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Items: 13

1.

Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy.

Gomes B, Driessens G, Bartlett D, Cai D, Cauwenberghs S, Crosignani S, Dalvie D, Denies S, Dillon CP, Fantin VR, Guo J, Letellier MC, Li W, Maegley K, Marillier R, Miller N, Pirson R, Rabolli V, Ray C, Streiner N, Torti VR, Tsaparikos K, Van den Eynde BJ, Wythes M, Yao LC, Zheng X, Tumang J, Kraus M.

Mol Cancer Ther. 2018 Dec;17(12):2530-2542. doi: 10.1158/1535-7163.MCT-17-1104. Epub 2018 Sep 19.

PMID:
30232146
2.

Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells.

Pierre F, Regan CF, Chevrel MC, Siddiqui-Jain A, Macalino D, Streiner N, Drygin D, Haddach M, O'Brien SE, Rice WG, Ryckman DM.

Bioorg Med Chem Lett. 2012 May 1;22(9):3327-31. doi: 10.1016/j.bmcl.2012.02.099. Epub 2012 Mar 6.

PMID:
22460033
3.

Combined inhibition of EGFR and CK2 augments the attenuation of PI3K-Akt-mTOR signaling and the killing of cancer cells.

Bliesath J, Huser N, Omori M, Bunag D, Proffitt C, Streiner N, Ho C, Siddiqui-Jain A, O'Brien SE, Lim JK, Ryckman DM, Anderes K, Rice WG, Drygin D.

Cancer Lett. 2012 Sep 1;322(1):113-8. doi: 10.1016/j.canlet.2012.02.032. Epub 2012 Mar 2.

PMID:
22387988
4.

Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.

Haddach M, Michaux J, Schwaebe MK, Pierre F, O'Brien SE, Borsan C, Tran J, Raffaele N, Ravula S, Drygin D, Siddiqui-Jain A, Darjania L, Stansfield R, Proffitt C, Macalino D, Streiner N, Bliesath J, Omori M, Whitten JP, Anderes K, Rice WG, Ryckman DM.

ACS Med Chem Lett. 2011 Dec 27;3(2):135-9. doi: 10.1021/ml200259q. eCollection 2012 Feb 9.

5.

CK2 inhibitor CX-4945 suppresses DNA repair response triggered by DNA-targeted anticancer drugs and augments efficacy: mechanistic rationale for drug combination therapy.

Siddiqui-Jain A, Bliesath J, Macalino D, Omori M, Huser N, Streiner N, Ho CB, Anderes K, Proffitt C, O'Brien SE, Lim JK, Von Hoff DD, Ryckman DM, Rice WG, Drygin D.

Mol Cancer Ther. 2012 Apr;11(4):994-1005. doi: 10.1158/1535-7163.MCT-11-0613. Epub 2012 Jan 20.

6.

7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity.

Pierre F, Stefan E, N├ędellec AS, Chevrel MC, Regan CF, Siddiqui-Jain A, Macalino D, Streiner N, Drygin D, Haddach M, O'Brien SE, Anderes K, Ryckman DM.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6687-92. doi: 10.1016/j.bmcl.2011.09.059. Epub 2011 Sep 22.

PMID:
21982499
7.

Pre-clinical characterization of CX-4945, a potent and selective small molecule inhibitor of CK2 for the treatment of cancer.

Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Rice WG, Ryckman DM, Anderes K.

Mol Cell Biochem. 2011 Oct;356(1-2):37-43. doi: 10.1007/s11010-011-0956-5. Epub 2011 Jul 14.

PMID:
21755459
8.

Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties.

Pierre F, O'Brien SE, Haddach M, Bourbon P, Schwaebe MK, Stefan E, Darjania L, Stansfield R, Ho C, Siddiqui-Jain A, Streiner N, Rice WG, Anderes K, Ryckman DM.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1687-91. doi: 10.1016/j.bmcl.2011.01.091. Epub 2011 Jan 26.

PMID:
21316963
9.

Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.

Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Anderes K, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Trent K, Rice WG, Ryckman DM.

J Med Chem. 2011 Jan 27;54(2):635-54. doi: 10.1021/jm101251q. Epub 2010 Dec 21.

PMID:
21174434
10.

Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth.

Drygin D, Lin A, Bliesath J, Ho CB, O'Brien SE, Proffitt C, Omori M, Haddach M, Schwaebe MK, Siddiqui-Jain A, Streiner N, Quin JE, Sanij E, Bywater MJ, Hannan RD, Ryckman D, Anderes K, Rice WG.

Cancer Res. 2011 Feb 15;71(4):1418-30. doi: 10.1158/0008-5472.CAN-10-1728. Epub 2010 Dec 15.

11.

CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy.

Siddiqui-Jain A, Drygin D, Streiner N, Chua P, Pierre F, O'Brien SE, Bliesath J, Omori M, Huser N, Ho C, Proffitt C, Schwaebe MK, Ryckman DM, Rice WG, Anderes K.

Cancer Res. 2010 Dec 15;70(24):10288-98. doi: 10.1158/0008-5472.CAN-10-1893.

12.

Early placental insulin-like protein (INSL4 or EPIL) in placental and fetal membrane growth.

Millar L, Streiner N, Webster L, Yamamoto S, Okabe R, Kawamata T, Shimoda J, B├╝llesbach E, Schwabe C, Bryant-Greenwood G.

Biol Reprod. 2005 Oct;73(4):695-702. Epub 2005 Jun 15.

13.

Design and synthesis of an expanded porphyrin that has selectivity for the c-MYC G-quadruplex structure.

Seenisamy J, Bashyam S, Gokhale V, Vankayalapati H, Sun D, Siddiqui-Jain A, Streiner N, Shin-Ya K, White E, Wilson WD, Hurley LH.

J Am Chem Soc. 2005 Mar 9;127(9):2944-59.

PMID:
15740131

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