Biological Chemistry and Drug Discovery

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2019
1 Citation (Scopus)
55 Downloads (Pure)

A chemical-genetics approach to study the role of atypical Protein Kinase C in Drosophila

Hannaford, M., Loyer, N., Tonelli, F., Zoltner, M. & Januschke, J., 29 Jan 2019, In : Development. 146, 2, p. 1-11 11 p., dev170589.

Research output: Contribution to journalArticle

Open Access
File
Drosophila
Phosphotransferases
Drosophila Proteins
Cell Polarity
Nuclear Envelope
31 Downloads (Pure)

A high-throughput screen for the identification of compounds that inhibit nematode gene expression by targeting spliced leader trans-splicing

Pandarakalam, G. C., Speake, M., McElroy, S., Alturkistani, A., Philippe, L., Pettitt, J., Müller, B. & Connolly, B., Aug 2019, In : International Journal for Parasitology: Drugs and Drug Resistance. 10, p. 28-37 10 p.

Research output: Contribution to journalArticle

Open Access
File
Spliced Leader RNA
Trans-Splicing
Gene Targeting
Anthelmintics
Gene Expression

Amino acid substitutions in the human homomeric β3 GABAA receptor that enable activation by GABA

Gottschald Chiodi, C., Baptista-Hon, D., Hunter, W. & Hales, T., 15 Feb 2019, In : Journal of Biological Chemistry. 294, 7, p. 2375-2385 11 p.

Research output: Contribution to journalArticle

GABA-A Receptors
Amino Acid Substitution
gamma-Aminobutyric Acid
Substitution reactions
Chemical activation
65 Downloads (Pure)
Open Access
File
Methylenetetrahydrofolate Dehydrogenase (NADP)
dehydrogenases
inhibitors
Ligands
enzymes
25 Downloads (Pure)

An Extensively Humanized Mouse Model to Predict Pathways of Drug Disposition and Drug/Drug Interactions, and to Facilitate Design of Clinical Trials

Henderson, C. J., Kapelyukh, Y., Scheer, N., Rode, A., McLaren, A., MacLeod, K., Lin, D., Wright, J., Stanley, L. A. & Wolf, C. R., Jun 2019, In : Drug Metabolism and Disposition. 47, 6, p. 601-615 15 p.

Research output: Contribution to journalArticle

Open Access
File
Drug Interactions
Clinical Trials
Pharmaceutical Preparations
Pharmacokinetics
Cytochrome P-450 CYP3A
5 Downloads (Pure)

A post-transcriptional respiratome regulon in trypanosomes

Trenaman, A., Glover, L., Hutchinson, S. & Horn, D., 26 Jul 2019, In : Nucleic Acids Research. 47, 13, p. 7063-7077 15 p.

Research output: Contribution to journalArticle

Open Access
File
Regulon
Trypanosomiasis
Membrane Glycoproteins
Trypanosoma brucei brucei
RNA-Binding Proteins
1 Citation (Scopus)

Author Correction: Landscape of somatic mutations in 560 breast cancer whole-genome sequences

Nik-Zainal, S., Davies, H., Staaf, J., Ramakrishna, M., Glodzik, D., Zou, X., Martincorena, I., Alexandrov, L. B., Martin, S., Wedge, D. C., Van Loo, P., Ju, Y. S., Smid, M., Brinkman, A. B., Morganella, S., Aure, M. R., Lingjærde, O. C., Langerød, A., Ringnér, M., Ahn, S-M. & 68 others, Boyault, S., Brock, J. E., Broeks, A., Butler, A., Desmedt, C., Dirix, L., Dronov, S., Fatima, A., Foekens, J. A., Gerstung, M., Hooijer, G. K. J., Jang, S. J., Jones, D. R., Kim, H-Y., King, T. A., Krishnamurthy, S., Lee, H. J., Lee, J-Y., Li, Y., McLaren, S., Menzies, A., Mustonen, V., O'Meara, S., Pauporté, I., Pivot, X., Purdie, C. A., Raine, K., Ramakrishnan, K., Rodríguez-González, F. G., Romieu, G., Sieuwerts, A. M., Simpson, P. T., Shepherd, R., Stebbings, L., Stefansson, O. A., Teague, J., Tommasi, S., Treilleux, I., Van den Eynden, G. G., Vermeulen, P., Vincent-Salomon, A., Yates, L., Caldas, C., Van't Veer, L., Tutt, A., Knappskog, S., Tan, B. K. T., Jonkers, J., Borg, Å., Ueno, N. T., Sotiriou, C., Viari, A., Futreal, P. A., Campbell, P. J., Span, P. N., Van Laere, S., Lakhani, S. R., Eyfjord, J. E., Thompson, A. M., Birney, E., Stunnenberg, H. G., van de Vijver, M. J., Martens, J. W. M., Børresen-Dale, A-L., Richardson, A. L., Kong, G., Thomas, G. & Stratton, M. R., 7 Feb 2019, In : Nature. 566, 7742, p. E1 1 p.

