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Specific RITA Modification Produces Hyperselective Cytotoxicity While Maintaining In Vivo Antitumor Efficacy.

Peyser BD, Hermone A, Salamoun JM, Burnett JC, Hollingshead MG, McGrath CF, Gussio R, Wipf P.

Mol Cancer Ther. 2019 Oct;18(10):1765-1774. doi: 10.1158/1535-7163.MCT-19-0185. Epub 2019 Jul 24.


Modified carbazoles destabilize microtubules and kill glioblastoma multiform cells.

Diaz P, Horne E, Xu C, Hamel E, Wagenbach M, Petrov RR, Uhlenbruck B, Haas B, Hothi P, Wordeman L, Gussio R, Stella N.

Eur J Med Chem. 2018 Nov 5;159:74-89. doi: 10.1016/j.ejmech.2018.09.026. Epub 2018 Sep 11.


A threonine turnstile defines a dynamic amphiphilic binding motif in the AAA ATPase p97 allosteric binding site.

Burnett JC, Lim C, Peyser BD, Samankumara LP, Kovaliov M, Colombo R, Bulfer SL, LaPorte MG, Hermone AR, McGrath CF, Arkin MR, Gussio R, Huryn DM, Wipf P.

Org Biomol Chem. 2017 May 16;15(19):4096-4114. doi: 10.1039/c7ob00526a.


Phosphatase Inhibitors Function as Novel, Broad Spectrum Botulinum Neurotoxin Antagonists in Mouse and Human Embryonic Stem Cell-Derived Motor Neuron-Based Assays.

Kiris E, Nuss JE, Stanford SM, Wanner LM, Cazares L, Maestre MF, Du HT, Gomba GY, Burnett JC, Gussio R, Bottini N, Panchal RG, Kane CD, Tessarollo L, Bavari S.

PLoS One. 2015 Jun 10;10(6):e0129264. doi: 10.1371/journal.pone.0129264. eCollection 2015.


SRC family kinase inhibitors antagonize the toxicity of multiple serotypes of botulinum neurotoxin in human embryonic stem cell-derived motor neurons.

Kiris E, Burnett JC, Nuss JE, Wanner LM, Peyser BD, Du HT, Gomba GY, Kota KP, Panchal RG, Gussio R, Kane CD, Tessarollo L, Bavari S.

Neurotox Res. 2015 May;27(4):384-98. doi: 10.1007/s12640-015-9526-z. Epub 2015 Mar 18.


Synthesis of heterocyclic triads by Pd-catalyzed cross-couplings and evaluation of their cell-specific toxicity profile.

Salamoun J, Anderson S, Burnett JC, Gussio R, Wipf P.

Org Lett. 2014 Apr 4;16(7):2034-7. doi: 10.1021/ol500620m. Epub 2014 Mar 18.


Anthrax toxin-induced rupture of artificial lipid bilayer membranes.

Nablo BJ, Panchal RG, Bavari S, Nguyen TL, Gussio R, Ribot W, Friedlander A, Chabot D, Reiner JE, Robertson JW, Balijepalli A, Halverson KM, Kasianowicz JJ.

J Chem Phys. 2013 Aug 14;139(6):065101. doi: 10.1063/1.4816467.


Interaction of pseudolaric acid B with the colchicine site of tubulin.

Sarkar T, Nguyen TL, Su ZW, Hao J, Bai R, Gussio R, Qiu SX, Hamel E.

Biochem Pharmacol. 2012 Aug 15;84(4):444-50. doi: 10.1016/j.bcp.2012.05.014. Epub 2012 May 23.


The synthesis of 2,5-bis(4-amidinophenyl)thiophene derivatives providing submicromolar-range inhibition of the botulinum neurotoxin serotype A metalloprotease.

Opsenica I, Filipovic V, Nuss JE, Gomba LM, Opsenica D, Burnett JC, Gussio R, Solaja BA, Bavari S.

