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Glycogen Synthase Kinase-3 Inhibition Sensitizes Pancreatic Cancer Cells to Chemotherapy by Abrogating the TopBP1/ATR-Mediated DNA Damage Response.

Ding L, Madamsetty VS, Kiers S, Alekhina O, Ugolkov A, Dube J, Zhang Y, Zhang JS, Wang E, Dutta SK, Schmitt DM, Giles FJ, Kozikowski AP, Mazar AP, Mukhopadhyay D, Billadeau DD.

Clin Cancer Res. 2019 Nov 1;25(21):6452-6462. doi: 10.1158/1078-0432.CCR-19-0799. Epub 2019 Sep 18.


Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT2C) receptor agonist without 5-HT2B agonism.

Zhang G, McCorvy JD, Shen S, Cheng J, Roth BL, Kozikowski AP.

Eur J Med Chem. 2019 Nov 15;182:111626. doi: 10.1016/j.ejmech.2019.111626. Epub 2019 Aug 14.


Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.

Shen S, Hadley M, Ustinova K, Pavlicek J, Knox T, Noonepalle S, Tavares MT, Zimprich CA, Zhang G, Robers MB, Bařinka C, Kozikowski AP, Villagra A.

J Med Chem. 2019 Sep 26;62(18):8557-8577. doi: 10.1021/acs.jmedchem.9b00946. Epub 2019 Sep 4.


The preclinical candidate indole-2-carboxamide improves immune responses to Mycobacterium tuberculosis infection in healthy subjects and individuals with type 2 diabetes.

Cao R, Islamoglu H, Teskey G, Gyurjian K, Abrahem R, Onajole OK, Lun S, Bishai W, Kozikowski AP, Fraix MP, Sathananthan A, Zhong L, Stec J, Venketaraman V.

Int Microbiol. 2019 Jun 19. doi: 10.1007/s10123-019-00086-0. [Epub ahead of print]


Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer.

Suri A, Bailey AW, Tavares MT, Gunosewoyo H, Dyer CP, Grupenmacher AT, Piper DR, Horton RA, Tomita T, Kozikowski AP, Roy SM, Sredni ST.

Int J Mol Sci. 2019 Apr 29;20(9). pii: E2112. doi: 10.3390/ijms20092112.


Optimization of Drug Candidates That Inhibit the D-Loop Activity of RAD51.

Budke B, Tueckmantel W, Miles K, Kozikowski AP, Connell PP.

ChemMedChem. 2019 May 17;14(10):1031-1040. doi: 10.1002/cmdc.201900075. Epub 2019 Apr 17.


Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor.

Porter NJ, Shen S, Barinka C, Kozikowski AP, Christianson DW.

ACS Med Chem Lett. 2018 Nov 21;9(12):1301-1305. doi: 10.1021/acsmedchemlett.8b00487. eCollection 2018 Dec 13.


Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and Learning Impairments in a Mouse Model of Fragile X Syndrome.

Kozikowski AP, Shen S, Pardo M, Tavares MT, Szarics D, Benoy V, Zimprich CA, Kutil Z, Zhang G, Bařinka C, Robers MB, Van Den Bosch L, Eubanks JH, Jope RS.

ACS Chem Neurosci. 2019 Mar 20;10(3):1679-1695. doi: 10.1021/acschemneuro.8b00600. Epub 2018 Dec 14.


2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics.

Nakajima R, Nováková Z, Tueckmantel W, Motlová L, Bařinka C, Kozikowski AP.

ACS Med Chem Lett. 2018 Oct 24;9(11):1099-1104. doi: 10.1021/acsmedchemlett.8b00318. eCollection 2018 Nov 8.


HDAC6 is a therapeutic target in mutant GARS-induced Charcot-Marie-Tooth disease.

Benoy V, Van Helleputte L, Prior R, d'Ydewalle C, Haeck W, Geens N, Scheveneels W, Schevenels B, Cader MZ, Talbot K, Kozikowski AP, Vanden Berghe P, Van Damme P, Robberecht W, Van Den Bosch L.

