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Structure-activity analysis of peptidic Chlamydia HtrA inhibitors.

Agbowuro AA, Hwang J, Peel E, Mazraani R, Springwald A, Marsh JW, McCaughey L, Gamble AB, Huston WM, Tyndall JDA.

Bioorg Med Chem. 2019 Sep 15;27(18):4185-4199. doi: 10.1016/j.bmc.2019.07.049. Epub 2019 Jul 30.


Development of selective, fluorescent cannabinoid type 2 receptor ligands based on a 1,8-naphthyridin-2-(1H)-one-3-carboxamide scaffold.

Cooper AG, Oyagawa CRM, Manning JJ, Singh S, Hook S, Grimsey NL, Glass M, Tyndall JDA, Vernall AJ.

Medchemcomm. 2018 Oct 23;9(12):2055-2067. doi: 10.1039/c8md00448j. eCollection 2018 Dec 1.


Azole Resistance Reduces Susceptibility to the Tetrazole Antifungal VT-1161.

Monk BC, Keniya MV, Sabherwal M, Wilson RK, Graham DO, Hassan HF, Chen D, Tyndall JDA.

Antimicrob Agents Chemother. 2018 Dec 21;63(1). pii: e02114-18. doi: 10.1128/AAC.02114-18. Print 2019 Jan.


Crystal Structures of Full-Length Lanosterol 14α-Demethylases of Prominent Fungal Pathogens Candida albicans and Candida glabrata Provide Tools for Antifungal Discovery.

Keniya MV, Sabherwal M, Wilson RK, Woods MA, Sagatova AA, Tyndall JDA, Monk BC.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01134-18. doi: 10.1128/AAC.01134-18. Print 2018 Nov.


Heterologous Expression of Full-Length Lanosterol 14α-Demethylases of Prominent Fungal Pathogens Candida albicans and Candida glabrata Provides Tools for Antifungal Discovery.

Keniya MV, Ruma YN, Tyndall JDA, Monk BC.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01131-18. doi: 10.1128/AAC.01131-18. Print 2018 Nov.


Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.

Cooper AG, MacDonald C, Glass M, Hook S, Tyndall JDA, Vernall AJ.

Eur J Med Chem. 2018 Feb 10;145:770-789. doi: 10.1016/j.ejmech.2017.11.076. Epub 2017 Nov 28.


Impact of Homologous Resistance Mutations from Pathogenic Yeast on Saccharomyces cerevisiae Lanosterol 14α-Demethylase.

Sagatova AA, Keniya MV, Tyndall JDA, Monk BC.

Antimicrob Agents Chemother. 2018 Feb 23;62(3). pii: e02242-17. doi: 10.1128/AAC.02242-17. Print 2018 Mar.


Intrinsic short-tailed azole resistance in mucormycetes is due to an evolutionary conserved aminoacid substitution of the lanosterol 14α-demethylase.

Caramalho R, Tyndall JDA, Monk BC, Larentis T, Lass-Flörl C, Lackner M.

Sci Rep. 2017 Nov 21;7(1):15898. doi: 10.1038/s41598-017-16123-9.


Proteases and protease inhibitors in infectious diseases.

Agbowuro AA, Huston WM, Gamble AB, Tyndall JDA.

Med Res Rev. 2018 Jul;38(4):1295-1331. doi: 10.1002/med.21475. Epub 2017 Nov 17. Review.


Chemical Tools for Studying Lipid-Binding Class A G Protein-Coupled Receptors.

Cooper A, Singh S, Hook S, Tyndall JDA, Vernall AJ.

Pharmacol Rev. 2017 Jul;69(3):316-353. doi: 10.1124/pr.116.013243. Review.


CtHtrA: the lynchpin of the chlamydial surface and a promising therapeutic target.

Marsh JW, Ong VA, Lott WB, Timms P, Tyndall JD, Huston WM.

Future Microbiol. 2017 Jul;12:817-829. doi: 10.2217/fmb-2017-0017. Epub 2017 Jun 8. Review.


Stability, Kinetic, and Mechanistic Investigation of 1,8-Self-Immolative Cinnamyl Ether Spacers for Controlled Release of Phenols and Generation of Resonance and Inductively Stabilized Methides.

Matikonda SS, Fairhall JM, Tyndall JD, Hook S, Gamble AB.

Org Lett. 2017 Feb 3;19(3):528-531. doi: 10.1021/acs.orglett.6b03695. Epub 2017 Jan 12.


Structural and Functional Elucidation of Yeast Lanosterol 14α-Demethylase in Complex with Agrochemical Antifungals.

