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Clinical Implications of Targeting XPO1-mediated Nuclear Export in Multiple Myeloma.

Gandhi UH, Senapedis W, Baloglu E, Unger TJ, Chari A, Vogl D, Cornell RF.

Clin Lymphoma Myeloma Leuk. 2018 Mar 14. pii: S2152-2650(17)31881-5. doi: 10.1016/j.clml.2018.03.003. [Epub ahead of print] Review.


Target identification of small molecules using large-scale CRISPR-Cas mutagenesis scanning of essential genes.

Neggers JE, Kwanten B, Dierckx T, Noguchi H, Voet A, Bral L, Minner K, Massant B, Kint N, Delforge M, Vercruysse T, Baloglu E, Senapedis W, Jacquemyn M, Daelemans D.

Nat Commun. 2018 Feb 5;9(1):502. doi: 10.1038/s41467-017-02349-8.


XPO1 target occupancy measurements confirm the selinexor recommended phase 2 dose.

Crochiere ML, Hannus S, Hansen K, Becker F, Baloglu E, Lee M, Kauffman M, Shacham S, Landesman Y.

Oncotarget. 2017 Nov 30;8(66):110503-110516. doi: 10.18632/oncotarget.22801. eCollection 2017 Dec 15.


Exportin 1 (XPO1) inhibition leads to restoration of tumor suppressor miR-145 and consequent suppression of pancreatic cancer cell proliferation and migration.

Azmi AS, Li Y, Muqbil I, Aboukameel A, Senapedis W, Baloglu E, Landesman Y, Shacham S, Kauffman MG, Philip PA, Mohammad RM.

Oncotarget. 2017 Jul 17;8(47):82144-82155. doi: 10.18632/oncotarget.19285. eCollection 2017 Oct 10.


Decrypting the PAK4 transcriptome profile in mammary tumor forming cells using Next Generation Sequencing.

Rane CK, Patel M, Cai L, Senapedis W, Baloglu E, Minden A.

Genomics. 2017 Oct 18. pii: S0888-7543(17)30128-3. doi: 10.1016/j.ygeno.2017.10.004. [Epub ahead of print]


Targeting the vulnerability to NAD+ depletion in B-cell acute lymphoblastic leukemia.

Takao S, Chien W, Madan V, Lin DC, Ding LW, Sun QY, Mayakonda A, Sudo M, Xu L, Chen Y, Jiang YY, Gery S, Lill M, Park E, Senapedis W, Baloglu E, Müschen M, Koeffler HP.

Leukemia. 2018 Mar;32(3):616-625. doi: 10.1038/leu.2017.281. Epub 2017 Sep 14.


Selinexor (KPT-330) has antitumor activity against anaplastic thyroid carcinoma in vitro and in vivo and enhances sensitivity to doxorubicin.

Garg M, Kanojia D, Mayakonda A, Ganesan TS, Sadhanandhan B, Suresh S, S S, Nagare RP, Said JW, Doan NB, Ding LW, Baloglu E, Shacham S, Kauffman M, Koeffler HP.

Sci Rep. 2017 Aug 29;7(1):9749. doi: 10.1038/s41598-017-10325-x.


Targeting Rho GTPase effector p21 activated kinase 4 (PAK4) suppresses p-Bad-microRNA drug resistance axis leading to inhibition of pancreatic ductal adenocarcinoma proliferation.

Mohammad RM, Li Y, Muqbil I, Aboukameel A, Senapedis W, Baloglu E, Landesman Y, Philip PA, Azmi AS.

Small GTPases. 2017 Jun 22:0. doi: 10.1080/21541248.2017.1329694. [Epub ahead of print]


A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action.

Campaner E, Rustighi A, Zannini A, Cristiani A, Piazza S, Ciani Y, Kalid O, Golan G, Baloglu E, Shacham S, Valsasina B, Cucchi U, Pippione AC, Lolli ML, Giabbai B, Storici P, Carloni P, Rossetti G, Benvenuti F, Bello E, D'Incalci M, Cappuzzello E, Rosato A, Del Sal G.

Nat Commun. 2017 Jun 9;8:15772. doi: 10.1038/ncomms15772.


Anticystogenic activity of a small molecule PAK4 inhibitor may be a novel treatment for autosomal dominant polycystic kidney disease.

