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Items: 1 to 20 of 120

1.

Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.

De Clercq DJH, Heppner DE, To C, Jang J, Park E, Yun CH, Mushajiang M, Shin BH, Gero TW, Scott DA, Jänne PA, Eck MJ, Gray NS.

ACS Med Chem Lett. 2019 Oct 22;10(11):1549-1553. doi: 10.1021/acsmedchemlett.9b00381. eCollection 2019 Nov 14.

PMID:
31749909
2.

Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes.

Park E, Rawson S, Li K, Kim BW, Ficarro SB, Pino GG, Sharif H, Marto JA, Jeon H, Eck MJ.

Nature. 2019 Nov;575(7783):545-550. doi: 10.1038/s41586-019-1660-y. Epub 2019 Oct 3.

PMID:
31581174
3.

A driving test for oncogenic mutations.

Heppner DE, Beyett TS, Eck MJ.

J Biol Chem. 2019 Jun 14;294(24):9390-9391. doi: 10.1074/jbc.H119.009452.

4.

Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor.

To C, Jang J, Chen T, Park E, Mushajiang M, De Clercq DJH, Xu M, Wang S, Cameron MD, Heppner DE, Shin BH, Gero TW, Yang A, Dahlberg SE, Wong KK, Eck MJ, Gray NS, Jänne PA.

Cancer Discov. 2019 Jul;9(7):926-943. doi: 10.1158/2159-8290.CD-18-0903. Epub 2019 May 15.

PMID:
31092401
5.

Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.

McNally R, Li Q, Li K, Dekker C, Vangrevelinghe E, Jones M, Chène P, Machauer R, Radimerski T, Eck MJ.

ACS Chem Biol. 2019 Apr 19;14(4):587-593. doi: 10.1021/acschembio.8b00722. Epub 2019 Mar 11.

PMID:
30763067
6.

Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor.

Jang J, Son J, Park E, Kosaka T, Saxon JA, De Clercq DJH, Choi HG, Tanizaki J, Eck MJ, Jänne PA, Gray NS.

Angew Chem Int Ed Engl. 2018 Sep 3;57(36):11629-11633. doi: 10.1002/anie.201805187. Epub 2018 Aug 3.

7.

Correction: MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells.

Wang Y, Li YM, Baitsch L, Huang A, Xiang Y, Tong H, Lako A, Von T, Choi C, Lim E, Min J, Li L, Stegmeier F, Schlegel R, Eck MJ, Gray NS, Mitchison TJ, Zhao JJ.

Elife. 2018 Mar 12;7. pii: e36414. doi: 10.7554/eLife.36414. No abstract available.

8.

MELK is not necessary for the proliferation of basal-like breast cancer cells.

Huang HT, Seo HS, Zhang T, Wang Y, Jiang B, Li Q, Buckley DL, Nabet B, Roberts JM, Paulk J, Dastjerdi S, Winter GE, McLauchlan H, Moran J, Bradner JE, Eck MJ, Dhe-Paganon S, Zhao JJ, Gray NS.

Elife. 2017 Sep 19;6. pii: e26693. doi: 10.7554/eLife.26693.

9.

Crystal Structure of Leiomodin 2 in Complex with Actin: A Structural and Functional Reexamination.

Boczkowska M, Yurtsever Z, Rebowski G, Eck MJ, Dominguez R.

Biophys J. 2017 Aug 22;113(4):889-899. doi: 10.1016/j.bpj.2017.07.007.

10.

CRKL Mediates p110β-Dependent PI3K Signaling in PTEN-Deficient Cancer Cells.

Zhang J, Gao X, Schmit F, Adelmant G, Eck MJ, Marto JA, Zhao JJ, Roberts TM.

Cell Rep. 2017 Jul 18;20(3):549-557. doi: 10.1016/j.celrep.2017.06.054.

11.

Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors.

Kosaka T, Tanizaki J, Paranal RM, Endoh H, Lydon C, Capelletti M, Repellin CE, Choi J, Ogino A, Calles A, Ercan D, Redig AJ, Bahcall M, Oxnard GR, Eck MJ, Jänne PA.

Cancer Res. 2017 May 15;77(10):2712-2721. doi: 10.1158/0008-5472.CAN-16-3404. Epub 2017 Mar 31.

12.

Domain-dependent effects of insulin and IGF-1 receptors on signalling and gene expression.

Cai W, Sakaguchi M, Kleinridders A, Gonzalez-Del Pino G, Dreyfuss JM, O'Neill BT, Ramirez AK, Pan H, Winnay JN, Boucher J, Eck MJ, Kahn CR.