Eur J Med Chem. 2012 Jul;53:374-9. doi: 10.1016/j.ejmech.2012.03.043. Epub 2012 Mar 30.


Evading Pgp activity in drug-resistant cancer cells: a structural and functional study of antitubulin furan metotica compounds.

Nguyen TL, Cera MR, Pinto A, Lo Presti L, Hamel E, Conti P, Gussio R, De Wulf P.

Mol Cancer Ther. 2012 May;11(5):1103-11. doi: 10.1158/1535-7163.MCT-11-1018. Epub 2012 Mar 21.


A pharmacologic inhibitor of the protease Taspase1 effectively inhibits breast and brain tumor growth.

Chen DY, Lee Y, Van Tine BA, Searleman AC, Westergard TD, Liu H, Tu HC, Takeda S, Dong Y, Piwnica-Worms DR, Oh KJ, Korsmeyer SJ, Hermone A, Gussio R, Shoemaker RH, Cheng EH, Hsieh JJ.

Cancer Res. 2012 Feb 1;72(3):736-46. doi: 10.1158/0008-5472.CAN-11-2584. Epub 2011 Dec 13.


Interactions of halichondrin B and eribulin with tubulin.

Bai R, Nguyen TL, Burnett JC, Atasoylu O, Munro MH, Pettit GR, Smith AB 3rd, Gussio R, Hamel E.

J Chem Inf Model. 2011 Jun 27;51(6):1393-404. doi: 10.1021/ci200077t. Epub 2011 May 13.


Embryonic stem cell-derived motoneurons provide a highly sensitive cell culture model for botulinum neurotoxin studies, with implications for high-throughput drug discovery.

Kiris E, Nuss JE, Burnett JC, Kota KP, Koh DC, Wanner LM, Torres-Melendez E, Gussio R, Tessarollo L, Bavari S.

Stem Cell Res. 2011 May;6(3):195-205. doi: 10.1016/j.scr.2011.01.002. Epub 2011 Jan 19.


A chemotype that inhibits three unrelated pathogenic targets: the botulinum neurotoxin serotype A light chain, P. falciparum malaria, and the Ebola filovirus.

Opsenica I, Burnett JC, Gussio R, Opsenica D, Todorović N, Lanteri CA, Sciotti RJ, Gettayacamin M, Basilico N, Taramelli D, Nuss JE, Wanner L, Panchal RG, Solaja BA, Bavari S.

J Med Chem. 2011 Mar 10;54(5):1157-69. doi: 10.1021/jm100938u. Epub 2011 Jan 25.


Pharmacophore Refinement Guides the Rational Design of Nanomolar-Range Inhibitors of the Botulinum Neurotoxin Serotype A Metalloprotease.

Nuss JE, Dong Y, Wanner LM, Ruthel G, Wipf P, Gussio R, Vennerstrom JL, Bavari S, Burnett JC.

ACS Med Chem Lett. 2010 Oct 14;1(7):301-305.


The assembly-inducing laulimalide/peloruside a binding site on tubulin: molecular modeling and biochemical studies with [³H]peloruside A.

Nguyen TL, Xu X, Gussio R, Ghosh AK, Hamel E.

J Chem Inf Model. 2010 Nov 22;50(11):2019-28. doi: 10.1021/ci1002894. Epub 2010 Oct 28.


A screen for kinetochore-microtubule interaction inhibitors identifies novel antitubulin compounds.

Screpanti E, Santaguida S, Nguyen T, Silvestri R, Gussio R, Musacchio A, Hamel E, De Wulf P.

PLoS One. 2010 Jul 15;5(7):e11603. doi: 10.1371/journal.pone.0011603.


Iterative structure-based peptide-like inhibitor design against the botulinum neurotoxin serotype A.

Zuniga JE, Hammill JT, Drory O, Nuss JE, Burnett JC, Gussio R, Wipf P, Bavari S, Brunger AT.

PLoS One. 2010 Jun 30;5(6):e11378. doi: 10.1371/journal.pone.0011378.


