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Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.

Kearney SE, Zahoránszky-Kőhalmi G, Brimacombe KR, Henderson MJ, Lynch C, Zhao T, Wan KK, Itkin Z, Dillon C, Shen M, Cheff DM, Lee TD, Bougie D, Cheng K, Coussens NP, Dorjsuren D, Eastman RT, Huang R, Iannotti MJ, Karavadhi S, Klumpp-Thomas C, Roth JS, Sakamuru S, Sun W, Titus SA, Yasgar A, Zhang YQ, Zhao J, Andrade RB, Brown MK, Burns NZ, Cha JK, Mevers EE, Clardy J, Clement JA, Crooks PA, Cuny GD, Ganor J, Moreno J, Morrill LA, Picazo E, Susick RB, Garg NK, Goess BC, Grossman RB, Hughes CC, Johnston JN, Joullie MM, Kinghorn AD, Kingston DGI, Krische MJ, Kwon O, Maimone TJ, Majumdar S, Maloney KN, Mohamed E, Murphy BT, Nagorny P, Olson DE, Overman LE, Brown LE, Snyder JK, Porco JA Jr, Rivas F, Ross SA, Sarpong R, Sharma I, Shaw JT, Xu Z, Shen B, Shi W, Stephenson CRJ, Verano AL, Tan DS, Tang Y, Taylor RE, Thomson RJ, Vosburg DA, Wu J, Wuest WM, Zakarian A, Zhang Y, Ren T, Zuo Z, Inglese J, Michael S, Simeonov A, Zheng W, Shinn P, Jadhav A, Boxer MB, Hall MD, Xia M, Guha R, Rohde JM.

ACS Cent Sci. 2018 Dec 26;4(12):1727-1741. doi: 10.1021/acscentsci.8b00747. Epub 2018 Dec 5.


Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.

Jiang JK, Huang X, Shamim K, Patel PR, Lee A, Wang AQ, Nguyen K, Tawa G, Cuny GD, Yu PB, Zheng W, Xu X, Sanderson P, Huang W.

Bioorg Med Chem Lett. 2018 Nov 1;28(20):3356-3362. doi: 10.1016/j.bmcl.2018.09.006. Epub 2018 Sep 6.


Discovery of 7-hydroxyaporphines as conformationally restricted ligands for beta-1 and beta-2 adrenergic receptors.

Ku AF, Cuny GD.

Medchemcomm. 2018 Jan 22;9(2):353-356. doi: 10.1039/c7md00656j. eCollection 2018 Feb 1.


Small molecule inhibitors reveal an indispensable scaffolding role of RIPK2 in NOD2 signaling.

Hrdinka M, Schlicher L, Dai B, Pinkas DM, Bufton JC, Picaud S, Ward JA, Rogers C, Suebsuwong C, Nikhar S, Cuny GD, Huber KV, Filippakopoulos P, Bullock AN, Degterev A, Gyrd-Hansen M.

EMBO J. 2018 Sep 3;37(17). pii: e99372. doi: 10.15252/embj.201899372. Epub 2018 Jul 19.


Expanding Benzoxazole-Based Inosine 5'-Monophosphate Dehydrogenase (IMPDH) Inhibitor Structure-Activity As Potential Antituberculosis Agents.

Chacko S, Boshoff HIM, Singh V, Ferraris DM, Gollapalli DR, Zhang M, Lawson AP, Pepi MJ, Joachimiak A, Rizzi M, Mizrahi V, Cuny GD, Hedstrom L.

J Med Chem. 2018 Jun 14;61(11):4739-4756. doi: 10.1021/acs.jmedchem.7b01839. Epub 2018 May 30.


Activation loop targeting strategy for design of receptor-interacting protein kinase 2 (RIPK2) inhibitors.

Suebsuwong C, Pinkas DM, Ray SS, Bufton JC, Dai B, Bullock AN, Degterev A, Cuny GD.

Bioorg Med Chem Lett. 2018 Feb 15;28(4):577-583. doi: 10.1016/j.bmcl.2018.01.044. Epub 2018 Jan 31.


Optimization of a series of heterocycles as survival motor neuron gene transcription enhancers.

