University of Dundee

Biological Chemistry and Drug Discovery 2018

Amato A, Lucas X, Bortoluzzi A, Wright D, Ciulli A. 2018. Targeting ligandable pockets on PHD zinc finger domains by a fragment-based approach. ACS Chemical Biology. 13(4):915-921. Available from: 10.1021/acschembio.7b01093

Barini E, Miccoli A, Tinarelli F, Mulholland K, Kadri H, Khanim F, Stojanovski L, Read KD, Burness K, Blow JJ, Mehellou Y, Muqit MMK. 2018. The Anthelmintic Drug Niclosamide and Its Analogues Activate the Parkinson's Disease Associated Protein Kinase PINK1. ChemBioChem. 19(5):425-429. Available from: 10.1002/cbic.201700500

Chan KH, Zengerle M, Testa A, Ciulli A. 2018. Impact of target warhead and linkage vector on inducing protein degradation: comparison of Bromodomain and Extra-Terminal (BET) degraders derived from triazolodiazepine (JQ1) and tetrahydroquinoline (I-BET726) BET inhibitor scaffolds. Journal of Medicinal Chemistry. 61(2):504-513. Available from: 10.1021/acs.jmedchem.6b01912

Crozier TWM, Tinti M, Wheeler RJ, Ly T, Ferguson MAJ, Lamond AI. 2018. Proteomic analysis of the cell cycle of procylic form Trypanosoma brucei. Molecular & Cellular Proteomics. 17:1184-1195. Available from: 10.1074/mcp.RA118.000650

Dacks JB, Field MC. 2018. Evolutionary origins and specialisation of membrane transport. Current Opinion in Cell Biology. 53:70-76. Available from: 10.1016/

de Vos IJHM, Tao EY, Ong SLM, Goggi JL, Scerri T, Wilson GR, Low CGM, Wong ASW, Grussu D, Stegmann APA, van Geel M, Janssen R, Amor DJ, Bahlo M, Dunn NR, Carney TJ, Lockhart PJ, Coull B, van Steensel M. 2018. Functional analysis of a hypomorphic allele shows that MMP14 catalytic activity is the prime determinant of the Winchester syndrome phenotype. Human Molecular Genetics. Available from: 10.1093/hmg/ddy168

Easton JA, Alboulshi AK, Kamps MAF, Brouns GH, Broers MR, Coull BJ, Oji V, van Geel M, van Steensel MAM, Martin PE. 2018. A rare missense mutation in GJB3 (Cx31G45E) is associated with a unique cellular phenotype resulting in necrotic cell death. Experimental Dermatology. Available from: 10.1111/exd.13542

Fairlamb A, Horn D. 2018. Melarsoprol Resistance in African Trypanosomiasis. Trends in Parasitology. Available from: 10.1016/

Fairlamb AH, Patterson S. 2018. Current and Future Prospects of Nitro-compounds as Drugs for Trypanosomiasis and Leishmaniasis. Current Medicinal Chemistry. Available from: 10.2174/0929867325666180426164352

Herman EK, Ali M, Field MC, Dacks JB. 2018. Regulation of early endosomes across eukaryotes: Evolution and functional homology of Vps9 proteins. Traffic. Available from: 10.1111/tra.12570

Holden JM, Koreny L, Obado S, Ratushny AV, Chen W-M, Bart J-M, Navarro M, Chait BT, Aitchison JD, Rout MP, Field MC. 2018. Involvement in surface antigen expression by a moonlighting FG-repeat nucleoporin in trypanosomes. Molecular Biology of the Cell. 29(9). Available from: 10.1091/mbc.E17-06-0430

Jeacock L, Correia Faria J, Horn D. 2018. Codon usage bias controls mRNA and protein abundance in trypanosomatids. eLife. Available from: 10.7554/eLife.32496

