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Items: 21


Structure of the insulin receptor-insulin complex by single-particle cryo-EM analysis.

Scapin G, Dandey VP, Zhang Z, Prosise W, Hruza A, Kelly T, Mayhood T, Strickland C, Potter CS, Carragher B.

Nature. 2018 Apr 5;556(7699):122-125. doi: 10.1038/nature26153. Epub 2018 Feb 28.


Dual-Targeting Small-Molecule Inhibitors of the Staphylococcus aureus FMN Riboswitch Disrupt Riboflavin Homeostasis in an Infectious Setting.

Wang H, Mann PA, Xiao L, Gill C, Galgoci AM, Howe JA, Villafania A, Barbieri CM, Malinverni JC, Sher X, Mayhood T, McCurry MD, Murgolo N, Flattery A, Mack M, Roemer T.

Cell Chem Biol. 2017 May 18;24(5):576-588.e6. doi: 10.1016/j.chembiol.2017.03.014. Epub 2017 Apr 20.


Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor.

Mandal M, Tan Z, Madsen-Duggan C, Buevich AV, Caldwell JP, Dejesus R, Flattery A, Garlisi CG, Gill C, Ha SN, Ho G, Koseoglu S, Labroli M, Basu K, Lee SH, Liang L, Liu J, Mayhood T, McGuinness D, McLaren DG, Wen X, Parmee E, Rindgen D, Roemer T, Sheth P, Tawa P, Tata J, Yang C, Yang SW, Xiao L, Wang H, Tan C, Tang H, Walsh P, Walsh E, Wu J, Su J.

J Med Chem. 2017 May 11;60(9):3851-3865. doi: 10.1021/acs.jmedchem.7b00113. Epub 2017 Mar 29.


Epitopes and Mechanism of Action of the Clostridium difficile Toxin A-Neutralizing Antibody Actoxumab.

Hernandez LD, Kroh HK, Hsieh E, Yang X, Beaumont M, Sheth PR, DiNunzio E, Rutherford SA, Ohi MD, Ermakov G, Xiao L, Secore S, Karczewski J, Racine F, Mayhood T, Fischer P, Sher X, Gupta P, Lacy DB, Therien AG.

J Mol Biol. 2017 Apr 7;429(7):1030-1044. doi: 10.1016/j.jmb.2017.02.010. Epub 2017 Feb 21.


Benzimidazole analogs as WTA biosynthesis inhibitors targeting methicillin resistant Staphylococcus aureus.

Yang SW, Pan J, Yang C, Labroli M, Pan W, Caldwell J, Ha S, Koseoglu S, Xiao JC, Mayhood T, Sheth PR, Garlisi CG, Wu J, Lee SH, Wang H, Tan CM, Roemer T, Su J.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4743-4747. doi: 10.1016/j.bmcl.2016.08.036. Epub 2016 Aug 16.


Chemical Genetic Analysis and Functional Characterization of Staphylococcal Wall Teichoic Acid 2-Epimerases Reveals Unconventional Antibiotic Drug Targets.

Mann PA, Müller A, Wolff KA, Fischmann T, Wang H, Reed P, Hou Y, Li W, Müller CE, Xiao J, Murgolo N, Sher X, Mayhood T, Sheth PR, Mirza A, Labroli M, Xiao L, McCoy M, Gill CJ, Pinho MG, Schneider T, Roemer T.

PLoS Pathog. 2016 May 4;12(5):e1005585. doi: 10.1371/journal.ppat.1005585. eCollection 2016 May.


NMR Binding and Functional Assays for Detecting Inhibitors of S. aureus MnaA.

Hou Y, Mayhood T, Sheth P, Tan CM, Labroli M, Su J, Wyss DF, Roemer T, McCoy MA.

J Biomol Screen. 2016 Jul;21(6):579-89. doi: 10.1177/1087057116640199. Epub 2016 Mar 29.


TarO-specific inhibitors of wall teichoic acid biosynthesis restore β-lactam efficacy against methicillin-resistant staphylococci.

Lee SH, Wang H, Labroli M, Koseoglu S, Zuck P, Mayhood T, Gill C, Mann P, Sher X, Ha S, Yang SW, Mandal M, Yang C, Liang L, Tan Z, Tawa P, Hou Y, Kuvelkar R, DeVito K, Wen X, Xiao J, Batchlett M, Balibar CJ, Liu J, Xiao J, Murgolo N, Garlisi CG, Sheth PR, Flattery A, Su J, Tan C, Roemer T.

Sci Transl Med. 2016 Mar 9;8(329):329ra32. doi: 10.1126/scitranslmed.aad7364.


Selective small-molecule inhibition of an RNA structural element.