Brain. 2018 Mar 1;141(3):673-687. doi: 10.1093/brain/awx375.


Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models.

Tavares MT, Shen S, Knox T, Hadley M, Kutil Z, Bařinka C, Villagra A, Kozikowski AP.

ACS Med Chem Lett. 2017 Sep 5;8(10):1031-1036. doi: 10.1021/acsmedchemlett.7b00223. eCollection 2017 Oct 12.


Controlling Extra- and Intramacrophagic Mycobacterium abscessus by Targeting Mycolic Acid Transport.

Viljoen A, Herrmann JL, Onajole OK, Stec J, Kozikowski AP, Kremer L.

Front Cell Infect Microbiol. 2017 Sep 1;7:388. doi: 10.3389/fcimb.2017.00388. eCollection 2017.


Histone/protein deacetylase 11 targeting promotes Foxp3+ Treg function.

Huang J, Wang L, Dahiya S, Beier UH, Han R, Samanta A, Bergman J, Sotomayor EM, Seto E, Kozikowski AP, Hancock WW.

Sci Rep. 2017 Aug 17;7(1):8626. doi: 10.1038/s41598-017-09211-3.


Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.

Zhang G, Cheng J, McCorvy JD, Lorello PJ, Caldarone BJ, Roth BL, Kozikowski AP.

J Med Chem. 2017 Jul 27;60(14):6273-6288. doi: 10.1021/acs.jmedchem.7b00584. Epub 2017 Jul 18.


Targeting Mycolic Acid Transport by Indole-2-carboxamides for the Treatment of Mycobacterium abscessus Infections.

Kozikowski AP, Onajole OK, Stec J, Dupont C, Viljoen A, Richard M, Chaira T, Lun S, Bishai W, Raj VS, Ordway D, Kremer L.

J Med Chem. 2017 Jul 13;60(13):5876-5888. doi: 10.1021/acs.jmedchem.7b00582. Epub 2017 Jun 15.


Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors.

Lv W, Zhang G, Barinka C, Eubanks JH, Kozikowski AP.

ACS Med Chem Lett. 2017 Apr 7;8(5):510-515. doi: 10.1021/acsmedchemlett.7b00012. eCollection 2017 May 11.


5-HT2C Agonists Modulate Schizophrenia-Like Behaviors in Mice.

Pogorelov VM, Rodriguiz RM, Cheng J, Huang M, Schmerberg CM, Meltzer HY, Roth BL, Kozikowski AP, Wetsel WC.

Neuropsychopharmacology. 2017 Oct;42(11):2163-2177. doi: 10.1038/npp.2017.52. Epub 2017 Mar 15.


Recent Developments Using Small Molecules to Target RAD51: How to Best Modulate RAD51 for Anticancer Therapy?

Budke B, Lv W, Kozikowski AP, Connell PP.

ChemMedChem. 2016 Nov 21;11(22):2468-2473. doi: 10.1002/cmdc.201600426. Epub 2016 Oct 26. Review.


Design and Discovery of Functionally Selective Serotonin 2C (5-HT2C) Receptor Agonists.

Cheng J, McCorvy JD, Giguere PM, Zhu H, Kenakin T, Roth BL, Kozikowski AP.

J Med Chem. 2016 Nov 10;59(21):9866-9880. Epub 2016 Oct 25.


Synthesis and biological evaluation of novel hybrids of highly potent and selective α4β2-Nicotinic acetylcholine receptor (nAChR) partial agonists.

Zhang HK, Eaton JB, Fedolak A, Gunosewoyo H, Onajole OK, Brunner D, Lukas RJ, Yu LF, Kozikowski AP.

Eur J Med Chem. 2016 Nov 29;124:689-697. doi: 10.1016/j.ejmech.2016.09.016. Epub 2016 Sep 9.


Indole-2-carboxamide-based MmpL3 Inhibitors Show Exceptional Antitubercular Activity in an Animal Model of Tuberculosis Infection.