Kono M, Akiyama M, Inoue Y, Nomura T, Hata A, Okamoto Y, Takeichi T, Muro Y, McLean WHI, Shimizu H, Sugiura K, Suzuki Y, Shimojo N. 2018. Filaggrin gene mutations may influence the persistence of food allergies in Japanese primary school children. British Journal of Dermatology. Available from: 10.1111/bjd.16375

Kürklü E, Öztürk Ş, Cassidy AJ, Ak G, Koray M, Çefle K, Palandüz Ş, Güllüoğlu MG, Tanyeri H, McLean WHI. 2018. Clinical features and molecular genetic analysis in a Turkish family with oral white sponge nevus. Medicina Oral Patologia Oral y Cirugia Bucal. 23(2):e144-e150. Available from: 10.4317/medoral.21437

Luise N, Wyatt P. 2018. Generation of Polar Semi-Saturated Bicyclic Pyrazoles for Fragment-Based Drug Discovery Campaigns. Chemistry: a European Journal. Available from: 10.1002/chem.201801313

MacLean L, Thomas J, Lewis MD, Cotillo I, Gray D, De Rycker M. 2018. Development of Trypanosoma cruzi in vitro assays to identify compounds suitable for progression in Chagas’ disease drug discovery. PLoS Neglected Tropical Diseases.

McAleer MA, Jaska I, Raj N, O'Donnell CPF, Lane ME, Rawlings AV, Voegeli R, McLean W, Kezic S, Irvine AD. 2018. Early life regional and temporal variation in filaggrin-derived natural moisturising factor, filaggrin processing enzyme activity, corneocyte phenotypes and plasmin activity: Implications for atopic dermatitis. British Journal of Dermatology. Available from: 10.1111/bjd.16691

McKenzie C, Sutcliffe OB, Read K, Scullion S, Epemolu R, Fletcher D, Helander A, Beck O, Rylski A, Antonides L, Riley J, Smith S, Nic Daeid N. 2018. Chemical synthesis, characterisation and in vitro and in vivo metabolism of the synthetic opioid MT-45 and it's newly identified fluorinated analogue 2F-MT-45 with metabolite confirmation in urine samples from known drug users. Forensic Toxicology 36: 359-374

Murugesan D, Ray PC, Bayliss T, Prosser GA, Harrison JR, Green K, Soares De Melo C, Feng TS, Street LJ, Chibale K, Warner DF, Mizrahi V, Epemolu O, Scullion P, Ellis L, Riley J, Shishikura Y, Ferguson L, Osuna-Cabello M, Read KD, Green SR, Lamprecht DA, Steyn AJC, Ioerger TR, Sacchettini J, Rhee KY, Arora K, Barry CE, Wyatt PG, Boshoff HIM. 2018. 2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure-Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization. ACS Infectious Diseases. 4(6):954-969. Available from: 10.1021/acsinfecdis.7b00275

Navratilova IH, Aristotelous T, Bird LE, Hopkins AL. 2018. Surveying GPCR solubilisation conditions using surface plasmon resonance. Analytical Biochemistry. 556:23-34. Available from: 10.1016/j.ab.2018.06.012

Ohguchi Y, Nomura T, Suzuki S, Takeda M, Miyauchi T, Mizuno O, Shinkuma S, Fujita Y, Nemoto O, Ono K, McLean WHI, Shimizu H. 2018. Gentamicin-induced readthrough and nonsense-mediated mRNA decay of SERPINB7 nonsense mutant transcripts. Journal of Investigative Dermatology. 138(4):836-843. Available from: 10.1016/j.jid.2017.10.014

Owen RA, Fyfe PK, Lodge A, Biboy J, Vollmer W, Hunter WN, Sargent F. 2018. Structure and activity of ChiX, a peptidoglycan hydrolase required for chitinase secretion by Serratia marcescens. Biochemical Journal. 475(2):415-428. Available from: 10.1042/BCJ20170633

