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Items: 9

1.

Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6.

McCoull W, Cheung T, Anderson E, Barton P, Burgess J, Byth K, Cao Q, Castaldi MP, Chen H, Chiarparin E, Carbajo RJ, Code E, Cowan S, Davey PR, Ferguson AD, Fillery S, Fuller NO, Gao N, Hargreaves D, Howard MR, Hu J, Kawatkar A, Kemmitt PD, Leo E, Molina DM, O'Connell N, Petteruti P, Rasmusson T, Raubo P, Rawlins PB, Ricchiuto P, Robb GR, Schenone M, Waring MJ, Zinda M, Fawell S, Wilson DM.

ACS Chem Biol. 2018 Nov 16;13(11):3131-3141. doi: 10.1021/acschembio.8b00698. Epub 2018 Oct 17.

PMID:
30335946
2.

Pharmacological Inhibition of PARP6 Triggers Multipolar Spindle Formation and Elicits Therapeutic Effects in Breast Cancer.

Wang Z, Grosskurth SE, Cheung T, Petteruti P, Zhang J, Wang X, Wang W, Gharahdaghi F, Wu J, Su N, Howard RT, Mayo M, Widzowski D, Scott DA, Johannes JW, Lamb ML, Lawson D, Dry JR, Lyne PD, Tate EW, Zinda M, Mikule K, Fawell SE, Reimer C, Chen H.

Cancer Res. 2018 Dec 1;78(23):6691-6702. doi: 10.1158/0008-5472.CAN-18-1362. Epub 2018 Oct 8.

PMID:
30297535
3.

Identification of CCR2 and CD180 as Robust Pharmacodynamic Tumor and Blood Biomarkers for Clinical Use with BRD4/BET Inhibitors.

Yeh TC, O'Connor G, Petteruti P, Dulak A, Hattersley M, Barrett JC, Chen H.

Clin Cancer Res. 2017 Feb 15;23(4):1025-1035. doi: 10.1158/1078-0432.CCR-16-1658. Epub 2017 Jan 10.

4.

AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies.

Rhyasen GW, Hattersley MM, Yao Y, Dulak A, Wang W, Petteruti P, Dale IL, Boiko S, Cheung T, Zhang J, Wen S, Castriotta L, Lawson D, Collins M, Bao L, Ahdesmaki MJ, Walker G, O'Connor G, Yeh TC, Rabow AA, Dry JR, Reimer C, Lyne P, Mills GB, Fawell SE, Waring MJ, Zinda M, Clark E, Chen H.

Mol Cancer Ther. 2016 Nov;15(11):2563-2574. Epub 2016 Aug 29.

5.

Potent and selective bivalent inhibitors of BET bromodomains.

Waring MJ, Chen H, Rabow AA, Walker G, Bobby R, Boiko S, Bradbury RH, Callis R, Clark E, Dale I, Daniels DL, Dulak A, Flavell L, Holdgate G, Jowitt TA, Kikhney A, McAlister M, Méndez J, Ogg D, Patel J, Petteruti P, Robb GR, Robers MB, Saif S, Stratton N, Svergun DI, Wang W, Whittaker D, Wilson DM, Yao Y.

Nat Chem Biol. 2016 Dec;12(12):1097-1104. doi: 10.1038/nchembio.2210. Epub 2016 Oct 24.

PMID:
27775716
6.

Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.

Johannes JW, Almeida L, Daly K, Ferguson AD, Grosskurth SE, Guan H, Howard T, Ioannidis S, Kazmirski S, Lamb ML, Larsen NA, Lyne PD, Mikule K, Ogoe C, Peng B, Petteruti P, Read JA, Su N, Sylvester M, Throner S, Wang W, Wang X, Wu J, Ye Q, Yu Y, Zheng X, Scott DA.

Bioorg Med Chem Lett. 2015 Dec 15;25(24):5743-7. doi: 10.1016/j.bmcl.2015.10.079. Epub 2015 Oct 27.

PMID:
26546219
7.

Discovery and mechanistic study of a small molecule inhibitor for motor protein KIFC1.

Wu J, Mikule K, Wang W, Su N, Petteruti P, Gharahdaghi F, Code E, Zhu X, Jacques K, Lai Z, Yang B, Lamb ML, Chuaqui C, Keen N, Chen H.

ACS Chem Biol. 2013 Oct 18;8(10):2201-8. doi: 10.1021/cb400186w. Epub 2013 Aug 16.

PMID:
23895133
8.

MEDI0639: a novel therapeutic antibody targeting Dll4 modulates endothelial cell function and angiogenesis in vivo.

Jenkins DW, Ross S, Veldman-Jones M, Foltz IN, Clavette BC, Manchulenko K, Eberlein C, Kendrew J, Petteruti P, Cho S, Damschroder M, Peng L, Baker D, Smith NR, Weir HM, Blakey DC, Bedian V, Barry ST.

Mol Cancer Ther. 2012 Aug;11(8):1650-60. doi: 10.1158/1535-7163.MCT-11-1027. Epub 2012 Jun 7.

9.

Shear stress decreases endothelial cell tissue factor activity by augmenting secretion of tissue factor pathway inhibitor.

Grabowski EF, Reininger AJ, Petteruti PG, Tsukurov O, Orkin RW.

Arterioscler Thromb Vasc Biol. 2001 Jan;21(1):157-62.

PMID:
11145948

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