Stec J, Onajole OK, Lun S, Guo H, Merenbloom B, Vistoli G, Bishai WR, Kozikowski AP.

J Med Chem. 2016 Jul 14;59(13):6232-47. doi: 10.1021/acs.jmedchem.6b00415. Epub 2016 Jun 22.


Development of Small Molecules that Specifically Inhibit the D-loop Activity of RAD51.

Lv W, Budke B, Pawlowski M, Connell PP, Kozikowski AP.

J Med Chem. 2016 May 26;59(10):4511-25. doi: 10.1021/acs.jmedchem.5b01762. Epub 2016 Apr 21.


Synthesis and Behavioral Studies of Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile. Part III.

Onajole OK, Vallerini GP, Eaton JB, Lukas RJ, Brunner D, Caldarone BJ, Kozikowski AP.

ACS Chem Neurosci. 2016 Jun 15;7(6):811-22. doi: 10.1021/acschemneuro.6b00050. Epub 2016 Apr 21.


GSK-3β Governs Inflammation-Induced NFATc2 Signaling Hubs to Promote Pancreatic Cancer Progression.

Baumgart S, Chen NM, Zhang JS, Billadeau DD, Gaisina IN, Kozikowski AP, Singh SK, Fink D, Ströbel P, Klindt C, Zhang L, Bamlet WR, Koenig A, Hessmann E, Gress TM, Ellenrieder V, Neesse A.

Mol Cancer Ther. 2016 Mar;15(3):491-502. doi: 10.1158/1535-7163.MCT-15-0309. Epub 2016 Jan 28.


Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.

Cheng J, Giguere PM, Schmerberg CM, Pogorelov VM, Rodriguiz RM, Huang XP, Zhu H, McCorvy JD, Wetsel WC, Roth BL, Kozikowski AP.

J Med Chem. 2016 Jan 28;59(2):578-91. doi: 10.1021/acs.jmedchem.5b01153. Epub 2016 Jan 13.


Exploration of the labeling of [11C]tubastatin A at the hydroxamic acid site with [11C]carbon monoxide.

Lu S, Zhang Y, Kalin JH, Cai L, Kozikowski AP, Pike VW.

J Labelled Comp Radiopharm. 2016 Jan;59(1):9-13. doi: 10.1002/jlcr.3360. Epub 2015 Dec 8.


Thiol-Based Potent and Selective HDAC6 Inhibitors Promote Tubulin Acetylation and T-Regulatory Cell Suppressive Function.

Segretti MC, Vallerini GP, Brochier C, Langley B, Wang L, Hancock WW, Kozikowski AP.

ACS Med Chem Lett. 2015 Oct 5;6(11):1156-61. doi: 10.1021/acsmedchemlett.5b00303. eCollection 2015 Nov 12.


Why Hydroxamates May Not Be the Best Histone Deacetylase Inhibitors--What Some May Have Forgotten or Would Rather Forget?

Shen S, Kozikowski AP.

ChemMedChem. 2016 Jan 5;11(1):15-21. doi: 10.1002/cmdc.201500486. Epub 2015 Nov 25.


Bicyclic-Capped Histone Deacetylase 6 Inhibitors with Improved Activity in a Model of Axonal Charcot-Marie-Tooth Disease.

Shen S, Benoy V, Bergman JA, Kalin JH, Frojuello M, Vistoli G, Haeck W, Van Den Bosch L, Kozikowski AP.

ACS Chem Neurosci. 2016 Feb 17;7(2):240-58. doi: 10.1021/acschemneuro.5b00286. Epub 2015 Dec 7.


Identification of HDAC6-Selective Inhibitors of Low Cancer Cell Cytotoxicity.

Gaisina IN, Tueckmantel W, Ugolkov A, Shen S, Hoffen J, Dubrovskyi O, Mazar A, Schoon RA, Billadeau D, Kozikowski AP.