Nat Commun. 2017 Mar 27;8:14892. doi: 10.1038/ncomms14892.

13.

Leveraging Gas-Phase Fragmentation Pathways for Improved Identification and Selective Detection of Targets Modified by Covalent Probes.

Ficarro SB, Browne CM, Card JD, Alexander WM, Zhang T, Park E, McNally R, Dhe-Paganon S, Seo HS, Lamberto I, Eck MJ, Buhrlage SJ, Gray NS, Marto JA.

Anal Chem. 2016 Dec 20;88(24):12248-12254. doi: 10.1021/acs.analchem.6b03394. Epub 2016 Nov 30.

PMID:
28193034
14.

Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival.

Wang Y, Begley M, Li Q, Huang HT, Lako A, Eck MJ, Gray NS, Mitchison TJ, Cantley LC, Zhao JJ.

Proc Natl Acad Sci U S A. 2016 Aug 30;113(35):9810-5. doi: 10.1073/pnas.1606862113. Epub 2016 Aug 15.

15.

Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors.

Jia Y, Yun CH, Park E, Ercan D, Manuia M, Juarez J, Xu C, Rhee K, Chen T, Zhang H, Palakurthi S, Jang J, Lelais G, DiDonato M, Bursulaya B, Michellys PY, Epple R, Marsilje TH, McNeill M, Lu W, Harris J, Bender S, Wong KK, Jänne PA, Eck MJ.

Nature. 2016 Jun 2;534(7605):129-32. doi: 10.1038/nature17960. Epub 2016 May 25.

16.

Crystal Structure of the FERM-SH2 Module of Human Jak2.

McNally R, Toms AV, Eck MJ.

PLoS One. 2016 May 26;11(5):e0156218. doi: 10.1371/journal.pone.0156218. eCollection 2016.

17.

Data publication with the structural biology data grid supports live analysis.

Meyer PA, Socias S, Key J, Ransey E, Tjon EC, Buschiazzo A, Lei M, Botka C, Withrow J, Neau D, Rajashankar K, Anderson KS, Baxter RH, Blacklow SC, Boggon TJ, Bonvin AM, Borek D, Brett TJ, Caflisch A, Chang CI, Chazin WJ, Corbett KD, Cosgrove MS, Crosson S, Dhe-Paganon S, Di Cera E, Drennan CL, Eck MJ, Eichman BF, Fan QR, Ferré-D'Amaré AR, Fromme JC, Garcia KC, Gaudet R, Gong P, Harrison SC, Heldwein EE, Jia Z, Keenan RJ, Kruse AC, Kvansakul M, McLellan JS, Modis Y, Nam Y, Otwinowski Z, Pai EF, Pereira PJ, Petosa C, Raman CS, Rapoport TA, Roll-Mecak A, Rosen MK, Rudenko G, Schlessinger J, Schwartz TU, Shamoo Y, Sondermann H, Tao YJ, Tolia NH, Tsodikov OV, Westover KD, Wu H, Foster I, Fraser JS, Maia FR, Gonen T, Kirchhausen T, Diederichs K, Crosas M, Sliz P.

Nat Commun. 2016 Mar 7;7:10882. doi: 10.1038/ncomms10882.

18.

SPLINTS: small-molecule protein ligand interface stabilizers.

Fischer ES, Park E, Eck MJ, Thomä NH.

Curr Opin Struct Biol. 2016 Apr;37:115-22. doi: 10.1016/j.sbi.2016.01.004. Epub 2016 Jan 30. Review.

19.

EGF-receptor specificity for phosphotyrosine-primed substrates provides signal integration with Src.

Begley MJ, Yun CH, Gewinner CA, Asara JM, Johnson JL, Coyle AJ, Eck MJ, Apostolou I, Cantley LC.

Nat Struct Mol Biol. 2015 Dec;22(12):983-90. doi: 10.1038/nsmb.3117. Epub 2015 Nov 9.

20.

Structure and mechanism of activity-based inhibition of the EGF receptor by Mig6.

Park E, Kim N, Ficarro SB, Zhang Y, Lee BI, Cho A, Kim K, Park AKJ, Park WY, Murray B, Meyerson M, Beroukhim R, Marto JA, Cho J, Eck MJ.

Nat Struct Mol Biol. 2015 Sep;22(9):703-711. doi: 10.1038/nsmb.3074. Epub 2015 Aug 17.

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