Tyndall JD, Sabherwal M, Sagatova AA, Keniya MV, Negroni J, Wilson RK, Woods MA, Tietjen K, Monk BC.

PLoS One. 2016 Dec 1;11(12):e0167485. doi: 10.1371/journal.pone.0167485. eCollection 2016.


Chlamydia Serine Protease Inhibitor, targeting HtrA, as a New Treatment for Koala Chlamydia infection.

Lawrence A, Fraser T, Gillett A, Tyndall JD, Timms P, Polkinghorne A, Huston WM.

Sci Rep. 2016 Aug 17;6:31466. doi: 10.1038/srep31466.


Triazole resistance mediated by mutations of a conserved active site tyrosine in fungal lanosterol 14α-demethylase.

Sagatova AA, Keniya MV, Wilson RK, Sabherwal M, Tyndall JD, Monk BC.

Sci Rep. 2016 May 18;6:26213. doi: 10.1038/srep26213.


A Chlamydia trachomatis strain with a chemically generated amino acid substitution (P370L) in the cthtrA gene shows reduced elementary body production.

Marsh JW, Wee BA, Tyndall JD, Lott WB, Bastidas RJ, Caldwell HD, Valdivia RH, Kari L, Huston WM.

BMC Microbiol. 2015 Sep 30;15:194. doi: 10.1186/s12866-015-0533-2.


Anxiogenic and Stressor Effects of the Hypothalamic Neuropeptide RFRP-3 Are Overcome by the NPFFR Antagonist GJ14.

Kim JS, Brownjohn PW, Dyer BS, Beltramo M, Walker CS, Hay DL, Painter GF, Tyndall JD, Anderson GM.

Endocrinology. 2015 Nov;156(11):4152-62. doi: 10.1210/en.2015-1532. Epub 2015 Aug 10.


Pinnatoxins E, F and G target multiple nicotinic receptor subtypes.

Hellyer SD, Indurthi D, Balle T, Runder-Varga V, Selwood AI, Tyndall JD, Chebib M, Rhodes L, Kerr DS.

J Neurochem. 2015 Nov;135(3):479-91. doi: 10.1111/jnc.13245. Epub 2015 Aug 3.


Structural Insights into Binding of the Antifungal Drug Fluconazole to Saccharomyces cerevisiae Lanosterol 14α-Demethylase.

Sagatova AA, Keniya MV, Wilson RK, Monk BC, Tyndall JD.

Antimicrob Agents Chemother. 2015 Aug;59(8):4982-9. doi: 10.1128/AAC.00925-15. Epub 2015 Jun 8.


Multiple binding modes of isothiocyanates that inhibit macrophage migration inhibitory factor.

Spencer ES, Dale EJ, Gommans AL, Rutledge MT, Vo CT, Nakatani Y, Gamble AB, Smith RA, Wilbanks SM, Hampton MB, Tyndall JD.

Eur J Med Chem. 2015 Mar 26;93:501-10. doi: 10.1016/j.ejmech.2015.02.012. Epub 2015 Feb 24.


Potent inhibition of macrophage migration inhibitory factor (MIF) by myeloperoxidase-dependent oxidation of epicatechins.

Dickerhof N, Magon NJ, Tyndall JD, Kettle AJ, Hampton MB.

Biochem J. 2014 Sep 1;462(2):303-14. doi: 10.1042/BJ20140612.


Architecture of a single membrane spanning cytochrome P450 suggests constraints that orient the catalytic domain relative to a bilayer.

Monk BC, Tomasiak TM, Keniya MV, Huschmann FU, Tyndall JD, O'Connell JD 3rd, Cannon RD, McDonald JG, Rodriguez A, Finer-Moore JS, Stroud RM.

Proc Natl Acad Sci U S A. 2014 Mar 11;111(10):3865-70. doi: 10.1073/pnas.1324245111. Epub 2014 Feb 3.


Proteolytic activation of Chlamydia trachomatis HTRA is mediated by PDZ1 domain interactions with protease domain loops L3 and LC and beta strand β5.

Marsh JW, Lott WB, Tyndall JD, Huston WW.

Cell Mol Biol Lett. 2013 Dec;18(4):522-37. doi: 10.2478/s11658-013-0103-2. Epub 2013 Sep 13.


Variable Expression of GLIPR1 Correlates with Invasive Potential in Melanoma Cells.

Awasthi A, Woolley AG, Lecomte FJ, Hung N, Baguley BC, Wilbanks SM, Jeffs AR, Tyndall JD.

Front Oncol. 2013 Aug 30;3:225. doi: 10.3389/fonc.2013.00225. eCollection 2013.