Hwang VJ, Zhou X, Chen X, Trott J, Abu Aboud O, Shim K, Dionne LK, Chmiel KJ, Senapedis W, Baloglu E, Mahjoub MR, Li X, Weiss RH.

Kidney Int. 2017 Oct;92(4):922-933. doi: 10.1016/j.kint.2017.03.031. Epub 2017 May 23.


A novel orally bioavailable compound KPT-9274 inhibits PAK4, and blocks triple negative breast cancer tumor growth.

Rane C, Senapedis W, Baloglu E, Landesman Y, Crochiere M, Das-Gupta S, Minden A.

Sci Rep. 2017 Feb 15;7:42555. doi: 10.1038/srep42555.


Functional role and therapeutic targeting of p21-activated kinase 4 in multiple myeloma.

Fulciniti M, Martinez-Lopez J, Senapedis W, Oliva S, Lakshmi Bandi R, Amodio N, Xu Y, Szalat R, Gulla A, Samur MK, Roccaro A, Linares M, Cea M, Baloglu E, Argueta C, Landesman Y, Shacham S, Liu S, Schenone M, Wu SL, Karger B, Prabhala R, Anderson KC, Munshi NC.

Blood. 2017 Apr 20;129(16):2233-2245. doi: 10.1182/blood-2016-06-724831. Epub 2017 Jan 17.


Novel p21-Activated Kinase 4 (PAK4) Allosteric Modulators Overcome Drug Resistance and Stemness in Pancreatic Ductal Adenocarcinoma.

Aboukameel A, Muqbil I, Senapedis W, Baloglu E, Landesman Y, Shacham S, Kauffman M, Philip PA, Mohammad RM, Azmi AS.

Mol Cancer Ther. 2017 Jan;16(1):76-87. doi: 10.1158/1535-7163.MCT-16-0205. Epub 2016 Nov 15.


Molecular mechanism and therapeutic implications of selinexor (KPT-330) in liposarcoma.

Garg M, Kanojia D, Mayakonda A, Said JW, Doan NB, Chien W, Ganesan TS, Chuang LS, Venkatachalam N, Baloglu E, Shacham S, Kauffman M, Koeffler HP.

Oncotarget. 2017 Jan 31;8(5):7521-7532. doi: 10.18632/oncotarget.13485.


The Second-Generation Exportin-1 Inhibitor KPT-8602 Demonstrates Potent Activity against Acute Lymphoblastic Leukemia.

Vercruysse T, De Bie J, Neggers JE, Jacquemyn M, Vanstreels E, Schmid-Burgk JL, Hornung V, Baloglu E, Landesman Y, Senapedis W, Shacham S, Dagklis A, Cools J, Daelemans D.

Clin Cancer Res. 2017 May 15;23(10):2528-2541. doi: 10.1158/1078-0432.CCR-16-1580. Epub 2016 Oct 25.


Anti-tumor activity of selective inhibitor of nuclear export (SINE) compounds, is enhanced in non-Hodgkin lymphoma through combination with mTOR inhibitor and dexamethasone.

Muqbil I, Aboukameel A, Elloul S, Carlson R, Senapedis W, Baloglu E, Kauffman M, Shacham S, Bhutani D, Zonder J, Azmi AS, Mohammad RM.

Cancer Lett. 2016 Dec 28;383(2):309-317. doi: 10.1016/j.canlet.2016.09.016. Epub 2016 Sep 28.


XPO1-dependent nuclear export is a druggable vulnerability in KRAS-mutant lung cancer.

Kim J, McMillan E, Kim HS, Venkateswaran N, Makkar G, Rodriguez-Canales J, Villalobos P, Neggers JE, Mendiratta S, Wei S, Landesman Y, Senapedis W, Baloglu E, Chow CB, Frink RE, Gao B, Roth M, Minna JD, Daelemans D, Wistuba II, Posner BA, Scaglioni PP, White MA.

Nature. 2016 Oct 6;538(7623):114-117. doi: 10.1038/nature19771. Epub 2016 Sep 28.


Inhibition of alveolar Na transport and LPS causes hypoxemia and pulmonary arterial vasoconstriction in ventilated rats.

Davieds B, Gross J, Berger MM, Baloğlu E, Bärtsch P, Mairbäurl H.