ChemMedChem. 2016 Jan 5;11(1):81-92. doi: 10.1002/cmdc.201500456. Epub 2015 Nov 23.


We Need 2C but Not 2B: Developing Serotonin 2C (5-HT2C) Receptor Agonists for the Treatment of CNS Disorders.

Cheng J, Kozikowski AP.

ChemMedChem. 2015 Dec;10(12):1963-7. doi: 10.1002/cmdc.201500437. Epub 2015 Oct 28.


Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.

Cheng J, Giguère PM, Onajole OK, Lv W, Gaisin A, Gunosewoyo H, Schmerberg CM, Pogorelov VM, Rodriguiz RM, Vistoli G, Wetsel WC, Roth BL, Kozikowski AP.

J Med Chem. 2015 Feb 26;58(4):1992-2002. doi: 10.1021/jm5019274. Epub 2015 Feb 10.


The potent and selective α4β2*/α6*-nicotinic acetylcholine receptor partial agonist 2-[5-[5-((S)Azetidin-2-ylmethoxy)-3-pyridinyl]-3-isoxazolyl]ethanol demonstrates antidepressive-like behavior in animal models and a favorable ADME-tox profile.

Yu LF, Brek Eaton J, Zhang HK, Sabath E, Hanania T, Li GN, van Breemen RB, Whiteaker P, Liu Q, Wu J, Chang YC, Lukas RJ, Brunner D, Kozikowski AP.

Pharmacol Res Perspect. 2014 Apr;2(2):e00026. doi: 10.1002/prp2.26. Epub 2014 Mar 12.


Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands.

Onajole OK, Eaton JB, Lukas RJ, Brunner D, Thiede L, Caldarone BJ, Kozikowski AP.

ACS Med Chem Lett. 2014 Sep 29;5(11):1196-201. doi: 10.1021/ml500129k. eCollection 2014 Nov 13.


Biological evaluation of potent triclosan-derived inhibitors of the enoyl-acyl carrier protein reductase InhA in drug-sensitive and drug-resistant strains of Mycobacterium tuberculosis.

Stec J, Vilchèze C, Lun S, Perryman AL, Wang X, Freundlich JS, Bishai W, Jacobs WR Jr, Kozikowski AP.

ChemMedChem. 2014 Nov;9(11):2528-37. doi: 10.1002/cmdc.201402255. Epub 2014 Aug 27.


Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.

Yu LF, Zhang HK, Caldarone BJ, Eaton JB, Lukas RJ, Kozikowski AP.

J Med Chem. 2014 Oct 23;57(20):8204-23. doi: 10.1021/jm401937a. Epub 2014 Jul 2. Review.


The RAD51-stimulatory compound RS-1 can exploit the RAD51 overexpression that exists in cancer cells and tumors.

Mason JM, Logan HL, Budke B, Wu M, Pawlowski M, Weichselbaum RR, Kozikowski AP, Bishop DK, Connell PP.

Cancer Res. 2014 Jul 1;74(13):3546-55. doi: 10.1158/0008-5472.CAN-13-3220. Epub 2014 Apr 21.


A selective histone deacetylase-6 inhibitor improves BDNF trafficking in hippocampal neurons from Mecp2 knockout mice: implications for Rett syndrome.

Xu X, Kozikowski AP, Pozzo-Miller L.

Front Cell Neurosci. 2014 Mar 7;8:68. doi: 10.3389/fncel.2014.00068. eCollection 2014.


Indoleamides are active against drug-resistant Mycobacterium tuberculosis.

Lun S, Guo H, Onajole OK, Pieroni M, Gunosewoyo H, Chen G, Tipparaju SK, Ammerman NC, Kozikowski AP, Bishai WR.

Nat Commun. 2013;4:2907. doi: 10.1038/ncomms3907.


Inhibition of GSK-3 induces differentiation and impaired glucose metabolism in renal cancer.

Pal K, Cao Y, Gaisina IN, Bhattacharya S, Dutta SK, Wang E, Gunosewoyo H, Kozikowski AP, Billadeau DD, Mukhopadhyay D.

