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Items: 47

1.

Development of High-Throughput Screening Assays for Inhibitors of ETS Transcription Factors.

Currie SL, Warner SL, Vankayalapati H, Liu X, Sharma S, Bearss DJ, Graves BJ.

SLAS Discov. 2018 Sep 11:2472555218798571. doi: 10.1177/2472555218798571. [Epub ahead of print]

PMID:
30204534
2.

Fragment-based design, synthesis, biological evaluation, and SAR of 1H-benzo[d]imidazol-2-yl)-1H-indazol derivatives as potent PDK1 inhibitors.

Chen T, Sorna V, Choi S, Call L, Bearss J, Carpenter K, Warner SL, Sharma S, Bearss DJ, Vankayalapati H.

Bioorg Med Chem Lett. 2017 Dec 15;27(24):5473-5480. doi: 10.1016/j.bmcl.2017.10.041. Epub 2017 Oct 28.

PMID:
29150397
3.

Mechanism and relevance of EWS/FLI-mediated transcriptional repression in Ewing sarcoma.

Sankar S, Bell R, Stephens B, Zhuo R, Sharma S, Bearss DJ, Lessnick SL.

Oncogene. 2016 Nov 24;35(47):6155-6156. doi: 10.1038/onc.2016.142. Epub 2016 Jun 27. No abstract available.

PMID:
27345405
4.

Are Accurins the cure for Aurora kinase inhibitors?

Bearss DJ.

Sci Transl Med. 2016 Feb 10;8(325):325fs4. doi: 10.1126/scitranslmed.aaf1417. Review.

PMID:
26865564
5.

Patterns and Significance of PIM Kinases in Urothelial Carcinoma.

Albertson DJ, Schmidt RL, Bearss JJ, Tripp SR, Bearss DJ, Liu T.

Appl Immunohistochem Mol Morphol. 2015 Nov-Dec;23(10):717-23. doi: 10.1097/PAI.0000000000000138.

PMID:
26551340
6.

Receptor tyrosine kinase Axl is required for resistance of leukemic cells to FLT3-targeted therapy in acute myeloid leukemia.

Park IK, Mundy-Bosse B, Whitman SP, Zhang X, Warner SL, Bearss DJ, Blum W, Marcucci G, Caligiuri MA.

Leukemia. 2015 Dec;29(12):2382-9. doi: 10.1038/leu.2015.147. Epub 2015 Jun 19.

PMID:
26172401
7.

Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors.

Sinha S, Boysen J, Nelson M, Secreto C, Warner SL, Bearss DJ, Lesnick C, Shanafelt TD, Kay NE, Ghosh AK.

Clin Cancer Res. 2015 May 1;21(9):2115-26. doi: 10.1158/1078-0432.CCR-14-1892. Epub 2015 Feb 11.

8.

Inhibition of Nek2 by small molecules affects proteasome activity.

Meng L, Carpenter K, Mollard A, Vankayalapati H, Warner SL, Sharma S, Tricot G, Zhan F, Bearss DJ.

Biomed Res Int. 2014;2014:273180. doi: 10.1155/2014/273180. Epub 2014 Sep 17.

9.

Activators of PKM2 in cancer metabolism.

Warner SL, Carpenter KJ, Bearss DJ.

Future Med Chem. 2014 Jun;6(10):1167-78. doi: 10.4155/fmc.14.70. Review.

PMID:
25078136
10.

Mitochondrial priming of chronic lymphocytic leukemia patients associates Bcl-xL dependence with alvocidib response.

Pierceall WE, Warner SL, Lena RJ, Doykan C, Blake N, Elashoff M, Hoff DV, Bearss DJ, Cardone MH, Andritsos L, Byrd JC, Lanasa MC, Grever MR, Johnson AJ.

Leukemia. 2014 Nov;28(11):2251-4. doi: 10.1038/leu.2014.206. Epub 2014 Jul 3. No abstract available.

11.

A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas.

Foulks JM, Carpenter KJ, Luo B, Xu Y, Senina A, Nix R, Chan A, Clifford A, Wilkes M, Vollmer D, Brenning B, Merx S, Lai S, McCullar MV, Ho KK, Albertson DJ, Call LT, Bearss JJ, Tripp S, Liu T, Stephens BJ, Mollard A, Warner SL, Bearss DJ, Kanner SB.

