. 2017;2(4). pii: 1000166. doi: 10.4172/2576-1471.1000166. Epub 2017 Oct 16. No abstract available.


Discovery of Macrocyclic Pyrimidines as MerTK-Specific Inhibitors.

McIver AL, Zhang W, Liu Q, Jiang X, Stashko MA, Nichols J, Miley MJ, Norris-Drouin J, Machius M, DeRyckere D, Wood E, Graham DK, Earp HS, Kireev D, Frye SV, Wang X.

ChemMedChem. 2017 Feb 3;12(3):207-213. doi: 10.1002/cmdc.201600589. Epub 2017 Jan 9.


Design and Synthesis of Novel Macrocyclic Mer Tyrosine Kinase Inhibitors.

Wang X, Liu J, Zhang W, Stashko MA, Nichols J, Miley MJ, Norris-Drouin J, Chen Z, Machius M, DeRyckere D, Wood E, Graham DK, Earp HS, Kireev D, Frye SV.

ACS Med Chem Lett. 2016 Sep 13;7(12):1044-1049. eCollection 2016 Dec 8.


Targeting the TAM Receptors in Leukemia.

Huey MG, Minson KA, Earp HS, DeRyckere D, Graham DK.

Cancers (Basel). 2016 Nov 8;8(11). pii: E101. Review.


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.


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.


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. 2016 Dec 1;35(48):6270. doi: 10.1038/onc.2016.295. Epub 2016 Sep 5. No abstract available.


The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia.

Minson KA, Smith CC, DeRyckere D, Libbrecht C, Lee-Sherick AB, Huey MG, Lasater EA, Kirkpatrick GD, Stashko MA, Zhang W, Jordan CT, Kireev D, Wang X, Frye SV, Earp HS, Shah NP, Graham DK.

JCI Insight. 2016 Mar;1(3):e85630. doi: 10.1172/jci.insight.85630.


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.


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.


The TAM family: phosphatidylserine sensing receptor tyrosine kinases gone awry in cancer.

Graham DK, DeRyckere D, Davies KD, Earp HS.

Nat Rev Cancer. 2014 Dec;14(12):769-85. doi: 10.1038/nrc3847. Review.


Tyrosine kinase inhibition in leukemia induces an altered metabolic state sensitive to mitochondrial perturbations.

Alvarez-Calderon F, Gregory MA, Pham-Danis C, DeRyckere D, Stevens BM, Zaberezhnyy V, Hill AA, Gemta L, Kumar A, Kumar V, Wempe MF, Pollyea DA, Jordan CT, Serkova NJ, Graham DK, DeGregori J.

Clin Cancer Res. 2015 Mar 15;21(6):1360-72. doi: 10.1158/1078-0432.CCR-14-2146. Epub 2014 Dec 29.


Mer590, a novel monoclonal antibody targeting MER receptor tyrosine kinase, decreases colony formation and increases chemosensitivity in non-small cell lung cancer.

Cummings CT, Linger RM, Cohen RA, Sather S, Kirkpatrick GD, Davies KD, DeRyckere D, Earp HS, Graham DK.

Oncotarget. 2014 Nov 15;5(21):10434-45.


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.


Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis.

Zhang W, McIver AL, Stashko MA, DeRyckere D, Branchford BR, Hunter D, Kireev D, Miley MJ, Norris-Drouin J, Stewart WM, Lee M, Sather S, Zhou Y, Di Paola JA, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X.

J Med Chem. 2013 Dec 12;56(23):9693-700. doi: 10.1021/jm4013888. Epub 2013 Nov 20.


Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors.

Zhang W, Zhang D, Stashko MA, DeRyckere D, Hunter D, Kireev D, Miley MJ, Cummings C, Lee M, Norris-Drouin J, Stewart WM, Sather S, Zhou Y, Kirkpatrick G, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X.

J Med Chem. 2013 Dec 12;56(23):9683-92. doi: 10.1021/jm401387j. Epub 2013 Nov 20. Erratum in: J Med Chem. 2014 Aug 28;57(16):7141.