Choi S, Calder AN, Miller EH, Anderson KP, Fiejtek DK, Rietz A, Li H, Cherry JJ, Quist KM, Xing X, Glicksman MA, Cuny GD, Lorson CL, Androphy EA, Hodgetts KJ.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5144-5148. doi: 10.1016/j.bmcl.2017.10.066. Epub 2017 Oct 26.


Benzoxazoles, Phthalazinones, and Arylurea-Based Compounds with IMP Dehydrogenase-Independent Antibacterial Activity against Francisella tularensis.

Gorla SK, Zhang Y, Rabideau MM, Qin A, Chacko S, House AL, Johnson CR, Mandapati K, Bernstein HM, McKenney ES, Boshoff H, Zhang M, Glomski IJ, Goldberg JB, Cuny GD, Mann BJ, Hedstrom L.

Antimicrob Agents Chemother. 2017 Sep 22;61(10). pii: e00939-17. doi: 10.1128/AAC.00939-17. Print 2017 Oct.


Discovery of a Small Molecule Probe That Post-Translationally Stabilizes the Survival Motor Neuron Protein for the Treatment of Spinal Muscular Atrophy.

Rietz A, Li H, Quist KM, Cherry JJ, Lorson CL, Burnett BG, Kern NL, Calder AN, Fritsche M, Lusic H, Boaler PJ, Choi S, Xing X, Glicksman MA, Cuny GD, Androphy EJ, Hodgetts KJ.

J Med Chem. 2017 Jun 8;60(11):4594-4610. doi: 10.1021/acs.jmedchem.6b01885. Epub 2017 May 19.


Inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitors: a patent and scientific literature review (2002-2016).

Cuny GD, Suebsuwong C, Ray SS.

Expert Opin Ther Pat. 2017 Jun;27(6):677-690. doi: 10.1080/13543776.2017.1280463. Epub 2017 Jan 27. Review.


Access to 6a-Alkyl Aporphines: Synthesis of (±)-N-Methylguattescidine.

Ku AF, Cuny GD.

J Org Chem. 2016 Oct 21;81(20):10062-10070. Epub 2016 Sep 30.


Divergent Approach for the Synthesis of Gombamide A and Derivatives.

Vippila MR, Nikhar S, Gracia AP, Cuny GD.

Org Lett. 2016 Sep 16;18(18):4726-9. doi: 10.1021/acs.orglett.6b02379. Epub 2016 Sep 7.


Synthesis and Antiproliferative Activity Evaluation of the Disulfide-Containing Cyclic Peptide Thiochondrilline C and Derivatives.

Vippila MR, Ly PK, Cuny GD.

J Nat Prod. 2015 Oct 23;78(10):2398-404. doi: 10.1021/acs.jnatprod.5b00428. Epub 2015 Oct 7.


Mycobacterium tuberculosis IMPDH in Complexes with Substrates, Products and Antitubercular Compounds.

Makowska-Grzyska M, Kim Y, Gorla SK, Wei Y, Mandapati K, Zhang M, Maltseva N, Modi G, Boshoff HI, Gu M, Aldrich C, Cuny GD, Hedstrom L, Joachimiak A.

PLoS One. 2015 Oct 6;10(10):e0138976. doi: 10.1371/journal.pone.0138976. eCollection 2015.


Inflammatory Signaling by NOD-RIPK2 Is Inhibited by Clinically Relevant Type II Kinase Inhibitors.

Canning P, Ruan Q, Schwerd T, Hrdinka M, Maki JL, Saleh D, Suebsuwong C, Ray S, Brennan PE, Cuny GD, Uhlig HH, Gyrd-Hansen M, Degterev A, Bullock AN.

Chem Biol. 2015 Sep 17;22(9):1174-84. doi: 10.1016/j.chembiol.2015.07.017. Epub 2015 Aug 27.


Discovery of LRRK2 inhibitors using sequential in silico joint pharmacophore space (JPS) and ensemble docking.

Lang CA, Ray SS, Liu M, Singh AK, Cuny GD.

Bioorg Med Chem Lett. 2015 Jul 1;25(13):2713-9. doi: 10.1016/j.bmcl.2015.04.027. Epub 2015 Apr 16.


Structure of Cryptosporidium IMP dehydrogenase bound to an inhibitor with in vivo antiparasitic activity.