Howe JA, Wang H, Fischmann TO, Balibar CJ, Xiao L, Galgoci AM, Malinverni JC, Mayhood T, Villafania A, Nahvi A, Murgolo N, Barbieri CM, Mann PA, Carr D, Xia E, Zuck P, Riley D, Painter RE, Walker SS, Sherborne B, de Jesus R, Pan W, Plotkin MA, Wu J, Rindgen D, Cummings J, Garlisi CG, Zhang R, Sheth PR, Gill CJ, Tang H, Roemer T.

Nature. 2015 Oct 29;526(7575):672-7. doi: 10.1038/nature15542. Epub 2015 Sep 30.


Mechanism of action and epitopes of Clostridium difficile toxin B-neutralizing antibody bezlotoxumab revealed by X-ray crystallography.

Orth P, Xiao L, Hernandez LD, Reichert P, Sheth PR, Beaumont M, Yang X, Murgolo N, Ermakov G, DiNunzio E, Racine F, Karczewski J, Secore S, Ingram RN, Mayhood T, Strickland C, Therien AG.

J Biol Chem. 2014 Jun 27;289(26):18008-21. doi: 10.1074/jbc.M114.560748. Epub 2014 May 12.


Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor.

Deng Y, Shipps GW Jr, Zhao L, Siddiqui MA, Popovici-Muller J, Curran PJ, Duca JS, Hruza AW, Fischmann TO, Madison VS, Zhang R, McNemar CW, Mayhood TW, Syto R, Annis A, Kirschmeier P, Lees EM, Parry DA, Windsor WT.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):199-203. doi: 10.1016/j.bmcl.2013.11.041. Epub 2013 Nov 23.


Fully activated MEK1 exhibits compromised affinity for binding of allosteric inhibitors U0126 and PD0325901.

Sheth PR, Liu Y, Hesson T, Zhao J, Vilenchik L, Liu YH, Mayhood TW, Le HV.

Biochemistry. 2011 Sep 20;50(37):7964-76. doi: 10.1021/bi200542r. Epub 2011 Aug 26.


Crystal structures of MEK1 binary and ternary complexes with nucleotides and inhibitors.

Fischmann TO, Smith CK, Mayhood TW, Myers JE, Reichert P, Mannarino A, Carr D, Zhu H, Wong J, Yang RS, Le HV, Madison VS.

Biochemistry. 2009 Mar 31;48(12):2661-74. doi: 10.1021/bi801898e.


Structure-guided discovery of cyclin-dependent kinase inhibitors.

Fischmann TO, Hruza A, Duca JS, Ramanathan L, Mayhood T, Windsor WT, Le HV, Guzi TJ, Dwyer MP, Paruch K, Doll RJ, Lees E, Parry D, Seghezzi W, Madison V.

Biopolymers. 2008 May;89(5):372-9.


Expression and purification of phosphorylated and non-phosphorylated human MEK1.

Smith CK, Carr D, Mayhood TW, Jin W, Gray K, Windsor WT.

Protein Expr Purif. 2007 Apr;52(2):446-56. Epub 2006 Nov 9.


Differential type 4 cAMP-specific phosphodiesterase (PDE4) expression and functional sensitivity to PDE4 inhibitors among rats, monkeys and humans.

Bian H, Zhang J, Wu P, Varty LA, Jia Y, Mayhood T, Hey JA, Wang P.

Biochem Pharmacol. 2004 Dec 1;68(11):2229-36.


Fluorescence polarization assay and inhibitor design for MDM2/p53 interaction.

Zhang R, Mayhood T, Lipari P, Wang Y, Durkin J, Syto R, Gesell J, McNemar C, Windsor W.

Anal Biochem. 2004 Aug 1;331(1):138-46.


Development of a fluorescence polarization bead-based coupled assay to target different activity/conformation states of a protein kinase.

Lu Z, Yin Z, James L, Syto R, Stafford JM, Koseoglu S, Mayhood T, Myers J, Windsor W, Kirschmeier P, Samatar AA, Malcolm B, Turek-Etienne TC, Kumar CC.

J Biomol Screen. 2004 Jun;9(4):309-21.


Inhibition of Tat-mediated transactivation of HIV-1 LTR transcription by polyamide nucleic acid targeted to TAR hairpin element.

Mayhood T, Kaushik N, Pandey PK, Kashanchi F, Deng L, Pandey VN.

Biochemistry. 2000 Sep 26;39(38):11532-9.


Overexpression of p21(waf1) in human T-cell lymphotropic virus type 1-infected cells and its association with cyclin A/cdk2.

de La Fuente C, Santiago F, Chong SY, Deng L, Mayhood T, Fu P, Stein D, Denny T, Coffman F, Azimi N, Mahieux R, Kashanchi F.

J Virol. 2000 Aug;74(16):7270-83.

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