Research output: Contribution to journalArticle

Genome
Breast Neoplasms
Mutation
3 Citations (Scopus)

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

Farnaby, W., Koegl, M., Roy, M. J., Whitworth, C., Diers, E., Trainor, N., Zollman, D., Steurer, S., Karolyi-Oezguer, J., Riedmueller, C., Gmaschitz, T., Wachter, J., Dank, C., Galant, M., Sharps, B., Rumpel, K., Traxler, E., Gerstberger, T., Schnitzer, R., Petermann, O. & 17 others, Greb, P., Weinstabl, H., Bader, G., Zoephel, A., Weiss-Puxbaum, A., Ehrenhöfer-Wölfer, K., Wöhrle, S., Boehmelt, G., Rinnenthal, J., Arnhof, H., Wiechens, N., Wu, M-Y., Owen-Hughes, T., Ettmayer, P., Pearson, M., McConnell, D. B. & Ciulli, A., Jul 2019, In : Nature Chemical Biology. 15, 7, p. 672-680 9 p.

Research output: Contribution to journalArticle

Proteolysis
Adenosine Triphosphatases
Biophysics
Neoplasms
Chromatin Assembly and Disassembly
10 Downloads (Pure)
Open Access
File
Burkholderia pseudomallei
Adenosine Monophosphate
Anti-Bacterial Agents
Ligands
Enzymes
1 Citation (Scopus)

Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs

Girardini, M., Maniaci, C., Hughes, S., Testa, A. & Ciulli, A., 15 Jun 2019, In : Bioorganic & Medicinal Chemistry. 27, 12, p. 2466-2479 14 p.

Research output: Contribution to journalArticle

Open Access
Proteolysis
Ubiquitin-Protein Ligases
Degradation
Cullin Proteins
Ubiquitination
65 Downloads (Pure)

Characterising Covalent Warhead Reactivity

Martin, J., Mackenzie, C., Fletcher, D. & Gilbert, I., 15 May 2019, In : Bioorganic & Medicinal Chemistry. 27, 10, p. 2066-2074 9 p.

Research output: Contribution to journalArticle

Open Access
File
Toxicity
Pharmaceutical Preparations
Aptitude
Pharmacokinetics
Threonine
11 Downloads (Pure)

Chemogenomic Profiling of Antileishmanial Efficacy and Resistance in the Related Kinetoplastid Parasite Trypanosoma brucei

Collett, C. F., Kitson, C., Baker, N., Steele-Stallard, H. B., Santrot, M-V., Hutchinson, S., Horn, D. & Alsford, S., Aug 2019, In : Antimicrobial Agents and Chemotherapy. 63, 8, p. 1-19 19 p., e00795-19.

Research output: Contribution to journalArticle

Open Access
File
Trypanosoma brucei brucei
miltefosine
Parasites
Pharmaceutical Preparations
Leishmania

Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader

Tovell, H., Testa, A., Zhou, H., Shpiro, N., Crafter, C., Ciulli, A. & Alessi, D., 28 Aug 2019, In : ACS Chemical Biology. 11 p.

Research output: Contribution to journalArticle

Phosphatidylinositol 3-Kinases
Protein Isoforms
Phosphotransferases
Cells
Degradation
1 Citation (Scopus)
49 Downloads (Pure)

Differentiation-Induced Remodelling of Store-Operated Calcium Entry Is Independent of Neuronal or Glial Phenotype but Modulated by Cellular Context

Whitworth, C. L., Redfern, C. P. F. & Cheek, T. R., 1 Feb 2019, In : Molecular Neurobiology. 56, 2, p. 857-872 16 p.