Kim Y, Makowska-Grzyska M, Gorla SK, Gollapalli DR, Cuny GD, Joachimiak A, Hedstrom L.

Acta Crystallogr F Struct Biol Commun. 2015 May;71(Pt 5):531-8. doi: 10.1107/S2053230X15000187. Epub 2015 Apr 21.


Structure guided design of potent and selective ponatinib-based hybrid inhibitors for RIPK1.

Najjar M, Suebsuwong C, Ray SS, Thapa RJ, Maki JL, Nogusa S, Shah S, Saleh D, Gough PJ, Bertin J, Yuan J, Balachandran S, Cuny GD, Degterev A.

Cell Rep. 2015 Mar 24;10(11):1850-60.


Restored glial glutamate transporter EAAT2 function as a potential therapeutic approach for Alzheimer's disease.

Takahashi K, Kong Q, Lin Y, Stouffer N, Schulte DA, Lai L, Liu Q, Chang LC, Dominguez S, Xing X, Cuny GD, Hodgetts KJ, Glicksman MA, Lin CL.

J Exp Med. 2015 Mar 9;212(3):319-32. doi: 10.1084/jem.20140413. Epub 2015 Feb 23.


Synthetic studies of 7-oxygenated aporphine alkaloids: preparation of (-)-oliveroline, (-)-nornuciferidine, and derivatives.

Ku AF, Cuny GD.

Org Lett. 2015 Mar 6;17(5):1134-7. doi: 10.1021/acs.orglett.5b00007. Epub 2015 Feb 24.


Synthesis, in vitro evaluation and cocrystal structure of 4-oxo-[1]benzopyrano[4,3-c]pyrazole Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase (CpIMPDH) inhibitors.

Sun Z, Khan J, Makowska-Grzyska M, Zhang M, Cho JH, Suebsuwong C, Vo P, Gollapalli DR, Kim Y, Joachimiak A, Hedstrom L, Cuny GD.

J Med Chem. 2014 Dec 26;57(24):10544-50. doi: 10.1021/jm501527z. Epub 2014 Dec 4.


Repurposing cryptosporidium inosine 5'-monophosphate dehydrogenase inhibitors as potential antibacterial agents.

Mandapati K, Gorla SK, House AL, McKenney ES, Zhang M, Rao SN, Gollapalli DR, Mann BJ, Goldberg JB, Cuny GD, Glomski IJ, Hedstrom L.

ACS Med Chem Lett. 2014 Jun 10;5(8):846-50. doi: 10.1021/ml500203p. eCollection 2014 Aug 14. Erratum in: ACS Med Chem Lett. 2014 Oct 9;5(10):1174.


Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.

Mohedas AH, Wang Y, Sanvitale CE, Canning P, Choi S, Xing X, Bullock AN, Cuny GD, Yu PB.

J Med Chem. 2014 Oct 9;57(19):7900-15. doi: 10.1021/jm501177w. Epub 2014 Sep 4.


Inhibitor of the tyrosine phosphatase STEP reverses cognitive deficits in a mouse model of Alzheimer's disease.

Xu J, Chatterjee M, Baguley TD, Brouillette J, Kurup P, Ghosh D, Kanyo J, Zhang Y, Seyb K, Ononenyi C, Foscue E, Anderson GM, Gresack J, Cuny GD, Glicksman MA, Greengard P, Lam TT, Tautz L, Nairn AC, Ellman JA, Lombroso PJ.

PLoS Biol. 2014 Aug 5;12(8):e1001923. doi: 10.1371/journal.pbio.1001923. eCollection 2014 Aug.


Enzymatic Characterization of ER Stress-Dependent Kinase, PERK, and Development of a High-Throughput Assay for Identification of PERK Inhibitors.

Pytel D, Seyb K, Liu M, Ray SS, Concannon J, Huang M, Cuny GD, Diehl JA, Glicksman MA.

J Biomol Screen. 2014 Aug;19(7):1024-34. doi: 10.1177/1087057114525853. Epub 2014 Mar 5.


Small-molecule activator of glutamate transporter EAAT2 translation provides neuroprotection.

Kong Q, Chang LC, Takahashi K, Liu Q, Schulte DA, Lai L, Ibabao B, Lin Y, Stouffer N, Das Mukhopadhyay C, Xing X, Seyb KI, Cuny GD, Glicksman MA, Lin CL.