Catalysis product captured in lumazine synthase from the fungal pathogen Candida glabrata.

Shankar M, Wilbanks SM, Nakatani Y, Monk BC, Tyndall JD.

Acta Crystallogr D Biol Crystallogr. 2013 Aug;69(Pt 8):1580-6. doi: 10.1107/S0907444913010949. Epub 2013 Jul 20.


Insight into pleiotropic drug resistance ATP-binding cassette pump drug transport through mutagenesis of Cdr1p transmembrane domains.

Rawal MK, Khan MF, Kapoor K, Goyal N, Sen S, Saxena AK, Lynn AM, Tyndall JD, Monk BC, Cannon RD, Komath SS, Prasad R.

J Biol Chem. 2013 Aug 23;288(34):24480-93. doi: 10.1074/jbc.M113.488353. Epub 2013 Jul 3.


Identification of a serine protease inhibitor which causes inclusion vacuole reduction and is lethal to Chlamydia trachomatis.

Gloeckl S, Ong VA, Patel P, Tyndall JD, Timms P, Beagley KW, Allan JA, Armitage CW, Turnbull L, Whitchurch CB, Merdanovic M, Ehrmann M, Powers JC, Oleksyszyn J, Verdoes M, Bogyo M, Huston WM.

Mol Microbiol. 2013 Aug;89(4):676-89. doi: 10.1111/mmi.12306. Epub 2013 Jul 12.


[Fe₂L₃]⁴⁺ cylinders derived from bis(bidentate) 2-pyridyl-1,2,3-triazole "click" ligands: synthesis, structures and exploration of biological activity.

Vellas SK, Lewis JE, Shankar M, Sagatova A, Tyndall JD, Monk BC, Fitchett CM, Hanton LR, Crowley JD.

Molecules. 2013 May 29;18(6):6383-407. doi: 10.3390/molecules18066383.


Heterologous expression of Candida albicans Pma1p in Saccharomyces cerevisiae.

Keniya MV, Cannon RD, Nguyễn Â, Tyndall JD, Monk BC.

FEMS Yeast Res. 2013 May;13(3):302-11. doi: 10.1111/1567-1364.12035. Epub 2013 Mar 15.


Macrophage migration inhibitory factor covalently complexed with phenethyl isothiocyanate.

Tyndall JD, Lue H, Rutledge MT, Bernhagen J, Hampton MB, Wilbanks SM.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012 Sep 1;68(Pt 9):999-1002. doi: 10.1107/S1744309112030552. Epub 2012 Aug 29.


Specific interactions between the Candida albicans ABC transporter Cdr1p ectodomain and a D-octapeptide derivative inhibitor.

Niimi K, Harding DR, Holmes AR, Lamping E, Niimi M, Tyndall JD, Cannon RD, Monk BC.

Mol Microbiol. 2012 Aug;85(4):747-67. doi: 10.1111/j.1365-2958.2012.08140.x. Epub 2012 Jul 13.


the active site residue V266 of Chlamydial HtrA is critical for substrate binding during both in vitro and in vivo conditions.

Gloeckl S, Tyndall JD, Stansfield SH, Timms P, Huston WM.

J Mol Microbiol Biotechnol. 2012;22(1):10-6. doi: 10.1159/000336312. Epub 2012 Feb 21.


Honey bee dopamine and octopamine receptors linked to intracellular calcium signaling have a close phylogenetic and pharmacological relationship.

Beggs KT, Tyndall JD, Mercer AR.

PLoS One. 2011;6(11):e26809. doi: 10.1371/journal.pone.0026809. Epub 2011 Nov 11.


Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA).

Matthews H, Ranson M, Tyndall JD, Kelso MJ.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6760-6. doi: 10.1016/j.bmcl.2011.09.044. Epub 2011 Sep 18.


Unique residues involved in activation of the multitasking protease/chaperone HtrA from Chlamydia trachomatis.

Huston WM, Tyndall JD, Lott WB, Stansfield SH, Timms P.

PLoS One. 2011;6(9):e24547. doi: 10.1371/journal.pone.0024547. Epub 2011 Sep 8.


Homology modeling and functional testing of an ABCA1 mutation causing Tangier disease.

Suetani RJ, Sorrenson B, Tyndall JD, Williams MJ, McCormick SP.

Atherosclerosis. 2011 Oct;218(2):404-10. doi: 10.1016/j.atherosclerosis.2011.06.019. Epub 2011 Jun 29.


Targeting the chromosome partitioning protein ParA in tuberculosis drug discovery.

Nisa S, Blokpoel MC, Robertson BD, Tyndall JD, Lun S, Bishai WR, O'Toole R.