Research output: Contribution to journalArticle

Open Access
File
Neuroglia
Calcium
Phenotype
Neurogenesis
Porins
50 Downloads (Pure)
Open Access
File
Lysosphingolipid Receptors
Drug Discovery
Modulators
Skin
Pharmaceutical Preparations
Obesity
Focus Groups
Weights and Measures
Public Health Practice
Health Priorities
10 Downloads (Pure)

Engineering a surrogate human heteromeric α/β glycine receptor orthosteric site exploiting the structural homology and stability of acetylcholine-binding protein

Dawson, A., Trumper, P., de Souza, J. O., Parker, H., Jones, M., Hales, T. G. & Hunter, W. N., 4 Sep 2019, In : IUCrJ. 6, Part 6, 10 p.

Research output: Contribution to journalArticle

Open Access
File
Glycine Receptors
Acetylcholine
Carrier Proteins
Binding Sites
Ligand-Gated Ion Channels

Filaggrin gene loss-of-function mutations constitute a factor in patients with multiple contact allergies

Elhaji, Y., Sasseville, D., Pratt, M., Asai, Y., Matheson, K., McLean, W. H. I. & Hull, P., Jun 2019, In : Contact Dermatitis. 80, 6, p. 354-358 5 p.

Research output: Contribution to journalArticle

Hypersensitivity
Mutation
Genes
Patch Tests
Dermatitis

Genome-wide association study of inhaled corticosteroid response in admixed children with asthma

Hernandez-Pacheco, N., Farzan, N., Francis, B., Karimi, L., Repnik, K., Vijverberg, S. J., Soares, P., Schieck, M., Gorenjak, M., Forno, E., Eng, C., Oh, S. S., Pérez-Méndez, L., Berce, V., Tavendale, R., Samedy, L. A., Hunstman, S., Hu, D., Meade, K., Farber, H. J. & 21 others, Avila, P. C., Serebrisky, D., Thyne, S. M., Brigino-Buenaventura, E., Rodriguez-Cintron, W., Sen, S., Kumar, R., Lenoir, M., Rodriguez-Santana, J. R., Celedón, J. C., Mukhopadhyay, S., Potočnik, U., Pirmohamed, M., Verhamme, K. M., Kabesch, M., Palmer, C. N. A., Hawcutt, D. B., Flores, C., van der Zee, A. H. M., Burchard, E. G. & Pino-Yanes, M., Jun 2019, In : Clinical and Experimental Allergy. 49, 6, p. 789-798 10 p.

Research output: Contribution to journalArticle

Genome-Wide Association Study
Adrenal Cortex Hormones
Asthma
Hispanic Americans
Population

High-Level Expression in Escherichia coli, Purification and Kinetic Characterization of LAPTc, a Trypanosoma cruzi M17-Aminopeptidase

Izquierdo, M., Aguado, M. E., Zoltner, M. & González-Bacerio, J., Apr 2019, In : Protein Journal. 38, 2, p. 167-180 14 p.

Research output: Contribution to journalArticle

Leucyl Aminopeptidase
Aminopeptidases
Trypanosoma cruzi
Escherichia coli
Purification

Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions

Popow, J., Arnhof, H., Bader, G., Berger, H., Ciulli, A., Covini, D., Dank, C., Gmaschitz, T., Greb, P., Karolyi-Özguer, J., Koegl, M., McConnell, D. B., Pearson, M., Rieger, M., Rinnenthal, J., Roessler, V., Schrenk, A., Spina, M., Steurer, S., Trainor, N. & 4 others, Traxler, E., Wieshofer, C., Zoephel, A. & Ettmayer, P., 14 Mar 2019, In : Journal of Medicinal Chemistry. 62, 5, p. 2508–2520 13 p.

Research output: Contribution to journalArticle

Focal Adhesion Protein-Tyrosine Kinases
Proteolysis
Hepatocellular Carcinoma
Cell Line
Ubiquitin-Protein Ligases
2 Citations (Scopus)

Human and computational models of atopic dermatitis: A review and perspectives by an expert panel of the International Eczema Council

Eyerich, K., Brown, S. J., Perez White, B. E., Tanaka, R. J., Bissonette, R., Dhar, S., Bieber, T., Hijnen, D. J., Guttman-Yassky, E., Irvine, A., Thyssen, J. P., Vestergaard, C., Werfel, T., Wollenberg, A., Paller, A. S. & Reynolds, N. J., 1 Jan 2019, In : Journal of Allergy and Clinical Immunology. 143, 1, p. 36-45 10 p.