RSK2 Binding Models Delineate Key Features for Activity.

Gussio R, Currens MJ, Scudiero DA, Smith JA, Lannigan DA, Shoemaker RH, Zaharevitz DW, Nguyen TL.

J Chem Pharm Res. 2010;2(5):587-598.


Pharmacophore-guided lead optimization: the rational design of a non-zinc coordinating, sub-micromolar inhibitor of the botulinum neurotoxin serotype a metalloprotease.

Burnett JC, Wang C, Nuss JE, Nguyen TL, Hermone AR, Schmidt JJ, Gussio R, Wipf P, Bavari S.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5811-3. doi: 10.1016/j.bmcl.2009.01.111. Epub 2009 Feb 13.


Novel broad-spectrum bis-(imidazolinylindole) derivatives with potent antibacterial activities against antibiotic-resistant strains.

Panchal RG, Ulrich RL, Lane D, Butler MM, Houseweart C, Opperman T, Williams JD, Peet NP, Moir DT, Nguyen T, Gussio R, Bowlin T, Bavari S.

Antimicrob Agents Chemother. 2009 Oct;53(10):4283-91. doi: 10.1128/AAC.01709-08. Epub 2009 Jul 27.


Reduced expression of CD45 protein-tyrosine phosphatase provides protection against anthrax pathogenesis.

Panchal RG, Ulrich RL, Bradfute SB, Lane D, Ruthel G, Kenny TA, Iversen PL, Anderson AO, Gussio R, Raschke WC, Bavari S.

J Biol Chem. 2009 May 8;284(19):12874-85. doi: 10.1074/jbc.M809633200. Epub 2009 Mar 6.


Evidence for a distinct ligand binding site on tubulin discovered through inhibition by GDP of paclitaxel-induced tubulin assembly in the absence of exogenous GTP.

Wilcox E, McGrath C, Blokhin AV, Gussio R, Hamel E.

Arch Biochem Biophys. 2009 Apr 1;484(1):55-62. doi: 10.1016/ Epub 2009 Jan 7.


Three-dimensional database mining identifies a unique chemotype that unites structurally diverse botulinum neurotoxin serotype A inhibitors in a three-zone pharmacophore.

Hermone AR, Burnett JC, Nuss JE, Tressler LE, Nguyen TL, Solaja BA, Vennerstrom JL, Schmidt JJ, Wipf P, Bavari S, Gussio R.

ChemMedChem. 2008 Dec;3(12):1905-12. doi: 10.1002/cmdc.200800241.


A potent peptidomimetic inhibitor of botulinum neurotoxin serotype A has a very different conformation than SNAP-25 substrate.

Zuniga JE, Schmidt JJ, Fenn T, Burnett JC, Araç D, Gussio R, Stafford RG, Badie SS, Bavari S, Brunger AT.

Structure. 2008 Oct 8;16(10):1588-97. doi: 10.1016/j.str.2008.07.011.


Sizing the Bacillus anthracis PA63 channel with nonelectrolyte poly(ethylene glycols).

Nablo BJ, Halverson KM, Robertson JW, Nguyen TL, Panchal RG, Gussio R, Bavari S, Krasilnikov OV, Kasianowicz JJ.

Biophys J. 2008 Aug;95(3):1157-64. doi: 10.1529/biophysj.107.121715.


Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A.

Solaja BA, Opsenica D, Smith KS, Milhous WK, Terzić N, Opsenica I, Burnett JC, Nuss J, Gussio R, Bavari S.

J Med Chem. 2008 Aug 14;51(15):4388-91. doi: 10.1021/jm800737y. Epub 2008 Jul 19.


A refined pharmacophore identifies potent 4-amino-7-chloroquinoline-based inhibitors of the botulinum neurotoxin serotype A metalloprotease.

