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Items: 34


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]


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.


Ruthenium(II)- and copper(I)-catalyzed synthesis of click-xylosides and assessment of their glycosaminoglycan priming activity.

Mencio CP, Garud DR, Doi Y, Bi Y, Vankayalapati H, Koketsu M, Kuberan B.

Bioorg Med Chem Lett. 2017 Nov 15;27(22):5027-5030. doi: 10.1016/j.bmcl.2017.10.004. Epub 2017 Oct 3.


Repurposing of Proton Pump Inhibitors as first identified small molecule inhibitors of endo-β-N-acetylglucosaminidase (ENGase) for the treatment of NGLY1 deficiency, a rare genetic disease.

Bi Y, Might M, Vankayalapati H, Kuberan B.

Bioorg Med Chem Lett. 2017 Jul 1;27(13):2962-2966. doi: 10.1016/j.bmcl.2017.05.010. Epub 2017 May 5.


SIK2 Restricts Autophagic Flux To Support Triple-Negative Breast Cancer Survival.

Maxfield KE, Macion J, Vankayalapati H, Whitehurst AW.

Mol Cell Biol. 2016 Nov 28;36(24):3048-3057. Print 2016 Dec 15.


A Novel Compound ARN-3236 Inhibits Salt-Inducible Kinase 2 and Sensitizes Ovarian Cancer Cell Lines and Xenografts to Paclitaxel.

Zhou J, Alfraidi A, Zhang S, Santiago-O'Farrill JM, Yerramreddy Reddy VK, Alsaadi A, Ahmed AA, Yang H, Liu J, Mao W, Wang Y, Takemori H, Vankayalapati H, Lu Z, Bast RC Jr.

Clin Cancer Res. 2017 Apr 15;23(8):1945-1954. doi: 10.1158/1078-0432.CCR-16-1562. Epub 2016 Sep 27.


Design, Synthesis, and Biological Evaluation of a Series of Anthracene-9,10-dione Dioxime β-Catenin Pathway Inhibitors.

Soldi R, Horrigan SK, Cholody MW, Padia J, Sorna V, Bearss J, Gilcrease G, Bhalla K, Verma A, Vankayalapati H, Sharma S.

J Med Chem. 2015 Aug 13;58(15):5854-62. doi: 10.1021/acs.jmedchem.5b00460. Epub 2015 Jul 31.


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.


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.


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.


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.


Novel homozygous VHL mutation in exon 2 is associated with congenital polycythemia but not with cancer.

Lanikova L, Lorenzo F, Yang C, Vankayalapati H, Drachtman R, Divoky V, Prchal JT.

Blood. 2013 May 9;121(19):3918-24. doi: 10.1182/blood-2012-11-469296. Epub 2013 Mar 28.


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.


A novel EPAS1/HIF2A germline mutation in a congenital polycythemia with paraganglioma.

Lorenzo FR, Yang C, Ng Tang Fui M, Vankayalapati H, Zhuang Z, Huynh T, Grossmann M, Pacak K, Prchal JT.

J Mol Med (Berl). 2013 Apr;91(4):507-12. doi: 10.1007/s00109-012-0967-z. Epub 2012 Oct 23.


Molecular heterogeneity of glucose-6-phosphate dehydrogenase deficiency in Gaza Strip Palestinians.

Sirdah M, Reading NS, Vankayalapati H, Perkins SL, Shubair ME, Aboud L, Roper D, Prchal JT.

Blood Cells Mol Dis. 2012 Oct 15-Dec 15;49(3-4):152-8. doi: 10.1016/j.bcmd.2012.06.003. Epub 2012 Jul 5.


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.


Structure-activity analysis and cell-based optimization of human galactokinase inhibitors.

Odejinmi S, Rascon R, Tang M, Vankayalapati H, Lai K.

ACS Med Chem Lett. 2011 Sep 8;2(9):667-672.


Innovative therapy for Classic Galactosemia - tale of two HTS.

Tang M, Odejinmi SI, Vankayalapati H, Wierenga KJ, Lai K.

Mol Genet Metab. 2012 Jan;105(1):44-55. doi: 10.1016/j.ymgme.2011.09.028. Epub 2011 Oct 1. Review.


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.


Identification of novel small molecule inhibitors of 4-diphosphocytidyl-2-C-methyl-D-erythritol (CDP-ME) kinase of Gram-negative bacteria.

Tang M, Odejinmi SI, Allette YM, Vankayalapati H, Lai K.

Bioorg Med Chem. 2011 Oct 1;19(19):5886-95. doi: 10.1016/j.bmc.2011.08.012. Epub 2011 Aug 16.


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.


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.


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].


Determination of the importance of the stereochemistry of psorospermin in topoisomerase II-induced alkylation of DNA and in vitro and in vivo biological activity.

Fellows IM, Schwaebe M, Dexheimer TS, Vankayalapati H, Gleason-Guzman M, Whitten JP, Hurley LH.

Mol Cancer Ther. 2005 Nov;4(11):1729-39.


Conformationally restricted analogues of psorospermin: design, synthesis, and bioactivity of natural-product-related bisfuranoxanthones.

Heald RA, Dexheimer TS, Vankayalapati H, Siddiqui-Jain A, Szabo LZ, Gleason-Guzman MC, Hurley LH.

J Med Chem. 2005 Apr 21;48(8):2993-3004.


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.


Structure of a quinobenzoxazine--G-quadruplex complex by REDOR NMR.

Mehta AK, Shayo Y, Vankayalapati H, Hurley LH, Schaefer J.

Biochemistry. 2004 Sep 28;43(38):11953-8.


Design, synthesis, and evaluation of psorospermin/quinobenzoxazine hybrids as structurally novel antitumor agents.

Kim MY, Na Y, Vankayalapati H, Gleason-Guzman M, Hurley LH.

J Med Chem. 2003 Jul 3;46(14):2958-72.


Specific inhibition of the Akt1 pleckstrin homology domain by D-3-deoxy-phosphatidyl-myo-inositol analogues.

Meuillet EJ, Mahadevan D, Vankayalapati H, Berggren M, Williams R, Coon A, Kozikowski AP, Powis G.

Mol Cancer Ther. 2003 Apr;2(4):389-99.


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.


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.


Design and synthesis of fluoroquinophenoxazines that interact with human telomeric G-quadruplexes and their biological effects.

Duan W, Rangan A, Vankayalapati H, Kim MY, Zeng Q, Sun D, Han H, Fedoroff OY, Nishioka D, Rha SY, Izbicka E, Von Hoff DD, Hurley LH.

Mol Cancer Ther. 2001 Dec;1(2):103-20.


Telomestatin, a potent telomerase inhibitor that interacts quite specifically with the human telomeric intramolecular g-quadruplex.

Kim MY, Vankayalapati H, Shin-Ya K, Wierzba K, Hurley LH.

J Am Chem Soc. 2002 Mar 13;124(10):2098-9.


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