J Clin Invest. 2014 Mar;124(3):1255-67. doi: 10.1172/JCI66163. Epub 2014 Feb 24.


Validation of IMP dehydrogenase inhibitors in a mouse model of cryptosporidiosis.

Gorla SK, McNair NN, Yang G, Gao S, Hu M, Jala VR, Haribabu B, Striepen B, Cuny GD, Mead JR, Hedstrom L.

Antimicrob Agents Chemother. 2014;58(3):1603-14. doi: 10.1128/AAC.02075-13. Epub 2013 Dec 23.


Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells.

Mistry H, Hsieh G, Buhrlage SJ, Huang M, Park E, Cuny GD, Galinsky I, Stone RM, Gray NS, D'Andrea AD, Parmar K.

Mol Cancer Ther. 2013 Dec;12(12):2651-62. doi: 10.1158/1535-7163.MCT-13-0103-T. Epub 2013 Oct 15.


A mild, one-pot Stadler-Ziegler synthesis of arylsulfides facilitated by photoredox catalysis in batch and continuous-flow.

Wang X, Cuny GD, Noël T.

Angew Chem Int Ed Engl. 2013 Jul 22;52(30):7860-4. doi: 10.1002/anie.201303483. Epub 2013 Jun 19.


Enhancement of SMN protein levels in a mouse model of spinal muscular atrophy using novel drug-like compounds.

Cherry JJ, Osman EY, Evans MC, Choi S, Xing X, Cuny GD, Glicksman MA, Lorson CL, Androphy EJ.

EMBO Mol Med. 2013 Jul;5(7):1103-18. doi: 10.1002/emmm.201202305. Epub 2013 Jun 5.


Diaminothiazoles modify Tau phosphorylation and improve the tauopathy in mouse models.

Zhang X, Hernandez I, Rei D, Mair W, Laha JK, Cornwell ME, Cuny GD, Tsai LH, Steen JA, Kosik KS.

J Biol Chem. 2013 Jul 26;288(30):22042-56. doi: 10.1074/jbc.M112.436402. Epub 2013 Jun 4.


Optimization of benzoxazole-based inhibitors of Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase.

Gorla SK, Kavitha M, Zhang M, Chin JE, Liu X, Striepen B, Makowska-Grzyska M, Kim Y, Joachimiak A, Hedstrom L, Cuny GD.

J Med Chem. 2013 May 23;56(10):4028-43. doi: 10.1021/jm400241j. Epub 2013 May 13.


A new class of small molecule inhibitor of BMP signaling.

Sanvitale CE, Kerr G, Chaikuad A, Ramel MC, Mohedas AH, Reichert S, Wang Y, Triffitt JT, Cuny GD, Yu PB, Hill CS, Bullock AN.

PLoS One. 2013 Apr 30;8(4):e62721. doi: 10.1371/journal.pone.0062721. Print 2013.


Development of an ALK2-biased BMP type I receptor kinase inhibitor.

Mohedas AH, Xing X, Armstrong KA, Bullock AN, Cuny GD, Yu PB.

ACS Chem Biol. 2013;8(6):1291-302. doi: 10.1021/cb300655w. Epub 2013 Apr 30.


Expression and purification of active receptor interacting protein 1 kinase using a baculovirus system.

Maki JL, Tres Brazell J, Teng X, Cuny GD, Degterev A.

Protein Expr Purif. 2013 Jun;89(2):156-61. doi: 10.1016/j.pep.2013.03.002. Epub 2013 Mar 21.


Akt Regulates TNFα synthesis downstream of RIP1 kinase activation during necroptosis.

McNamara CR, Ahuja R, Osafo-Addo AD, Barrows D, Kettenbach A, Skidan I, Teng X, Cuny GD, Gerber S, Degterev A.

PLoS One. 2013;8(3):e56576. doi: 10.1371/journal.pone.0056576. Epub 2013 Mar 1.


Type II kinase inhibitors show an unexpected inhibition mode against Parkinson's disease-linked LRRK2 mutant G2019S.

Liu M, Bender SA, Cuny GD, Sherman W, Glicksman M, Ray SS.

