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Identification, preclinical profile, and clinical proof of concept of an orally bioavailable pro-drug of miridesap.

Richards D, Bamford M, Liefaard L, Haque N, Lewis G, Storey J, Fernando D, Kumar S, Thompson D, Holmes DS.

Br J Pharmacol. 2019 Dec 26. doi: 10.1111/bph.14956. [Epub ahead of print]


Corrigendum to 'Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors' [Bioorg. Med. Chem. Lett. 29 (2019) 126675].

Walker AL, Denis A, Bingham RP, Bouillot A, Edgar EV, Ferrie A, Holmes DS, Laroze A, Liddle J, Fouchet MH, Moquette A, Nassau P, Pearce AC, Polyakova O, Smith KJ, Thomas P, Thorpe JH, Trottet L, Wang Y, Hovnanian A.

Bioorg Med Chem Lett. 2020 Jan 15;30(2):126771. doi: 10.1016/j.bmcl.2019.126771. Epub 2019 Dec 16. No abstract available.


Experimental study of the intrinsic permeability of municipal solid waste.

Xu XB, Powrie W, Zhang WJ, Holmes DS, Xu H, Beaven R.

Waste Manag. 2020 Feb 1;102:304-311. doi: 10.1016/j.wasman.2019.10.039. Epub 2019 Nov 25.


Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.

Walker AL, Denis A, Bingham RP, Bouillot A, Edgar EV, Ferrie A, Holmes DS, Laroze A, Liddle J, Fouchet MH, Moquette A, Nassau P, Pearce AC, Polyakova O, Smith KJ, Thomas P, Thorpe JH, Trottet L, Wang Y, Hovnanian A.

Bioorg Med Chem Lett. 2019 Oct 15;29(20):126675. doi: 10.1016/j.bmcl.2019.126675. Epub 2019 Sep 7. Erratum in: Bioorg Med Chem Lett. 2020 Jan 15;30(2):126771.


Identification and Unusual Properties of the Master Regulator FNR in the Extreme Acidophile Acidithiobacillus ferrooxidans.

Osorio H, Mettert E, Kiley P, Dopson M, Jedlicki E, Holmes DS.

Front Microbiol. 2019 Jul 19;10:1642. doi: 10.3389/fmicb.2019.01642. eCollection 2019.


Utilization of a Radiation Safety Time-Out Reduces Radiation Exposure During Electrophysiology Procedures.

Aizer A, Qiu JK, Cheng AV, Wu PB, Holmes DS, Wagner SR, Bernstein SA, Park DS, Cartolano B, Barbhaiya CR, Chinitz LA.

JACC Clin Electrophysiol. 2019 May;5(5):626-634. doi: 10.1016/j.jacep.2018.12.002. Epub 2019 Jan 30.


Evaluation of a crystallographic surrogate for kallikrein 5 in the discovery of novel inhibitors for Netherton syndrome.

Thorpe JH, Edgar EV, Smith KJ, Lewell XQ, Rella M, White GV, Polyakova O, Nassau P, Walker AL, Holmes DS, Pearce AC, Wang Y, Liddle J, Hovnanian A.

Acta Crystallogr F Struct Biol Commun. 2019 May 1;75(Pt 5):385-391. doi: 10.1107/S2053230X19003169. Epub 2019 Apr 26.


Effect of CO2 Concentration on Uptake and Assimilation of Inorganic Carbon in the Extreme Acidophile Acidithiobacillus ferrooxidans.

Esparza M, Jedlicki E, González C, Dopson M, Holmes DS.

Front Microbiol. 2019 Apr 4;10:603. doi: 10.3389/fmicb.2019.00603. eCollection 2019.


Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.

Walker AL, Bingham RP, Edgar EV, Ferrie A, Holmes DS, Liddle J, Polyakova O, Rella M, Smith KJ, Thorpe JH, Wang Y, White GV, Young RJ, Hovnanian A.

Bioorg Med Chem Lett. 2019 Jun 15;29(12):1454-1458. doi: 10.1016/j.bmcl.2019.04.022. Epub 2019 Apr 12.