J Antimicrob Chemother. 2010 Nov;65(11):2347-58. doi: 10.1093/jac/dkq311. Epub 2010 Sep 1.


In vivo seizure induction and affinity studies of domoic acid and isodomoic acids-D, -E and -F.

Sawant PM, Tyndall JD, Holland PT, Peake BM, Mountfort DO, Kerr DS.

Neuropharmacology. 2010 Sep;59(3):129-38. doi: 10.1016/j.neuropharm.2010.03.019. Epub 2010 Apr 21.


Update 1 of: Beta-strand mimetics.

Loughlin WA, Tyndall JD, Glenn MP, Hill TA, Fairlie DP.

Chem Rev. 2010 Jun 9;110(6):PR32-69. doi: 10.1021/cr900395y. Epub 2010 Apr 12. Review. No abstract available.


Update 1 of: Proteases universally recognize beta strands in their active sites.

Madala PK, Tyndall JD, Nall T, Fairlie DP.

Chem Rev. 2010 Jun 9;110(6):PR1-31. doi: 10.1021/cr900368a. Epub 2010 Apr 8. Review. No abstract available.


Update 1 of: Over one hundred peptide-activated G protein-coupled receptors recognize ligands with turn structure.

Ruiz-Gómez G, Tyndall JD, Pfeiffer B, Abbenante G, Fairlie DP.

Chem Rev. 2010 Apr 14;110(4):PR1-41. doi: 10.1021/cr900344w. Review. No abstract available.


The orf virus inhibitor of apoptosis functions in a Bcl-2-like manner, binding and neutralizing a set of BH3-only proteins and active Bax.

Westphal D, Ledgerwood EC, Tyndall JD, Hibma MH, Ueda N, Fleming SB, Mercer AA.

Apoptosis. 2009 Nov;14(11):1317-30. doi: 10.1007/s10495-009-0403-1.


Direct modification of the proinflammatory cytokine macrophage migration inhibitory factor by dietary isothiocyanates.

Brown KK, Blaikie FH, Smith RA, Tyndall JD, Lue H, Bernhagen J, Winterbourn CC, Hampton MB.

J Biol Chem. 2009 Nov 20;284(47):32425-33. doi: 10.1074/jbc.M109.047092. Epub 2009 Sep 23.


The toxicogenomic multiverse: convergent recruitment of proteins into animal venoms.

Fry BG, Roelants K, Champagne DE, Scheib H, Tyndall JD, King GF, Nevalainen TJ, Norman JA, Lewis RJ, Norton RS, Renjifo C, de la Vega RC.

Annu Rev Genomics Hum Genet. 2009;10:483-511. doi: 10.1146/annurev.genom.9.081307.164356. Review.


Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei.

Lamping E, Ranchod A, Nakamura K, Tyndall JD, Niimi K, Holmes AR, Niimi M, Cannon RD.

Antimicrob Agents Chemother. 2009 Feb;53(2):354-69. doi: 10.1128/AAC.01095-08. Epub 2008 Nov 17.


Cannabinoid CB1 and CB2 receptor ligand specificity and the development of CB2-selective agonists.

Ashton JC, Wright JL, McPartland JM, Tyndall JD.

Curr Med Chem. 2008;15(14):1428-43. Review.


Crystal structures of highly constrained substrate and hydrolysis products bound to HIV-1 protease. Implications for the catalytic mechanism.

Tyndall JD, Pattenden LK, Reid RC, Hu SH, Alewood D, Alewood PF, Walsh T, Fairlie DP, Martin JL.

Biochemistry. 2008 Mar 25;47(12):3736-44. doi: 10.1021/bi7023157. Epub 2008 Mar 1.


Peptides and small molecules targeting the plasminogen activation system: towards prophylactic anti-metastasis drugs for breast cancer.

Tyndall JD, Kelso MJ, Clingan P, Ranson M.

Recent Pat Anticancer Drug Discov. 2008 Jan;3(1):1-13. Review.


Enzyme adaptation to inhibitor binding: a cryptic binding site in phenylethanolamine N-methyltransferase.

Gee CL, Drinkwater N, Tyndall JD, Grunewald GL, Wu Q, McLeish MJ, Martin JL.

J Med Chem. 2007 Oct 4;50(20):4845-53. Epub 2007 Sep 11. Erratum in: J Med Chem. 2007 Dec 13;50(25):6441.


Sequence requirements for splicing by the Cne PRP8 intein.

Pearl EJ, Tyndall JD, Poulter RT, Wilbanks SM.

FEBS Lett. 2007 Jun 26;581(16):3000-4. Epub 2007 May 29.

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