Neoplasia. 2014 May;16(5):403-12. doi: 10.1016/j.neo.2014.05.004. Epub 2014 Jun 18.

12.

Discovery of Novel Putative Inhibitors of UDP-GlcNAc 2-Epimerase as Potent Antibacterial Agents.

Xu Y, Brenning B, Clifford A, Vollmer D, Bearss J, Jones C, McCarthy V, Shi C, Wolfe B, Aavula B, Warner S, Bearss DJ, McCullar MV, Schuch R, Pelzek A, Bhaskaran SS, Stebbins CE, Goldberg AR, Fischetti VA, Vankayalapati H.

ACS Med Chem Lett. 2013 Dec 12;4(12):1142-1147.

13.

High-throughput virtual screening identifies novel N'-(1-phenylethylidene)-benzohydrazides as potent, specific, and reversible LSD1 inhibitors.

Sorna V, Theisen ER, Stephens B, Warner SL, Bearss DJ, Vankayalapati H, Sharma S.

J Med Chem. 2013 Dec 12;56(23):9496-508. doi: 10.1021/jm400870h. Epub 2013 Nov 23.

PMID:
24237195
14.

The tumor suppressor axis p53/miR-34a regulates Axl expression in B-cell chronic lymphocytic leukemia: implications for therapy in p53-defective CLL patients.

Boysen J, Sinha S, Price-Troska T, Warner SL, Bearss DJ, Viswanatha D, Shanafelt TD, Kay NE, Ghosh AK.

Leukemia. 2014 Feb;28(2):451-5. doi: 10.1038/leu.2013.298. Epub 2013 Oct 18. No abstract available.

15.

TIG1 promotes the development and progression of inflammatory breast cancer through activation of Axl kinase.

Wang X, Saso H, Iwamoto T, Xia W, Gong Y, Pusztai L, Woodward WA, Reuben JM, Warner SL, Bearss DJ, Hortobagyi GN, Hung MC, Ueno NT.

Cancer Res. 2013 Nov 1;73(21):6516-25. doi: 10.1158/0008-5472.CAN-13-0967. Epub 2013 Sep 6.

16.

Use of a bacteriophage lysin to identify a novel target for antimicrobial development.

Schuch R, Pelzek AJ, Raz A, Euler CW, Ryan PA, Winer BY, Farnsworth A, Bhaskaran SS, Stebbins CE, Xu Y, Clifford A, Bearss DJ, Vankayalapati H, Goldberg AR, Fischetti VA.

PLoS One. 2013 Apr 10;8(4):e60754. doi: 10.1371/journal.pone.0060754. Print 2013.

17.

Chemical genetic screen reveals a role for desmosomal adhesion in mammary branching morphogenesis.

Basham KJ, Kieffer C, Shelton DN, Leonard CJ, Bhonde VR, Vankayalapati H, Milash B, Bearss DJ, Looper RE, Welm BE.

J Biol Chem. 2013 Jan 25;288(4):2261-70. doi: 10.1074/jbc.M112.411033. Epub 2012 Dec 3.

18.

Mechanism and relevance of EWS/FLI-mediated transcriptional repression in Ewing sarcoma.

Sankar S, Bell R, Stephens B, Zhuo R, Sharma S, Bearss DJ, Lessnick SL.

Oncogene. 2013 Oct 17;32(42):5089-100. doi: 10.1038/onc.2012.525. Epub 2012 Nov 26. Erratum in: Oncogene. 2016 Nov 24;35(47):6155-6156.

19.

An epithelial-mesenchymal transition gene signature predicts resistance to EGFR and PI3K inhibitors and identifies Axl as a therapeutic target for overcoming EGFR inhibitor resistance.

Byers LA, Diao L, Wang J, Saintigny P, Girard L, Peyton M, Shen L, Fan Y, Giri U, Tumula PK, Nilsson MB, Gudikote J, Tran H, Cardnell RJ, Bearss DJ, Warner SL, Foulks JM, Kanner SB, Gandhi V, Krett N, Rosen ST, Kim ES, Herbst RS, Blumenschein GR, Lee JJ, Lippman SM, Ang KK, Mills GB, Hong WK, Weinstein JN, Wistuba II, Coombes KR, Minna JD, Heymach JV.

Clin Cancer Res. 2013 Jan 1;19(1):279-90. doi: 10.1158/1078-0432.CCR-12-1558. Epub 2012 Oct 22.

20.

Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.

Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ.