Uncovering the Mechanisms of Halotolerance in the Extremely Acidophilic Members of the Acidihalobacter Genus Through Comparative Genome Analysis.

Khaleque HN, González C, Shafique R, Kaksonen AH, Holmes DS, Watkin ELJ.

Front Microbiol. 2019 Feb 8;10:155. doi: 10.3389/fmicb.2019.00155. eCollection 2019.


Kallikrein 5 inhibitors identified through structure based drug design in search for a treatment for Netherton Syndrome.

White GV, Edgar EV, Holmes DS, Lewell XQ, Liddle J, Polyakova O, Smith KJ, Thorpe JH, Walker AL, Wang Y, Young RJ, Hovnanian A.

Bioorg Med Chem Lett. 2019 Mar 15;29(6):821-825. doi: 10.1016/j.bmcl.2019.01.020. Epub 2019 Jan 22.


Improved ontology for eukaryotic single-exon coding sequences in biological databases.

Jorquera R, González C, Clausen P, Petersen B, Holmes DS.

Database (Oxford). 2018 Jan 1;2018:1-6. doi: 10.1093/database/bay089.


Pacing Mediated Heart Rate Acceleration Improves Catheter Stability and Enhances Markers for Lesion Delivery in Human Atria During Atrial Fibrillation Ablation.

Aizer A, Cheng AV, Wu PB, Qiu JK, Barbhaiya CR, Fowler SJ, Bernstein SA, Park DS, Holmes DS, Chinitz LA.

JACC Clin Electrophysiol. 2018 Apr;4(4):483-490. doi: 10.1016/j.jacep.2017.12.017. Epub 2018 Mar 1.


Draft genome sequence of Acidithiobacillus thiooxidans CLST isolated from the acidic hypersaline Gorbea salt flat in northern Chile.

Quatrini R, Escudero LV, Moya-Beltrán A, Galleguillos PA, Issotta F, Acosta M, Cárdenas JP, Nuñez H, Salinas K, Holmes DS, Demergasso C.

Stand Genomic Sci. 2017 Dec 19;12:84. doi: 10.1186/s40793-017-0305-8. eCollection 2017.


Draft genome sequence of the type strain of the sulfur-oxidizing acidophile, Acidithiobacillus albertensis (DSM 14366).

Castro M, Moya-Beltrán A, Covarrubias PC, Gonzalez M, Cardenas JP, Issotta F, Nuñez H, Acuña LG, Encina G, Holmes DS, Johnson DB, Quatrini R.

Stand Genomic Sci. 2017 Dec 15;12:77. doi: 10.1186/s40793-017-0282-y. eCollection 2017.


Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H1 receptor antagonists for use in allergic rhinitis.

Procopiou PA, Ford AJ, Gore PM, Hancock AP, Hodgson ST, Holmes DS, Looker BE, Vile S, Clark KL, Saunders KA, Slack RJ, Watts CJ.

Bioorg Med Chem Lett. 2017 Nov 1;27(21):4914-4919. doi: 10.1016/j.bmcl.2017.09.020. Epub 2017 Sep 9.


In search of a small molecule agonist of the relaxin receptor RXFP1 for the treatment of liver fibrosis.

McBride A, Hoy AM, Bamford MJ, Mossakowska DE, Ruediger MP, Griggs J, Desai S, Simpson K, Caballero-Hernandez I, Iredale JP, Pell T, Aucott RL, Holmes DS, Webster SP, Fallowfield JA.

Sci Rep. 2017 Sep 7;7(1):10806. doi: 10.1038/s41598-017-10521-9.


Family Consumer Behaviors, Adolescent Prediabetes and Diabetes in the National Health and Nutrition Examination Survey (2007-2010).

Nagarajan S, Khokhar A, Holmes DS, Chandwani S.

J Am Coll Nutr. 2017 Sep-Oct;36(7):520-527. doi: 10.1080/07315724.2017.1327828. Epub 2017 Aug 30.


Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase.