Biochemistry. 2013 Mar 12;52(10):1725-36. doi: 10.1021/bi3012077. Epub 2013 Mar 1.


Phthalazinone inhibitors of inosine-5'-monophosphate dehydrogenase from Cryptosporidium parvum.

Johnson CR, Gorla SK, Kavitha M, Zhang M, Liu X, Striepen B, Mead JR, Cuny GD, Hedstrom L.

Bioorg Med Chem Lett. 2013 Feb 15;23(4):1004-7. doi: 10.1016/j.bmcl.2012.12.037. Epub 2012 Dec 27.


Selective and potent urea inhibitors of cryptosporidium parvum inosine 5'-monophosphate dehydrogenase.

Gorla SK, Kavitha M, Zhang M, Liu X, Sharling L, Gollapalli DR, Striepen B, Hedstrom L, Cuny GD.

J Med Chem. 2012 Sep 13;55(17):7759-71. doi: 10.1021/jm3007917. Epub 2012 Sep 5.


Glutamate transporter EAAT2: a new target for the treatment of neurodegenerative diseases.

Lin CL, Kong Q, Cuny GD, Glicksman MA.

Future Med Chem. 2012 Sep;4(13):1689-700. doi: 10.4155/fmc.12.122.


Small-molecule Klotho enhancers as novel treatment of neurodegeneration.

Abraham CR, Chen C, Cuny GD, Glicksman MA, Zeldich E.

Future Med Chem. 2012 Sep;4(13):1671-9. doi: 10.4155/fmc.12.134.


Foreword: neurodegenerative diseases: challenges and opportunities.

Cuny GD.

Future Med Chem. 2012 Sep;4(13):1647-9. doi: 10.4155/fmc.12.123. No abstract available.


Optimization of tricyclic Nec-3 necroptosis inhibitors for in vitro liver microsomal stability.

Choi S, Keys H, Staples RJ, Yuan J, Degterev A, Cuny GD.

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5685-8. doi: 10.1016/j.bmcl.2012.06.098. Epub 2012 Jul 6.


Lowering of amyloid beta peptide production with a small molecule inhibitor of amyloid-β precursor protein dimerization.

So PP, Zeldich E, Seyb KI, Huang MM, Concannon JB, King GD, Chen CD, Cuny GD, Glicksman MA, Abraham CR.

Am J Neurodegener Dis. 2012;1(1):75-87.


Fluorescence polarization assay for inhibitors of the kinase domain of receptor interacting protein 1.

Maki JL, Smith EE, Teng X, Ray SS, Cuny GD, Degterev A.

Anal Biochem. 2012 Aug 15;427(2):164-74. doi: 10.1016/j.ab.2012.05.019. Epub 2012 May 29.


A high-throughput screen to identify inhibitors of SOD1 transcription.

Wright PD, Wightman N, Huang M, Weiss A, Sapp PC, Cuny GD, Ivinson AJ, Glicksman MA, Ferrante RJ, Matson W, Matson S, Brown RH Jr.

Front Biosci (Elite Ed). 2012 Jun 1;4:2701-8.


Synthesis of tetracyclic indoles via intramolecular α-arylation of ketones.

Hellal M, Singh S, Cuny GD.

J Org Chem. 2012 Apr 20;77(8):4123-30. doi: 10.1021/jo300052z. Epub 2012 Apr 5.


Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors.

Cuny GD, Ulyanova NP, Patnaik D, Liu JF, Lin X, Auerbach K, Ray SS, Xian J, Glicksman MA, Stein RL, Higgins JM.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):2015-9. doi: 10.1016/j.bmcl.2012.01.028. Epub 2012 Jan 28.


Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH.

Kirubakaran S, Gorla SK, Sharling L, Zhang M, Liu X, Ray SS, Macpherson IS, Striepen B, Hedstrom L, Cuny GD.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1985-8. doi: 10.1016/j.bmcl.2012.01.029. Epub 2012 Jan 24.


Identification of novel compounds that increase SMN protein levels using an improved SMN2 reporter cell assay.

Cherry JJ, Evans MC, Ni J, Cuny GD, Glicksman MA, Androphy EJ.

J Biomol Screen. 2012 Apr;17(4):481-95. doi: 10.1177/1087057111431605. Epub 2012 Jan 10.

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