ACS Med Chem Lett. 2011 Dec 8;2(12):907-912.

21.

Shining the light on aurora-a kinase as a drug target in pancreatic cancer.

Bearss DJ.

Mol Cancer Ther. 2011 Nov;10(11):2012. doi: 10.1158/1535-7163.MCT-11-0720. No abstract available.

22.

Targeting Axl and Mer kinases in cancer.

Verma A, Warner SL, Vankayalapati H, Bearss DJ, Sharma S.

Mol Cancer Ther. 2011 Oct;10(10):1763-73. doi: 10.1158/1535-7163.MCT-11-0116. Epub 2011 Sep 20. Review.

23.

Competitive enhancement of HGF-induced epithelial scattering by accessory growth factors.

Chung JY, Davis JA, Price BD, Staley DM, Wagner MV, Warner SL, Bearss DJ, Hansen MD.

Exp Cell Res. 2011 Feb 1;317(3):307-18. doi: 10.1016/j.yexcr.2010.11.002. Epub 2010 Nov 11.

PMID:
21075102
24.

In vitro and in vivo characterization of SGI-1252, a small molecule inhibitor of JAK2.

Ahmed KB, Warner SL, Chen A, Gourley ES, Liu X, Vankayalapati H, Nussenzveig R, Prchal JT, Bearss DJ, Parker CJ.

Exp Hematol. 2011 Jan;39(1):14-25. doi: 10.1016/j.exphem.2010.09.013. Epub 2010 Oct 8.

PMID:
20934482
25.

S110, a 5-Aza-2'-deoxycytidine-containing dinucleotide, is an effective DNA methylation inhibitor in vivo and can reduce tumor growth.

Chuang JC, Warner SL, Vollmer D, Vankayalapati H, Redkar S, Bearss DJ, Qiu X, Yoo CB, Jones PA.

Mol Cancer Ther. 2010 May;9(5):1443-50. doi: 10.1158/1535-7163.MCT-09-1048. Epub 2010 May 4.

26.

Pdx-1-driven overexpression of aurora a kinase induces mild ductal dysplasia of pancreatic ducts near islets in transgenic mice.

Warner SL, Muñoz RM, Bearss DJ, Grippo P, Han H, Von Hoff DD.

Pancreas. 2008 Oct;37(3):e39-44. doi: 10.1097/MPA.0b013e318176b9ae.

27.

Identification of a lead small-molecule inhibitor of the Aurora kinases using a structure-assisted, fragment-based approach.

Warner SL, Bashyam S, Vankayalapati H, Bearss DJ, Han H, Mahadevan D, Von Hoff DD, Hurley LH.

Mol Cancer Ther. 2006 Jul;5(7):1764-73. Erratum in: Mol Cancer Ther. 2006 Dec;5(12):3312. Mahadevan, Daruka [added].

28.

Mutations in the G-quadruplex silencer element and their relationship to c-MYC overexpression, NM23 repression, and therapeutic rescue.

Grand CL, Powell TJ, Nagle RB, Bearss DJ, Tye D, Gleason-Guzman M, Hurley LH.

Proc Natl Acad Sci U S A. 2005 Jan 11;102(2):516. No abstract available.

29.

Laminin-5 beta3A expression in LNCaP human prostate carcinoma cells increases cell migration and tumorigenicity.

Calaluce R, Bearss DJ, Barrera J, Zhao Y, Han H, Beck SK, McDaniel K, Nagle RB.

Neoplasia. 2004 Sep-Oct;6(5):468-79.

30.

Identification of human polo-like kinase 1 as a potential therapeutic target in pancreatic cancer.

Gray PJ Jr, Bearss DJ, Han H, Nagle R, Tsao MS, Dean N, Von Hoff DD.

Mol Cancer Ther. 2004 May;3(5):641-6.

31.
32.

The mitotic serine threonine kinase, Aurora-2, is a potential target for drug development in human pancreatic cancer.

Rojanala S, Han H, Muñoz RM, Browne W, Nagle R, Von Hoff DD, Bearss DJ.

Mol Cancer Ther. 2004 Apr;3(4):451-7.

33.

Targeting Aurora-2 kinase in cancer.

Warner SL, Bearss DJ, Han H, Von Hoff DD.

Mol Cancer Ther. 2003 Jun;2(6):589-95. Review.

34.

Structure-based design of novel anti-cancer agents targeting aurora kinases.