Physiol Rep. 2016 Sep;4(18). pii: e12985.


Heterozygous mutation of cysteine528 in XPO1 is sufficient for resistance to selective inhibitors of nuclear export.

Neggers JE, Vanstreels E, Baloglu E, Shacham S, Landesman Y, Daelemans D.

Oncotarget. 2016 Oct 18;7(42):68842-68850. doi: 10.18632/oncotarget.11995.


Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth.

Abu Aboud O, Chen CH, Senapedis W, Baloglu E, Argueta C, Weiss RH.

Mol Cancer Ther. 2016 Sep;15(9):2119-29. doi: 10.1158/1535-7163.MCT-16-0197. Epub 2016 Jul 7.


Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies.

Hing ZA, Fung HY, Ranganathan P, Mitchell S, El-Gamal D, Woyach JA, Williams K, Goettl VM, Smith J, Yu X, Meng X, Sun Q, Cagatay T, Lehman AM, Lucas DM, Baloglu E, Shacham S, Kauffman MG, Byrd JC, Chook YM, Garzon R, Lapalombella R.

Leukemia. 2016 Dec;30(12):2364-2372. doi: 10.1038/leu.2016.136. Epub 2016 May 20.


KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells.

Etchin J, Berezovskaya A, Conway AS, Galinsky IA, Stone RM, Baloglu E, Senapedis W, Landesman Y, Kauffman M, Shacham S, Wang JC, Look AT.

Leukemia. 2017 Jan;31(1):143-150. doi: 10.1038/leu.2016.145. Epub 2016 May 23.


Targeting super-enhancer-associated oncogenes in oesophageal squamous cell carcinoma.

Jiang YY, Lin DC, Mayakonda A, Hazawa M, Ding LW, Chien WW, Xu L, Chen Y, Xiao JF, Senapedis W, Baloglu E, Kanojia D, Shang L, Xu X, Yang H, Tyner JW, Wang MR, Koeffler HP.

Gut. 2017 Aug;66(8):1358-1368. doi: 10.1136/gutjnl-2016-311818. Epub 2016 May 10.


Mucoadhesive in situ gel formulation for vaginal delivery of clotrimazole: formulation, preparation, and in vitro/in vivo evaluation.

Rençber S, Karavana SY, Şenyiğit ZA, Eraç B, Limoncu MH, Baloğlu E.

Pharm Dev Technol. 2017 Jun;22(4):551-561. doi: 10.3109/10837450.2016.1163385. Epub 2016 Apr 7.


XPO1 Inhibition Preferentially Disrupts the 3D Nuclear Organization of Telomeres in Tumor Cells.

Taylor-Kashton C, Lichtensztejn D, Baloglu E, Senapedis W, Shacham S, Kauffman MG, Kotb R, Mai S.

J Cell Physiol. 2016 Dec;231(12):2711-9. doi: 10.1002/jcp.25378. Epub 2016 Apr 8.


CRM1 Inhibition Promotes Cytotoxicity in Ewing Sarcoma Cells by Repressing EWS-FLI1-Dependent IGF-1 Signaling.

Sun H, Lin DC, Cao Q, Guo X, Marijon H, Zhao Z, Gery S, Xu L, Yang H, Pang B, Lee VK, Lim HJ, Doan N, Said JW, Chu P, Mayakonda A, Thomas T, Forscher C, Baloglu E, Shacham S, Rajalingam R, Koeffler HP.

Cancer Res. 2016 May 1;76(9):2687-97. doi: 10.1158/0008-5472.CAN-15-1572. Epub 2016 Mar 8.


A method for quantification of exportin-1 (XPO1) occupancy by Selective Inhibitor of Nuclear Export (SINE) compounds.

Crochiere ML, Baloglu E, Klebanov B, Donovan S, Del Alamo D, Lee M, Kauffman M, Shacham S, Landesman Y.

Oncotarget. 2016 Jan 12;7(2):1863-77. doi: 10.18632/oncotarget.6495.


Targeting the Nuclear Export Protein XPO1/CRM1 Reverses Epithelial to Mesenchymal Transition.

Azmi AS, Muqbil I, Wu J, Aboukameel A, Senapedis W, Baloglu E, Bollig-Fischer A, Dyson G, Kauffman M, Landesman Y, Shacham S, Philip PA, Mohammad RM.