Burnett JC, Opsenica D, Sriraghavan K, Panchal RG, Ruthel G, Hermone AR, Nguyen TL, Kenny TA, Lane DJ, McGrath CF, Schmidt JJ, Vennerstrom JL, Gussio R, Solaja BA, Bavari S.

J Med Chem. 2007 May 3;50(9):2127-36. Epub 2007 Apr 7.


Chemical genetic screening identifies critical pathways in anthrax lethal toxin-induced pathogenesis.

Panchal RG, Ruthel G, Brittingham KC, Lane D, Kenny TA, Gussio R, Lazo JS, Bavari S.

Chem Biol. 2007 Mar;14(3):245-55.


Inhibition of metalloprotease botulinum serotype A from a pseudo-peptide binding mode to a small molecule that is active in primary neurons.

Burnett JC, Ruthel G, Stegmann CM, Panchal RG, Nguyen TL, Hermone AR, Stafford RG, Lane DJ, Kenny TA, McGrath CF, Wipf P, Stahl AM, Schmidt JJ, Gussio R, Brunger AT, Bavari S.

J Biol Chem. 2007 Feb 16;282(7):5004-14. Epub 2006 Nov 8.


Comparison of the activities of the truncated halichondrin B analog NSC 707389 (E7389) with those of the parent compound and a proposed binding site on tubulin.

Dabydeen DA, Burnett JC, Bai R, Verdier-Pinard P, Hickford SJ, Pettit GR, Blunt JW, Munro MH, Gussio R, Hamel E.

Mol Pharmacol. 2006 Dec;70(6):1866-75. Epub 2006 Aug 29.


Homology model of RSK2 N-terminal kinase domain, structure-based identification of novel RSK2 inhibitors, and preliminary common pharmacophore.

Nguyen TL, Gussio R, Smith JA, Lannigan DA, Hecht SM, Scudiero DA, Shoemaker RH, Zaharevitz DW.

Bioorg Med Chem. 2006 Sep 1;14(17):6097-105. Epub 2006 May 24.


A common pharmacophore for a diverse set of colchicine site inhibitors using a structure-based approach.

Nguyen TL, McGrath C, Hermone AR, Burnett JC, Zaharevitz DW, Day BW, Wipf P, Hamel E, Gussio R.

J Med Chem. 2005 Sep 22;48(19):6107-16. Erratum in: J Med Chem. 2005 Dec 1;48(24):7917.


Cyclostreptin (FR182877), an antitumor tubulin-polymerizing agent deficient in enhancing tubulin assembly despite its high affinity for the taxoid site.

Edler MC, Buey RM, Gussio R, Marcus AI, Vanderwal CD, Sorensen EJ, Díaz JF, Giannakakou P, Hamel E.

Biochemistry. 2005 Aug 30;44(34):11525-38. Erratum in: Biochemistry. 2006 May 9;45(18):5932.


Anthrax biosensor, protective antigen ion channel asymmetric blockade.

Halverson KM, Panchal RG, Nguyen TL, Gussio R, Little SF, Misakian M, Bavari S, Kasianowicz JJ.

J Biol Chem. 2005 Oct 7;280(40):34056-62. Epub 2005 Aug 8.


Epoxide-containing side chains enhance antiproliferative activity of paullones.

Xie X, Lemcke T, Gussio R, Zaharevitz DW, Leost M, Meijer L, Kunick C.

Eur J Med Chem. 2005 Jul;40(7):655-61. Epub 2005 Apr 7.


An all-atom model of the pore-like structure of hexameric VP40 from Ebola: structural insights into the monomer-hexamer transition.

Nguyen TL, Schoehn G, Weissenhorn W, Hermone AR, Burnett JC, Panchal RG, McGrath C, Zaharevitz DW, Aman MJ, Gussio R, Bavari S.

J Struct Biol. 2005 Jul;151(1):30-40.


Homology model of the CDK1/cyclin B complex.

McGrath CF, Pattabiraman N, Kellogg GE, Lemcke T, Kunick C, Sausville EA, Zaharevitz DW, Gussio R.