Pre-clinical evaluation of tyrosine kinase inhibitors for treatment of acute leukemia.

Christoph S, Lee-Sherick AB, Sather S, DeRyckere D, Graham DK.

J Vis Exp. 2013 Sep 18;(79):e50720. doi: 10.3791/50720.


UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo.

Christoph S, Deryckere D, Schlegel J, Frazer JK, Batchelor LA, Trakhimets AY, Sather S, Hunter DM, Cummings CT, Liu J, Yang C, Kireev D, Simpson C, Norris-Drouin J, Hull-Ryde EA, Janzen WP, Johnson GL, Wang X, Frye SV, Earp HS 3rd, Graham DK.

Mol Cancer Ther. 2013 Nov;12(11):2367-77. doi: 10.1158/1535-7163.MCT-13-0040. Epub 2013 Aug 30.


MerTK inhibition in tumor leukocytes decreases tumor growth and metastasis.

Cook RS, Jacobsen KM, Wofford AM, DeRyckere D, Stanford J, Prieto AL, Redente E, Sandahl M, Hunter DM, Strunk KE, Graham DK, Earp HS 3rd.

J Clin Invest. 2013 Aug;123(8):3231-42. doi: 10.1172/JCI67655. Epub 2013 Jul 8.


Mer receptor tyrosine kinase is a therapeutic target in pre-B-cell acute lymphoblastic leukemia.

Linger RM, Lee-Sherick AB, DeRyckere D, Cohen RA, Jacobsen KM, McGranahan A, Brandão LN, Winges A, Sawczyn KK, Liang X, Keating AK, Tan AC, Earp HS, Graham DK.

Blood. 2013 Aug 29;122(9):1599-609. doi: 10.1182/blood-2013-01-478156. Epub 2013 Jul 16.


Molecular pathways: MERTK signaling in cancer.

Cummings CT, Deryckere D, Earp HS, Graham DK.

Clin Cancer Res. 2013 Oct 1;19(19):5275-80. doi: 10.1158/1078-0432.CCR-12-1451. Epub 2013 Jul 5. Review.


UNC1062, a new and potent Mer inhibitor.

Liu J, Zhang W, Stashko MA, Deryckere D, Cummings CT, Hunter D, Yang C, Jayakody CN, Cheng N, Simpson C, Norris-Drouin J, Sather S, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X.

Eur J Med Chem. 2013 Jul;65:83-93. doi: 10.1016/j.ejmech.2013.03.035. Epub 2013 Apr 2.


Dual ALK and MYC rearrangements leading to an aggressive variant of anaplastic large cell lymphoma.

Liang X, Branchford B, Greffe B, McGavran L, Carstens B, Meltesen L, Albano EA, Quinones R, Cook B, Graham DK.

J Pediatr Hematol Oncol. 2013 Jul;35(5):e209-13. doi: 10.1097/MPH.0b013e3182815046.


MERTK receptor tyrosine kinase is a therapeutic target in melanoma.

Schlegel J, Sambade MJ, Sather S, Moschos SJ, Tan AC, Winges A, DeRyckere D, Carson CC, Trembath DG, Tentler JJ, Eckhardt SG, Kuan PF, Hamilton RL, Duncan LM, Miller CR, Nikolaishvili-Feinberg N, Midkiff BR, Liu J, Zhang W, Yang C, Wang X, Frye SV, Earp HS, Shields JM, Graham DK.

J Clin Invest. 2013 May;123(5):2257-67. doi: 10.1172/JCI67816. Epub 2013 Apr 15.


A mechanism of resistance to gefitinib mediated by cellular reprogramming and the acquisition of an FGF2-FGFR1 autocrine growth loop.

Ware KE, Hinz TK, Kleczko E, Singleton KR, Marek LA, Helfrich BA, Cummings CT, Graham DK, Astling D, Tan AC, Heasley LE.

Oncogenesis. 2013 Mar 25;2:e39. doi: 10.1038/oncsis.2013.4.


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.


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.


Bioluminescence imaging of leukemia cell lines in vitro and in mouse xenografts: effects of monoclonal and polyclonal cell populations on intensity and kinetics of photon emission.