Sci Rep. 2015 Nov 5;5:16077. doi: 10.1038/srep16077.


Design and evaluation of an intravesical delivery system for superficial bladder cancer: preparation of gemcitabine HCl-loaded chitosan-thioglycolic acid nanoparticles and comparison of chitosan/poloxamer gels as carriers.

Şenyiğit ZA, Karavana SY, İlem-Özdemir D, Çalışkan Ç, Waldner C, Şen S, Bernkop-Schnürch A, Baloğlu E.

Int J Nanomedicine. 2015 Oct 14;10:6493-507. doi: 10.2147/IJN.S93750. eCollection 2015.


FXYD1 negatively regulates Na(+)/K(+)-ATPase activity in lung alveolar epithelial cells.

Wujak ŁA, Blume A, Baloğlu E, Wygrecka M, Wygowski J, Herold S, Mayer K, Vadász I, Besuch P, Mairbäurl H, Seeger W, Morty RE.

Respir Physiol Neurobiol. 2016 Jan;220:54-61. doi: 10.1016/j.resp.2015.09.008. Epub 2015 Sep 26.


Rebuttal to the PRO Statement.

Mairbäurl H, Baloglu E.

High Alt Med Biol. 2015 Sep;16(3):194. doi: 10.1089/ham.2015.0075. Epub 2015 Aug 25. No abstract available.


Con: Corticosteroids Are Useful in the Management of HAPE.

Mairbäurl H, Baloglu E.

High Alt Med Biol. 2015 Sep;16(3):190-2. doi: 10.1089/ham.2015.0071. Epub 2015 Aug 25. No abstract available.


Therapeutic Potential of Targeting PAK Signaling.

Senapedis W, Crochiere M, Baloglu E, Landesman Y.

Anticancer Agents Med Chem. 2016;16(1):75-88. Review.


In vivo regulation of gene expression and T helper type 17 differentiation by RORγt inverse agonists.

Skepner J, Trocha M, Ramesh R, Qu XA, Schmidt D, Baloglu E, Lobera M, Davis S, Nolan MA, Carlson TJ, Hill J, Ghosh S, Sundrud MS, Yang J.

Immunology. 2015 Jul;145(3):347-56. doi: 10.1111/imm.12444. Epub 2015 Apr 3.


Identifying drug-target selectivity of small-molecule CRM1/XPO1 inhibitors by CRISPR/Cas9 genome editing.

Neggers JE, Vercruysse T, Jacquemyn M, Vanstreels E, Baloglu E, Shacham S, Crochiere M, Landesman Y, Daelemans D.

Chem Biol. 2015 Jan 22;22(1):107-16. doi: 10.1016/j.chembiol.2014.11.015. Epub 2015 Jan 8.


Nucleo-cytoplasmic transport as a therapeutic target of cancer.

Gravina GL, Senapedis W, McCauley D, Baloglu E, Shacham S, Festuccia C.

J Hematol Oncol. 2014 Dec 5;7:85. doi: 10.1186/s13045-014-0085-1. Review.


Verdinexor, a novel selective inhibitor of nuclear export, reduces influenza a virus replication in vitro and in vivo.

Perwitasari O, Johnson S, Yan X, Howerth E, Shacham S, Landesman Y, Baloglu E, McCauley D, Tamir S, Tompkins SM, Tripp RA.

J Virol. 2014 Sep 1;88(17):10228-43. doi: 10.1128/JVI.01774-14. Epub 2014 Jun 25.


Evaluation of chitosan based vaginal bioadhesive gel formulations for antifungal drugs.

Senyiğit ZA, Karavana SY, Eraç B, Gürsel O, Limoncu MH, Baloğlu E.

Acta Pharm. 2014 Jun;64(2):139-56. doi: 10.2478/acph-2014-0013.


Clinical translation of nuclear export inhibitors in cancer.

Senapedis WT, Baloglu E, Landesman Y.

Semin Cancer Biol. 2014 Aug;27:74-86. doi: 10.1016/j.semcancer.2014.04.005. Epub 2014 Apr 19. Review.


Small-molecule RORγt antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms.