Parren LJMT, Baron JM, Joussen S, Marquardt Y, Hanneken S, van Steensel MAM, Steijlen PM, van Geel M, Frank J. 2018. CYLD mutations differentially affect splicing and mRNA decay in Brooke-Spiegler syndrome. Journal of the European Academy of Dermatology and Venereology. Available from: 10.1111/jdv.14889

Pedron J, Boudot C, Hutter S, Bourgeade-Delmas S, Stigliani J-L, Sournia-Saquet A, Moreau A, Boutet-Robinet E, Paloque L, Mothes E, Laget M, Vendier L, Pratviel G, Wyllie S, Fairlamb A, Azas N, Courtioux B, Valentin A, Verhaeghe P. 2018. Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study. European Journal of Medicinal Chemistry. 155:135-152. Available from: 10.1016/j.ejmech.2018.06.001

Pigors M, Common JEA, Wong XFCC, Malik S, Scott CA, Tabarra N, Liany H, Liu J, Limviphuvadh V, Maurer-Stroh S, Tang MB, Lench N, Margolis DJ, van Heel DA, Mein CA, Novak N, Baurecht H, Weidinger S, McLean WHI, Irvine AD, O'Toole EA, Simpson MA, Kelsell DP. 2018. Exome sequencing and rare variant analysis reveals multiple filaggrin mutations in Bangladeshi atopic eczema families and additional risk genes. Journal of Investigative Dermatology. Available from: 10.1016/j.jid.2018.05.013

Portnoi M-F, Dumargne M-C, Rojo S, Witchel SF, Duncan AJ, Eozenou C, Bignon-Topalovic J, Yatsenko SA, Rajkovic A, Reyes-Mugica M, Almstrup K, Fusee L, Srivastava Y, Chantot-Bastaraud S, Hyon C, Louis-Sylvestre C, Validire P, de Malleray Pichard C, Ravel C, Christin-Maitre S, Brauner R, Rossetti R, Persani L, Charreau EH, Dain L, Chiauzzi VA, Mazen I, Rouba H, Schluth-Bolard C, MacGowan S, McLean WHI, Patin E, Rajpert-De Meyts E, Jauch R, Achermann JC, Siffroi J-P, McElreavey K, Bashamboo A. 2018. Mutations involving the SRY-related gene SOX8 are associated with a spectrum of human reproductive anomalies. Human Molecular Genetics. 27(7):1228-1240. Available from: 10.1093/hmg/ddy037

Prati F, Zuccotto F, Fletcher D, Convery MA, Fernandez-Menendez R, Bates R, Encinas L, Zeng J, Chung C-W, De Dios Anton P, Mendoza-Losana A, Mackenzie C, Green SR, Huggett M, Barros D, Wyatt PG, Ray PC. 2018. Screening of a novel fragment library with functional complexity against Mycobacterium tuberculosis InhA. ChemMedChem. 13(7):672-677. Available from: 10.1002/cmdc.201700774

Quintata J, Del Pino RC, Yamada K, Zhang N, Field MC. 2018. Adaptation and therapeutic exploration: a two edged tale of membrane space in trypanosomes. Genes 9, 368

Rico Vidal E, Jeacock L, Kovarova J, Horn D. 2018. Inducible high-efficiency CRISPR-Cas9-targeted gene editing and precision base editing in African trypanosomes. Scientific Reports. 8:1-10. Available from: 1038/s41598-018-26303-w

Roekevisch E, Leeflang MMG, Schram ME, Campbell LE, Irwin McLean WH, Kezic S, Bos JD, Spuls PI, Middelkamp-Hup MA. 2018. Patients with filaggrin loss-of-function mutations show good but lower responses to immunosuppressive treatment. British Journal of Dermatology. 177(6):1745-1746. Available from: 10.1111/bjd.15191

Runcie A, Zengerle M, Chan KH, Testa A, Van Beurden L, Baud M, Epemolu R, Ellis L, Read K, Coulthard V, Brien A, Ciulli A. 2018. Optimization of a “Bump-and-Hole” Approach to Allele-Selective BET Bromodomain Inhibition. Chemical Science. 2018(9):2452-2468. Available from: 10.1039/C7SC02536J