Hutchinson JP, Rowland P, Taylor MRD, Christodoulou EM, Haslam C, Hobbs CI, Holmes DS, Homes P, Liddle J, Mole DJ, Uings I, Walker AL, Webster SP, Mowat CG, Chung CW.

Nat Commun. 2017 Jun 12;8:15827. doi: 10.1038/ncomms15827.


Design of Phthalazinone Amide Histamine H1 Receptor Antagonists for Use in Rhinitis.

Procopiou PA, Ford AJ, Gore PM, Looker BE, Hodgson ST, Holmes DS, Vile S, Clark KL, Saunders KA, Slack RJ, Rowedder JE, Watts CJ.

ACS Med Chem Lett. 2017 Apr 21;8(5):577-581. doi: 10.1021/acsmedchemlett.7b00112. eCollection 2017 May 11.


Development of a Series of Kynurenine 3-Monooxygenase Inhibitors Leading to a Clinical Candidate for the Treatment of Acute Pancreatitis.

Walker AL, Ancellin N, Beaufils B, Bergeal M, Binnie M, Bouillot A, Clapham D, Denis A, Haslam CP, Holmes DS, Hutchinson JP, Liddle J, McBride A, Mirguet O, Mowat CG, Rowland P, Tiberghien N, Trottet L, Uings I, Webster SP, Zheng X, Mole DJ.

J Med Chem. 2017 Apr 27;60(8):3383-3404. doi: 10.1021/acs.jmedchem.7b00055. Epub 2017 Apr 11.


The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis.

Liddle J, Beaufils B, Binnie M, Bouillot A, Denis AA, Hann MM, Haslam CP, Holmes DS, Hutchinson JP, Kranz M, McBride A, Mirguet O, Mole DJ, Mowat CG, Pal S, Rowland P, Trottet L, Uings IJ, Walker AL, Webster SP.

Bioorg Med Chem Lett. 2017 May 1;27(9):2023-2028. doi: 10.1016/j.bmcl.2017.02.078. Epub 2017 Mar 9.


Mutantelec: An In Silico mutation simulation platform for comparative electrostatic potential profiling of proteins.

Valdebenito-Maturana B, Reyes-Suarez JA, Henriquez J, Holmes DS, Quatrini R, Pohl E, Arenas-Salinas M.

J Comput Chem. 2017 Mar 15;38(7):467-474. doi: 10.1002/jcc.24712.


Multiple Osmotic Stress Responses in Acidihalobacter prosperus Result in Tolerance to Chloride Ions.

Dopson M, Holmes DS, Lazcano M, McCredden TJ, Bryan CG, Mulroney KT, Steuart R, Jackaman C, Watkin EL.

Front Microbiol. 2017 Jan 5;7:2132. doi: 10.3389/fmicb.2016.02132. eCollection 2016.


The discovery of quinoline based single-ligand human H1 and H3 receptor antagonists.

Procopiou PA, Ancliff RA, Gore PM, Hancock AP, Hodgson ST, Holmes DS, Keeling SP, Looker BE, Parr NA, Rowedder JE, Slack RJ.

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5855-5859. doi: 10.1016/j.bmcl.2016.11.022. Epub 2016 Nov 10.


Graphlet Based Metrics for the Comparison of Gene Regulatory Networks.

Martin AJ, Dominguez C, Contreras-Riquelme S, Holmes DS, Perez-Acle T.

PLoS One. 2016 Oct 3;11(10):e0163497. doi: 10.1371/journal.pone.0163497. eCollection 2016.


Genomic and metagenomic challenges and opportunities for bioleaching: a mini-review.

Cárdenas JP, Quatrini R, Holmes DS.

Res Microbiol. 2016 Sep;167(7):529-38. doi: 10.1016/j.resmic.2016.06.007. Epub 2016 Jul 7. Review.


Gene Loss and Horizontal Gene Transfer Contributed to the Genome Evolution of the Extreme Acidophile "Ferrovum".