J Biomol Struct Dyn. 2005 Apr;22(5):493-502.


Structure-aided optimization of kinase inhibitors derived from alsterpaullone.

Kunick C, Zeng Z, Gussio R, Zaharevitz D, Leost M, Totzke F, Schächtele C, Kubbutat MH, Meijer L, Lemcke T.

Chembiochem. 2005 Mar;6(3):541-9.


Conformational sampling of the botulinum neurotoxin serotype A light chain: implications for inhibitor binding.

Burnett JC, Schmidt JJ, McGrath CF, Nguyen TL, Hermone AR, Panchal RG, Vennerstrom JL, Kodukula K, Zaharevitz DW, Gussio R, Bavari S.

Bioorg Med Chem. 2005 Jan 17;13(2):333-41.


CDK1-inhibitory activity of paullones depends on electronic properties of 9-substituents.

Pies T, Schaper KJ, Leost M, Zaharevitz DW, Gussio R, Meijer L, Kunicke C.

Arch Pharm (Weinheim). 2004 Sep;337(9):486-92.


Identification of small molecule inhibitors of anthrax lethal factor.

Panchal RG, Hermone AR, Nguyen TL, Wong TY, Schwarzenbacher R, Schmidt J, Lane D, McGrath C, Turk BE, Burnett J, Aman MJ, Little S, Sausville EA, Zaharevitz DW, Cantley LC, Liddington RC, Gussio R, Bavari S.

Nat Struct Mol Biol. 2004 Jan;11(1):67-72. Epub 2003 Dec 29.


Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.

Kunick C, Lauenroth K, Wieking K, Xie X, Schultz C, Gussio R, Zaharevitz D, Leost M, Meijer L, Weber A, Jørgensen FS, Lemcke T.

J Med Chem. 2004 Jan 1;47(1):22-36.


Novel small molecule inhibitors of botulinum neurotoxin A metalloprotease activity.

Burnett JC, Schmidt JJ, Stafford RG, Panchal RG, Nguyen TL, Hermone AR, Vennerstrom JL, McGrath CF, Lane DJ, Sausville EA, Zaharevitz DW, Gussio R, Bavari S.

Biochem Biophys Res Commun. 2003 Oct 10;310(1):84-93.


Identification of a potent and selective pharmacophore for Cdc25 dual specificity phosphatase inhibitors.

Lazo JS, Nemoto K, Pestell KE, Cooley K, Southwick EC, Mitchell DA, Furey W, Gussio R, Zaharevitz DW, Joo B, Wipf P.

Mol Pharmacol. 2002 Apr;61(4):720-8.


Synthesis and biological evaluation of 12,13-cyclopropyl and 12,13-cyclobutyl epothilones.

Nicolaou KC, Namoto K, Li J, Ritzén A, Ulven T, Shoji M, Zaharevitz D, Gussio R, Sackett DL, Ward RD, Hensler A, Fojo T, Giannakakou P.

Chembiochem. 2001 Jan 8;2(1):69-75. No abstract available.


Biochemical genetic analysis of indanocine resistance in human leukemia.

Hua XH, Genini D, Gussio R, Tawatao R, Shih H, Kipps TJ, Carson DA, Leoni LM.

Cancer Res. 2001 Oct 1;61(19):7248-54.


Chemical synthesis and biological properties of pyridine epothilones.

Nicolaou KC, Scarpelli R, Bollbuck B, Werschkun B, Pereira MM, Wartmann M, Altmann KH, Zaharevitz D, Gussio R, Giannakakou P.

Chem Biol. 2000 Aug;7(8):593-9.


Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25.

Leost M, Schultz C, Link A, Wu YZ, Biernat J, Mandelkow EM, Bibb JA, Snyder GL, Greengard P, Zaharevitz DW, Gussio R, Senderowicz AM, Sausville EA, Kunick C, Meijer L.

Eur J Biochem. 2000 Oct;267(19):5983-94.

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