Research output: Contribution to journalArticle

Eczema
Atopic Dermatitis
Therapeutics
Biological Models
Precision Medicine
3 Citations (Scopus)

Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis

Thomas, M. G., De Rycker, M., Ajakane, M., Albrecht, S., Álvarez-Pedraglio, A. I., Boesche, M., Brand, S., Campbell, L., Cantizani-Perez, J., Cleghorn, L. A. T., Copley, R. C. B., Crouch, S. D., Daugan, A., Drewes, G., Ferrer, S., Ghidelli-Disse, S., Gonzalez, S., Gresham, S. L., Hill, A. P., Hindley, S. J. & 32 others, Lowe, R. M., MacKenzie, C. J., MacLean, L., Manthri, S., Martin, F., Miguel-Siles, J., Nguyen, V. L., Norval, S., Osuna-Cabello, M., Woodland, A., Patterson, S., Pena, I., Quesada-Campos, M. T., Reid, I. H., Revill, C., Riley, J., Ruiz-Gomez, J. R., Shishikura, Y., Simeons, F. R. C., Smith, A., Smith, V. C., Spinks, D., Stojanovski, L., Thomas, J., Thompson, S., Underwood, T., Gray, D. W., Fiandor, J. M., Gilbert, I. H., Wyatt, P. G., Read, K. D. & Miles, T. J., 14 Feb 2019, In : Journal of Medicinal Chemistry. 62, 3, p. 1180-1202 23 p.

Research output: Contribution to journalArticle

Visceral Leishmaniasis
Leishmania major
Leishmania donovani
Standard of Care
Solubility
20 Downloads (Pure)

Identification of inhibitors of an unconventional Trypanosoma brucei kinetochore kinase

Torrie, L., Zuccotto, F., Robinson, D., Gray, D., Gilbert, I. & De Rycker, M., 31 May 2019, In : PLoS ONE. 14, 5, p. 1-16 16 p., e0217828.

Research output: Contribution to journalArticle

Open Access
File
Kinetochores
Trypanosoma brucei
kinetochores
Trypanosoma brucei brucei
phosphotransferases (kinases)
2 Citations (Scopus)
50 Downloads (Pure)

Identification of Leishmania major UDP-Sugar Pyrophosphorylase Inhibitors Using Biosensor-Based Small Molecule Fragment Library Screening

Prakash, O., Führing, J., Post, J., Shepherd, S. M., Eadsforth, T. C., Gray, D., Fedorov, R. & Routier, F. H., 12 Mar 2019, In : Molecules and Cells. 24, 5, p. 1-16 16 p., 996.

Research output: Contribution to journalArticle

Open Access
File
Uridine Diphosphate Sugars
Small Molecule Libraries
Leishmania major
Biosensing Techniques
sugars
10 Downloads (Pure)

Identification of Novel Trypanosoma cruzi Proteasome Inhibitors Using a Luminescence-Based High-Throughput Screening Assay

Zmuda, F., Sastry, L., Shepherd, S. M., Jones, D., Scott, A., Craggs, P. D., Cortes, A., Gray, D. W., Torrie, L. S. & De Rycker, M., Sep 2019, In : Antimicrobial Agents and Chemotherapy. 63, 9, p. 1-15 15 p., e00309-19.

Research output: Contribution to journalArticle

Open Access
File
High-Throughput Screening Assays
Proteasome Inhibitors
Trypanosoma cruzi
Proteasome Endopeptidase Complex
Luminescence

Inhibition of CorA dependent Magnesium Homeostasis is cidal in Mycobacterium tuberculosis

Park, Y., Ahn, Y-M., Jonnala, S., Oh, S., Fisher, J. M., Goodwin, M. B., Loerger, T. R., Via, L. E., Bayliss, T., Green, S. R., Ray, P. C., Wyatt, P. G., Barry, C. E. & Boshoff, H. I., 5 Aug 2019, In : Antimicrobial Agents and Chemotherapy. 37 p.