Ullrich SR, González C, Poehlein A, Tischler JS, Daniel R, Schlömann M, Holmes DS, Mühling M.

Front Microbiol. 2016 May 31;7:797. doi: 10.3389/fmicb.2016.00797. eCollection 2016.


SinEx DB: a database for single exon coding sequences in mammalian genomes.

Jorquera R, Ortiz R, Ossandon F, Cárdenas JP, Sepúlveda R, González C, Holmes DS.

Database (Oxford). 2016 Jun 7;2016. pii: baw095. doi: 10.1093/database/baw095. Print 2016.


Draft genome sequence of chloride-tolerant Leptospirillum ferriphilum Sp-Cl from industrial bioleaching operations in northern Chile.

Issotta F, Galleguillos PA, Moya-Beltrán A, Davis-Belmar CS, Rautenbach G, Covarrubias PC, Acosta M, Ossandon FJ, Contador Y, Holmes DS, Marín-Eliantonio S, Quatrini R, Demergasso C.

Stand Genomic Sci. 2016 Feb 27;11:19. doi: 10.1186/s40793-016-0142-1. eCollection 2016.


Genome Analysis of the Biotechnologically Relevant Acidophilic Iron Oxidising Strain JA12 Indicates Phylogenetic and Metabolic Diversity within the Novel Genus "Ferrovum".

Ullrich SR, Poehlein A, Tischler JS, González C, Ossandon FJ, Daniel R, Holmes DS, Schlömann M, Mühling M.

PLoS One. 2016 Jan 25;11(1):e0146832. doi: 10.1371/journal.pone.0146832. eCollection 2016.


Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis.

Mole DJ, Webster SP, Uings I, Zheng X, Binnie M, Wilson K, Hutchinson JP, Mirguet O, Walker A, Beaufils B, Ancellin N, Trottet L, Bénéton V, Mowat CG, Wilkinson M, Rowland P, Haslam C, McBride A, Homer NZ, Baily JE, Sharp MG, Garden OJ, Hughes J, Howie SE, Holmes DS, Liddle J, Iredale JP.

Nat Med. 2016 Feb;22(2):202-9. doi: 10.1038/nm.4020. Epub 2016 Jan 11.


Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.

Demont EH, Bailey JM, Bit RA, Brown JA, Campbell CA, Deeks N, Dowell SJ, Eldred C, Gaskin P, Gray JR, Haynes A, Hirst DJ, Holmes DS, Kumar U, Morse MA, Osborne GJ, Renaux JF, Seal GA, Smethurst CA, Taylor S, Watson R, Willis R, Witherington J.

J Med Chem. 2016 Feb 11;59(3):1003-20. doi: 10.1021/acs.jmedchem.5b01512. Epub 2016 Jan 22.


Reclassification of 'Thiobacillus prosperus' Huber and Stetter 1989 as Acidihalobacter prosperus gen. nov., sp. nov., a member of the family Ectothiorhodospiraceae.

Pablo Cárdenas J, Ortiz R, Norris PR, Watkin E, Holmes DS.

Int J Syst Evol Microbiol. 2015 Oct;65(10):3641-4. doi: 10.1099/ijsem.0.000468. Epub 2015 Jul 21.


Expression and activity of the Calvin-Benson-Bassham cycle transcriptional regulator CbbR from Acidithiobacillus ferrooxidans in Ralstonia eutropha.

Esparza M, Jedlicki E, Dopson M, Holmes DS.

FEMS Microbiol Lett. 2015 Aug;362(15):fnv108. doi: 10.1093/femsle/fnv108. Epub 2015 Jul 6.


Metagenomic analysis reveals adaptations to a cold-adapted lifestyle in a low-temperature acid mine drainage stream.

Liljeqvist M, Ossandon FJ, González C, Rajan S, Stell A, Valdes J, Holmes DS, Dopson M.

FEMS Microbiol Ecol. 2015 Apr;91(4). pii: fiv011. doi: 10.1093/femsec/fiv011. Epub 2015 Jan 27.


Draft Genome Sequence of the Iron-Oxidizing Acidophile Leptospirillum ferriphilum Type Strain DSM 14647.

