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Items: 12

1.

BET bromodomain inhibition cooperates with PD-1 blockade to facilitate antitumor response in Kras-mutant non-small cell lung cancer.

Adeegbe DO, Liu S, Hattersley M, Bowden M, Zhou CW, Li S, Vlahos R, Grondine M, Dolgalev I, Ivanova E, Quinn MM, Gao P, Hammerman PS, Bradner JE, Diehl JA, Rustgi AK, Bass AJ, Tsirigos A, Freeman GJ, Chen H, Wong KK.

Cancer Immunol Res. 2018 Aug 7. pii: canimm.0077.2018. doi: 10.1158/2326-6066.CIR-18-0077. [Epub ahead of print]

PMID:
30087114
2.

Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.

Yang B, Vasbinder MM, Hird AW, Su Q, Wang H, Yu Y, Toader D, Lyne PD, Read JA, Breed J, Ioannidis S, Deng C, Grondine M, DeGrace N, Whitston D, Brassil P, Janetka JW.

J Med Chem. 2018 Feb 8;61(3):1061-1073. doi: 10.1021/acs.jmedchem.7b01490. Epub 2018 Jan 19.

PMID:
29301085
3.

Generation of stable PDX derived cell lines using conditional reprogramming.

Borodovsky A, McQuiston TJ, Stetson D, Ahmed A, Whitston D, Zhang J, Grondine M, Lawson D, Challberg SS, Zinda M, Pollok BA, Dougherty BA, D'Cruz CM.

Mol Cancer. 2017 Dec 6;16(1):177. doi: 10.1186/s12943-017-0745-1.

4.

Sensitivity to PI3K and AKT inhibitors is mediated by divergent molecular mechanisms in subtypes of DLBCL.

Erdmann T, Klener P, Lynch JT, Grau M, Vočková P, Molinsky J, Tuskova D, Hudson K, Polanska UM, Grondine M, Mayo M, Dai B, Pfeifer M, Erdmann K, Schwammbach D, Zapukhlyak M, Staiger AM, Ott G, Berdel WE, Davies BR, Cruzalegui F, Trneny M, Lenz P, Barry ST, Lenz G.

Blood. 2017 Jul 20;130(3):310-322. doi: 10.1182/blood-2016-12-758599. Epub 2017 Feb 15.

5.

AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules.

Guichard SM, Curwen J, Bihani T, D'Cruz CM, Yates JW, Grondine M, Howard Z, Davies BR, Bigley G, Klinowska T, Pike KG, Pass M, Chresta CM, Polanska UM, McEwen R, Delpuech O, Green S, Cosulich SC.

Mol Cancer Ther. 2015 Nov;14(11):2508-18. doi: 10.1158/1535-7163.MCT-15-0365. Epub 2015 Sep 10.

6.

AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia.

Keeton EK, McEachern K, Dillman KS, Palakurthi S, Cao Y, Grondine MR, Kaur S, Wang S, Chen Y, Wu A, Shen M, Gibbons FD, Lamb ML, Zheng X, Stone RM, Deangelo DJ, Platanias LC, Dakin LA, Chen H, Lyne PD, Huszar D.

Blood. 2014 Feb 6;123(6):905-13. doi: 10.1182/blood-2013-04-495366. Epub 2013 Dec 20.

7.

Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.

Vasbinder MM, Aquila B, Augustin M, Chen H, Cheung T, Cook D, Drew L, Fauber BP, Glossop S, Grondine M, Hennessy E, Johannes J, Lee S, Lyne P, Mörtl M, Omer C, Palakurthi S, Pontz T, Read J, Sha L, Shen M, Steinbacher S, Wang H, Wu A, Ye M.

J Med Chem. 2013 Mar 14;56(5):1996-2015. doi: 10.1021/jm301658d. Epub 2013 Feb 27.

PMID:
23398453
8.

Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.

Oza V, Ashwell S, Almeida L, Brassil P, Breed J, Deng C, Gero T, Grondine M, Horn C, Ioannidis S, Liu D, Lyne P, Newcombe N, Pass M, Read J, Ready S, Rowsell S, Su M, Toader D, Vasbinder M, Yu D, Yu Y, Xue Y, Zabludoff S, Janetka J.

J Med Chem. 2012 Jun 14;55(11):5130-42. doi: 10.1021/jm300025r. Epub 2012 Jun 4.

PMID:
22551018
9.

Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.

Oza V, Ashwell S, Brassil P, Breed J, Ezhuthachan J, Deng C, Grondine M, Horn C, Liu D, Lyne P, Newcombe N, Pass M, Read J, Su M, Toader D, Yu D, Yu Y, Zabludoff S.

Bioorg Med Chem Lett. 2012 Mar 15;22(6):2330-7. doi: 10.1016/j.bmcl.2012.01.043. Epub 2012 Feb 1.

PMID:
22342147
10.

Avoidance of the Ames test liability for aryl-amines via computation.

McCarren P, Bebernitz GR, Gedeck P, Glowienke S, Grondine MS, Kirman LC, Klickstein J, Schuster HF, Whitehead L.

Bioorg Med Chem. 2011 May 15;19(10):3173-82. doi: 10.1016/j.bmc.2011.03.066. Epub 2011 Apr 3.

PMID:
21524589
11.

Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes.

Bebernitz GR, Beaulieu V, Dale BA, Deacon R, Duttaroy A, Gao J, Grondine MS, Gupta RC, Kakmak M, Kavana M, Kirman LC, Liang J, Maniara WM, Munshi S, Nadkarni SS, Schuster HF, Stams T, St Denny I, Taslimi PM, Vash B, Caplan SL.

J Med Chem. 2009 Oct 8;52(19):6142-52. doi: 10.1021/jm900839k.

PMID:
19746978
12.

AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies.

Zabludoff SD, Deng C, Grondine MR, Sheehy AM, Ashwell S, Caleb BL, Green S, Haye HR, Horn CL, Janetka JW, Liu D, Mouchet E, Ready S, Rosenthal JL, Queva C, Schwartz GK, Taylor KJ, Tse AN, Walker GE, White AM.

Mol Cancer Ther. 2008 Sep;7(9):2955-66. doi: 10.1158/1535-7163.MCT-08-0492.

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