Sienkiewicz N, Ong H, Fairlamb A. 2018. Characterisation of a putative glutamate 5‐kinase from Leishmania donovani. FEBS Journal. Available from: 10.1111/febs.14511

Soares P, Lucas X, Ciulli A. 2018. Thioamide substitution to probe the hydroxyproline recognition of VHL ligands. Bioorganic & Medicinal Chemistry. Available from: 10.1016/j.bmc.2018.03.034

Soares P, Gadd MS, Frost J, Galdeano C, Ellis L, Epemolu O, Rocha S, Read KD, Ciulli A. 2018. Group-based optimization of potent and cell-active inhibitors of the von Hippel-Lindaw (VHL) E3 ubiquitin ligase: structure-activity relationships leading to the chemical probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrodlidine-2-carboxamide (VH298). J Med Chem 61: 599-618.

Steketee PC, Vincent IM, Achcar F, Giordani F, Kim DH, Creek DJ, Freund Y, Jacobs R, Rattigan K, Horn D, Field MC, MacLeod A, Barrett MP. 2018. Benzoxaborole treatment perturbs S-adenosyl-L-methionine metabolism in Trypanosoma brucei. PLoS Neglected Tropical Diseases. 12(5). Available from: 10.1371/journal.pntd.0006450

Testa A, Lucas X, Castro G, Chan K-H, Wright J, Runcie A, Gadd M, Harrison WTA, Ko E-J, Fletcher D, Ciulli A. 2018. 3-Fluoro-4-hydroxyprolines: Synthesis, conformational analysis and stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation. Journal of the American Chemical Society. Available from: 10.1021/jacs.8b05807

Venkatesh D, Zhang N, Zoltner M, Canavate Del Pino R, Field MC. 2018. Evolution of protein trafficking in kinetoplastid parasites: complexity and pathogenesis. Traffic. Available from: 10.1111/tra.12601

Wall R, Moniz S, Thomas M, Norval S, Ko EJ, Marco M, Miles TJ, Gilbert I, Horn D, Fairlamb A, Wyllie S. 2018. Anti-trypanosomal 8-hydroxyl naphthyridines are chelators of divalent transition metals. Antimicrobial Agents and Chemotherapy. Available from: 10.1128/AAC.00235-18

Wyllie S, Thomas M, Patterson S, Crouch S, De Rycker M, Lowe R, Gresham S, Urbaniak MD, Otto TD, Stojanovski L, Simeons FRC, Manthri S, MacLean LM, Zuccotto F, Homeyer N, Pflaumer H, Boesche M, Sastry L, Connolly P, Albrecht S, Berriman M, Drewes G, Gray DW, Ghidelli-Disse S, Dixon S, Fiandor JM, Wyatt PG, Fergucaon MAJ, Fairlamb AH, Miles TJ, Read KD, Gilbert IH. 2018. Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis. Nature 560(7717): 192-197

Wong XFCC, Denil SLIJ, Foo JN, Chen H, Ling Tay AS, Haines RL, Tang MBY, McLean WHI, Sandilands A, Smith FJD, Lane EB, Liu J, Common JEA. 2018. Array-based sequencing of filaggrin gene for comprehensive detection of disease-associated variants. Journal of Allergy and Clinical Immunology. 141(2):814-816. Available from: 10.1016/j.jaci.2017.10.001

Zhang N, Zoltner M, Leung K-F, Scullion P, Hutchinson S, Del Pino RC, Vincent IM, Zhang Y-K, Freund YR, Alley MRK, Jacobs RT, Read KD, Barrett MP, Horn D, Field MC. 2018. Host-parasite co-metabolic activation of antitrypanosomal aminomethyl-benzoxaboroles. PLoS Pathogens. 14(2): e1006850. Available from: 10.1371/journal.ppat.1006850