Cárdenas JP, Lazcano M, Ossandon FJ, Corbett M, Holmes DS, Watkin E.

Genome Announc. 2014 Nov 6;2(6). pii: e01153-14. doi: 10.1128/genomeA.01153-14.


Draft Genome Sequence of the Iron-Oxidizing, Acidophilic, and Halotolerant "Thiobacillus prosperus" Type Strain DSM 5130.

Ossandon FJ, Cárdenas JP, Corbett M, Quatrini R, Holmes DS, Watkin E.

Genome Announc. 2014 Oct 23;2(5). pii: e01042-14. doi: 10.1128/genomeA.01042-14.


Multi Locus Sequence Typing scheme for Acidithiobacillus caldus strain evaluation and differentiation.

Nuñez H, Loyola D, Cárdenas JP, Holmes DS, Johnson DB, Quatrini R.

Res Microbiol. 2014 Nov;165(9):735-42. doi: 10.1016/j.resmic.2014.07.014. Epub 2014 Aug 29.


Genetic variability of psychrotolerant Acidithiobacillus ferrivorans revealed by (meta)genomic analysis.

González C, Yanquepe M, Cardenas JP, Valdes J, Quatrini R, Holmes DS, Dopson M.

Res Microbiol. 2014 Nov;165(9):726-34. doi: 10.1016/j.resmic.2014.08.005. Epub 2014 Aug 27.


Draft Genome Sequence of the Nominated Type Strain of "Ferrovum myxofaciens," an Acidophilic, Iron-Oxidizing Betaproteobacterium.

Moya-Beltrán A, Cárdenas JP, Covarrubias PC, Issotta F, Ossandon FJ, Grail BM, Holmes DS, Quatrini R, Johnson DB.

Genome Announc. 2014 Aug 21;2(4). pii: e00834-14. doi: 10.1128/genomeA.00834-14.


Metal resistance in acidophilic microorganisms and its significance for biotechnologies.

Dopson M, Holmes DS.

Appl Microbiol Biotechnol. 2014 Oct;98(19):8133-44. doi: 10.1007/s00253-014-5982-2. Epub 2014 Aug 8. Review.


AFAL: a web service for profiling amino acids surrounding ligands in proteins.

Arenas-Salinas M, Ortega-Salazar S, Gonzales-Nilo F, Pohl E, Holmes DS, Quatrini R.

J Comput Aided Mol Des. 2014 Nov;28(11):1069-76. doi: 10.1007/s10822-014-9783-6. Epub 2014 Aug 2.


The role of multimodality imaging in percutaneous left atrial appendage suture ligation with the LARIAT device.

Laura DM, Chinitz LA, Aizer A, Holmes DS, Benenstein R, Freedberg RS, Kim EE, Saric M.

J Am Soc Echocardiogr. 2014 Jul;27(7):699-708. doi: 10.1016/j.echo.2014.04.014. Epub 2014 May 27. Review.


Metal resistance or tolerance? Acidophiles confront high metal loads via both abiotic and biotic mechanisms.

Dopson M, Ossandon FJ, Lövgren L, Holmes DS.

Front Microbiol. 2014 Apr 9;5:157. doi: 10.3389/fmicb.2014.00157. eCollection 2014.


α-fur, an antisense RNA gene to fur in the extreme acidophile Acidithiobacillus ferrooxidans.

Lefimil C, Jedlicki E, Holmes DS.

Microbiology. 2014 Mar;160(Pt 3):514-524. doi: 10.1099/mic.0.073171-0. Epub 2014 Jan 2.


Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing.

Procopiou PA, Barrett VJ, Biggadike K, Butchers PR, Craven A, Ford AJ, Guntrip SB, Holmes DS, Hughes SC, Jones AE, Looker BE, Mutch PJ, Ruston M, Needham D, Smith CE.

J Med Chem. 2014 Jan 9;57(1):159-70. doi: 10.1021/jm401532g. Epub 2013 Dec 20.


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