Mahadevan D, Bearss DJ, Vankayalapati H.

Curr Med Chem Anticancer Agents. 2003 Jan;3(1):25-34. Review.

PMID:
12678912
35.

Targeting aurora2 kinase in oncogenesis: a structural bioinformatics approach to target validation and rational drug design.

Vankayalapati H, Bearss DJ, Saldanha JW, Muñoz RM, Rojanala S, Von Hoff DD, Mahadevan D.

Mol Cancer Ther. 2003 Mar;2(3):283-94.

36.

p53-independent response to cisplatin and oxaliplatin in MMTV-ras mouse salivary tumors.

Petit T, Bearss DJ, Troyer DA, Munoz RM, Windle JJ.

Mol Cancer Ther. 2003 Feb;2(2):165-71.

37.

Telomere inhibition and telomere disruption as processes for drug targeting.

Rezler EM, Bearss DJ, Hurley LH.

Annu Rev Pharmacol Toxicol. 2003;43:359-79. Epub 2002 Jan 10. Review.

PMID:
12540745
38.

The cationic porphyrin TMPyP4 down-regulates c-MYC and human telomerase reverse transcriptase expression and inhibits tumor growth in vivo.

Grand CL, Han H, Muñoz RM, Weitman S, Von Hoff DD, Hurley LH, Bearss DJ.

Mol Cancer Ther. 2002 Jun;1(8):565-73. Erratum in: Mol Cancer Ther.2003 Feb;2(2):208.

39.

Potential mouse tumor model for pre-clinical testing of mage-specific breast cancer vaccines.

Sypniewska RK, Hoflack L, Bearss DJ, Gravekamp C.

Breast Cancer Res Treat. 2002 Jun;74(3):221-33.

PMID:
12211215
40.

Direct evidence for a G-quadruplex in a promoter region and its targeting with a small molecule to repress c-MYC transcription.

Siddiqui-Jain A, Grand CL, Bearss DJ, Hurley LH.

Proc Natl Acad Sci U S A. 2002 Sep 3;99(18):11593-8. Epub 2002 Aug 23.

41.

Telomeres and telomerases as drug targets.

Rezler EM, Bearss DJ, Hurley LH.

Curr Opin Pharmacol. 2002 Aug;2(4):415-23. Review.

PMID:
12127874
42.

Identification of differentially expressed genes in pancreatic cancer cells using cDNA microarray.

Han H, Bearss DJ, Browne LW, Calaluce R, Nagle RB, Von Hoff DD.

Cancer Res. 2002 May 15;62(10):2890-6. Erratum in: Cancer Res 2002 Aug;62(15):4532.

43.

Differential effects of p21(WAF1/CIP1) deficiency on MMTV-ras and MMTV-myc mammary tumor properties.

Bearss DJ, Lee RJ, Troyer DA, Pestell RG, Windle JJ.

Cancer Res. 2002 Apr 1;62(7):2077-84.

44.

Telomere maintenance mechanisms as a target for drug development.

Bearss DJ, Hurley LH, Von Hoff DD.

Oncogene. 2000 Dec 27;19(56):6632-41. Review.

45.

Genetic determinants of response to chemotherapy in transgenic mouse mammary and salivary tumors.

Bearss DJ, Subler MA, Hundley JE, Troyer DA, Salinas RA, Windle JJ.

Oncogene. 2000 Feb 21;19(8):1114-22.

PMID:
10713698
46.

Reciprocal regulation of neu tyrosine kinase activity and caveolin-1 protein expression in vitro and in vivo. Implications for human breast cancer.

Engelman JA, Lee RJ, Karnezis A, Bearss DJ, Webster M, Siegel P, Muller WJ, Windle JJ, Pestell RG, Lisanti MP.

J Biol Chem. 1998 Aug 7;273(32):20448-55.

47.

A farnesyltransferase inhibitor induces tumor regression in transgenic mice harboring multiple oncogenic mutations by mediating alterations in both cell cycle control and apoptosis.

Barrington RE, Subler MA, Rands E, Omer CA, Miller PJ, Hundley JE, Koester SK, Troyer DA, Bearss DJ, Conner MW, Gibbs JB, Hamilton K, Koblan KS, Mosser SD, O'Neill TJ, Schaber MD, Senderak ET, Windle JJ, Oliff A, Kohl NE.

Mol Cell Biol. 1998 Jan;18(1):85-92.

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