Christoph S, Schlegel J, Alvarez-Calderon F, Kim YM, Brandao LN, DeRyckere D, Graham DK.

J Hematol Oncol. 2013 Jan 23;6:10. doi: 10.1186/1756-8722-6-10.


Moderate aplastic anemia in children: preliminary outcomes for treatment versus observation from a single-institutional experience.

Brock K, Goldenberg N, Graham DK, Liang X, Hays T.

J Pediatr Hematol Oncol. 2013 Mar;35(2):148-52. doi: 10.1097/MPH.0b013e3182755f36.


Mer or Axl receptor tyrosine kinase inhibition promotes apoptosis, blocks growth and enhances chemosensitivity of human non-small cell lung cancer.

Linger RM, Cohen RA, Cummings CT, Sather S, Migdall-Wilson J, Middleton DH, Lu X, Barón AE, Franklin WA, Merrick DT, Jedlicka P, DeRyckere D, Heasley LE, Graham DK.

Oncogene. 2013 Jul 18;32(29):3420-31. doi: 10.1038/onc.2012.355. Epub 2012 Aug 13.


Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.

Liu J, Yang C, Simpson C, Deryckere D, Van Deusen A, Miley MJ, Kireev D, Norris-Drouin J, Sather S, Hunter D, Korboukh VK, Patel HS, Janzen WP, Machius M, Johnson GL, Earp HS, Graham DK, Frye SV, Wang X.

ACS Med Chem Lett. 2012 Feb 9;3(2):129-134.


Prolonged exposure to a Mer ligand in leukemia: Gas6 favors expression of a partial Mer glycoform and reveals a novel role for Mer in the nucleus.

Migdall-Wilson J, Bates C, Schlegel J, Brandão L, Linger RM, DeRyckere D, Graham DK.

PLoS One. 2012;7(2):e31635. doi: 10.1371/journal.pone.0031635. Epub 2012 Feb 20.


Mer receptor tyrosine kinase inhibition impedes glioblastoma multiforme migration and alters cellular morphology.

Rogers AE, Le JP, Sather S, Pernu BM, Graham DK, Pierce AM, Keating AK.

Oncogene. 2012 Sep 20;31(38):4171-81. doi: 10.1038/onc.2011.588. Epub 2011 Dec 19.


TAM receptors in leukemia: expression, signaling, and therapeutic implications.

Brandão L, Migdall-Wilson J, Eisenman K, Graham DK.

Crit Rev Oncog. 2011;16(1-2):47-63.


Constitutive induction of pro-inflammatory and chemotactic cytokines in cystathionine beta-synthase deficient homocystinuria.

Keating AK, Freehauf C, Jiang H, Brodsky GL, Stabler SP, Allen RH, Graham DK, Thomas JA, Van Hove JL, Maclean KN.

Mol Genet Metab. 2011 Aug;103(4):330-7. doi: 10.1016/j.ymgme.2011.04.012. Epub 2011 May 5.


Targeting paediatric acute lymphoblastic leukaemia: novel therapies currently in development.

Lee-Sherick AB, Linger RM, Gore L, Keating AK, Graham DK.

Br J Haematol. 2010 Nov;151(4):295-311. doi: 10.1111/j.1365-2141.2010.08282.x. Epub 2010 Aug 31. Review.


Taking aim at Mer and Axl receptor tyrosine kinases as novel therapeutic targets in solid tumors.

Linger RM, Keating AK, Earp HS, Graham DK.

Expert Opin Ther Targets. 2010 Oct;14(10):1073-90. doi: 10.1517/14728222.2010.515980. Review.


Inhibition of Mer and Axl receptor tyrosine kinases in astrocytoma cells leads to increased apoptosis and improved chemosensitivity.

Keating AK, Kim GK, Jones AE, Donson AM, Ware K, Mulcahy JM, Salzberg DB, Foreman NK, Liang X, Thorburn A, Graham DK.

Mol Cancer Ther. 2010 May;9(5):1298-307. doi: 10.1158/1535-7163.MCT-09-0707. Epub 2010 Apr 27.

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