Mol Cancer Ther. 2014 Feb;13(2):285-96. doi: 10.1158/1535-7163.MCT-13-0681. Epub 2013 Dec 10.


Discrimination of potent inhibitors of Toxoplasma gondii enoyl-acyl carrier protein reductase by a thermal shift assay.

Afanador GA, Muench SP, McPhillie M, Fomovska A, Schön A, Zhou Y, Cheng G, Stec J, Freundlich JS, Shieh HM, Anderson JW, Jacobus DP, Fidock DA, Kozikowski AP, Fishwick CW, Rice DW, Freire E, McLeod R, Prigge ST.

Biochemistry. 2013 Dec 23;52(51):9155-66. doi: 10.1021/bi400945y. Epub 2013 Dec 13.


A microenvironment-mediated c-Myc/miR-548m/HDAC6 amplification loop in non-Hodgkin B cell lymphomas.

Lwin T, Zhao X, Cheng F, Zhang X, Huang A, Shah B, Zhang Y, Moscinski LC, Choi YS, Kozikowski AP, Bradner JE, Dalton WS, Sotomayor E, Tao J.

J Clin Invest. 2013 Nov;123(11):4612-26.


Epigenetic regulation of autophagy by the methyltransferase G9a.

Artal-Martinez de Narvajas A, Gomez TS, Zhang JS, Mann AO, Taoda Y, Gorman JA, Herreros-Villanueva M, Gress TM, Ellenrieder V, Bujanda L, Kim DH, Kozikowski AP, Koenig A, Billadeau DD.

Mol Cell Biol. 2013 Oct;33(20):3983-93. doi: 10.1128/MCB.00813-13. Epub 2013 Aug 5.


Modification of triclosan scaffold in search of improved inhibitors for enoyl-acyl carrier protein (ACP) reductase in Toxoplasma gondii.

Stec J, Fomovska A, Afanador GA, Muench SP, Zhou Y, Lai BS, El Bissati K, Hickman MR, Lee PJ, Leed SE, Auschwitz JM, Sommervile C, Woods S, Roberts CW, Rice D, Prigge ST, McLeod R, Kozikowski AP.

ChemMedChem. 2013 Jul;8(7):1138-60. doi: 10.1002/cmdc.201300050. Epub 2013 Jun 14.


Chemistry, pharmacology, and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile. Part II.

Zhang HK, Yu LF, Eaton JB, Whiteaker P, Onajole OK, Hanania T, Brunner D, Lukas RJ, Kozikowski AP.

J Med Chem. 2013 Jul 11;56(13):5495-504. doi: 10.1021/jm400510u. Epub 2013 Jun 26.


Characterization of maleimide-based glycogen synthase kinase-3 (GSK-3) inhibitors as stimulators of steroidogenesis.

Gunosewoyo H, Midzak A, Gaisina IN, Sabath EV, Fedolak A, Hanania T, Brunner D, Papadopoulos V, Kozikowski AP.

J Med Chem. 2013 Jun 27;56(12):5115-29. doi: 10.1021/jm400511s. Epub 2013 Jun 17.


From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design.

Yu LF, Zhang HK, Gunosewoyo H, Kozikowski AP.

ACS Med Chem Lett. 2012 Dec 13;3(12):1054-1058.


Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.

Onajole OK, Pieroni M, Tipparaju SK, Lun S, Stec J, Chen G, Gunosewoyo H, Guo H, Ammerman NC, Bishai WR, Kozikowski AP.

J Med Chem. 2013 May 23;56(10):4093-103. doi: 10.1021/jm4003878. Epub 2013 May 3.


Structural analogs of huperzine A improve survival in guinea pigs exposed to soman.

Gunosewoyo H, Tipparaju SK, Pieroni M, Wang Y, Doctor BP, Nambiar MP, Kozikowski AP.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1544-7. doi: 10.1016/j.bmcl.2012.11.083. Epub 2012 Dec 1.


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