Xiao S, Yosef N, Yang J, Wang Y, Zhou L, Zhu C, Wu C, Baloglu E, Schmidt D, Ramesh R, Lobera M, Sundrud MS, Tsai PY, Xiang Z, Wang J, Xu Y, Lin X, Kretschmer K, Rahl PB, Young RA, Zhong Z, Hafler DA, Regev A, Ghosh S, Marson A, Kuchroo VK.

Immunity. 2014 Apr 17;40(4):477-89. doi: 10.1016/j.immuni.2014.04.004.


Pharmacologic inhibition of RORγt regulates Th17 signature gene expression and suppresses cutaneous inflammation in vivo.

Skepner J, Ramesh R, Trocha M, Schmidt D, Baloglu E, Lobera M, Carlson T, Hill J, Orband-Miller LA, Barnes A, Boudjelal M, Sundrud M, Ghosh S, Yang J.

J Immunol. 2014 Mar 15;192(6):2564-75. doi: 10.4049/jimmunol.1302190. Epub 2014 Feb 10.


Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group.

Lobera M, Madauss KP, Pohlhaus DT, Wright QG, Trocha M, Schmidt DR, Baloglu E, Trump RP, Head MS, Hofmann GA, Murray-Thompson M, Schwartz B, Chakravorty S, Wu Z, Mander PK, Kruidenier L, Reid RA, Burkhart W, Turunen BJ, Rong JX, Wagner C, Moyer MB, Wells C, Hong X, Moore JT, Williams JD, Soler D, Ghosh S, Nolan MA.

Nat Chem Biol. 2013 May;9(5):319-25. doi: 10.1038/nchembio.1223. Epub 2013 Mar 24.


In-situ gel formulations of econazole nitrate: preparation and in-vitro and in-vivo evaluation.

Baloglu E, Karavana SY, Senyigit ZA, Hilmioglu-Polat S, Metin DY, Zekioglu O, Guneri T, Jones DS.

J Pharm Pharmacol. 2011 Oct;63(10):1274-82. doi: 10.1111/j.2042-7158.2011.01315.x. Epub 2011 Aug 30.


In vitro evaluation of mucoadhesive vaginal tablets of antifungal drugs prepared with thiolated polymer and development of a new dissolution technique for vaginal formulations.

Baloglu E, Ay Senyıgıt Z, Karavana SY, Vetter A, Metın DY, Hilmioglu Polat S, Guneri T, Bernkop-Schnurch A.

Chem Pharm Bull (Tokyo). 2011;59(8):952-8.


β2-Adrenergics in hypoxia desensitize receptors but blunt inhibition of reabsorption in rat lungs.

Baloglu E, Reingruber T, Bärtsch P, Mairbäurl H.

Am J Respir Cell Mol Biol. 2011 Nov;45(5):1059-68. doi: 10.1165/rcmb.2010-0273OC. Epub 2011 May 11.


Rheological and mechanical properties of poloxamer mixtures as a mucoadhesive gel base.

Baloglu E, Karavana SY, Senyigit ZA, Guneri T.

Pharm Dev Technol. 2011 Nov-Dec;16(6):627-36. doi: 10.3109/10837450.2010.508074. Epub 2010 Aug 17.


A design and evaluation of layered matrix tablet formulations of metoprolol tartrate.

Baloğlu E, Senyiğit T.

AAPS PharmSciTech. 2010 Jun;11(2):563-73. doi: 10.1208/s12249-010-9409-9. Epub 2010 Mar 30.


Design and formulation of mebeverine HCl semisolid formulations for intraorally administration.

Baloğlu E, Karavana SY, Hyusein IY, Köse T.

AAPS PharmSciTech. 2010 Mar;11(1):181-8. doi: 10.1208/s12249-009-9374-3. Epub 2010 Jan 26.


Strategies to prolong the intravaginal residence time of drug delivery systems.

Baloglu E, Senyigit ZA, Karavana SY, Bernkop-Schnürch A.

J Pharm Pharm Sci. 2009;12(3):312-36. Review.


Beta2-adrenergic stimulation blunts inhibition of epithelial ion transport by hypoxia of rat alveolar epithelial cells.

Loeh B, Baloglu E, Ke A, Bärtsch P, Mairbäurl H.

Cell Physiol Biochem. 2010;25(1):123-34. doi: 10.1159/000272057. Epub 2009 Dec 22.

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