Research output: Contribution to journalArticle

Mycobacterium tuberculosis
Magnesium
Homeostasis
Amides
Drug Discovery
1 Citation (Scopus)
85 Downloads (Pure)

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis

Baragaña, B., Forte, B., Choi, R., Nakazawa Hewitt, S., Bueren-Calabuig, J. A., Pisco, J. P., Peet, C., Dranow, D. M., Robinson, D. A., Jansen, C., Norcross, N. R., Vinayak, S., Anderson, M., Brooks, C. F., Cooper, C. A., Damerow, S., Delves, M., Dowers, K., Duffy, J., Edwards, T. E. & 57 others, Hallyburton, I., Horst, B. G., Hulverson, M. A., Ferguson, L., Jiménez-Díaz, M. B., Jumani, R. S., Lorimer, D. D., Love, M. S., Maher, S., Matthews, H., McNamara, C. W., Miller, P., O'Neill, S., Ojo, K. K., Osuna-Cabello, M., Pinto, E., Post, J., Riley, J., Rottmann, M., Sanz, L. M., Scullion, P., Sharma, A., Shepherd, S. M., Shishikura, Y., Simeons, F. R. C., Stebbins, E. E., Stojanovski, L., Straschil, U., Tamaki, F. K., Tamjar, J., Torrie, L. S., Vantaux, A., Witkowski, B., Wittlin, S., Yogavel, M., Zuccotto, F., Angulo-Barturen, I., Sinden, R., Baum, J., Gamo, F-J., Mäser, P., Kyle, D. E., Winzeler, E. A., Myler, P. J., Wyatt, P. G., Floyd, D., Matthews, D., Sharma, A., Striepen, B., Huston, C. D., Gray, D. W., Fairlamb, A. H., Pisliakov, A. V., Walpole, C., Read, K. D., Van Voorhis, W. C. & Gilbert, I. H., 2 Apr 2019, In : Proceedings of the National Academy of Sciences. 116, 14, p. 7015-7020 6 p.

Research output: Contribution to journalArticle

Open Access
File
Lysine-tRNA Ligase
Cryptosporidiosis
Cryptosporidium parvum
Malaria
Plasmodium falciparum
7 Downloads (Pure)
Open Access
File
Guanine
Methyltransferases
Molecular Dynamics Simulation
RNA
S-Adenosylmethionine
41 Downloads (Pure)

Molecular and bioinformatics analyses reveal two differentially expressed intracellular GH1 β-glucosidases from the rare alkalophilic fungus Stachybotrys microspora

Abdeljalil, S., Borgi, I., Carvalho, S., Jmal-Hammami, L. & Gargouri, A., 30 Jun 2019, In : Gene. 703, p. 134-144 11 p.

Research output: Contribution to journalArticle

Open Access
File
Stachybotrys
Microsporidia
Glucosidases
Computational Biology
Fungi
4 Downloads (Pure)

Monoallelic expression and epigenetic inheritance sustained by a Trypanosoma brucei variant surface glycoprotein exclusion complex

Correia Faria, J., Glover, L., Hutchinson, S., Boehm, C., Field, M. C. & Horn, D., 9 Jul 2019, In : Nature Communications. 10, p. 1-14 14 p., 3023.

Research output: Contribution to journalArticle

Open Access
File
Trypanosoma Variant Surface Glycoproteins
Trypanosoma brucei brucei
Membrane Glycoproteins
exclusion
Epigenomics
2 Citations (Scopus)
91 Downloads (Pure)

Nongenotoxic 3-Nitroimidazo[1,2-a]pyridines Are NTR1 Substrates That Display Potent in Vitro Antileishmanial Activity

Fersing, C., Basmaciyan, L., Boudot, C., Pedron, J., Hutter, S., Cohen, A., Castera-Ducros, C., Primas, N., Laget, M., Casanova, M., Bourgeade-Delmas, S., Piednoel, M., Sournia-Saquet, A., Belle Mbou, V., Courtioux, B., Boutet-Robinet, É., Since, M., Milne, R., Wyllie, S., Fairlamb, A. H. & 5 others, Valentin, A., Rathelot, P., Verhaeghe, P., Vanelle, P. & Azas, N., 10 Jan 2019, In : ACS Medicinal Chemistry Letters. 10, 1, p. 34-39 6 p.

Research output: Contribution to journalArticle

Open Access
File
Pyridines
Inhibitory Concentration 50
sulfoxide
miltefosine
Display devices
47 Downloads (Pure)

Optimisation of a Key Cross-Coupling Reaction Towards the Synthesis of a Promising Antileishmanial Compound

Velasco, R. F., Guerrero, C., Fra, G., Moure, A., Miguel-Siles, J., Quesada-Campos, M. T., Ruiz-Gomez, J. R., Gilbert, I. H., Thomas, M. G. & Miles, T. J., 2 May 2019, In : Tetrahedron Letters. 60, 18, p. 1243-1247 5 p.

Research output: Contribution to journalArticle

Open Access
File
Sulfonamides
Cross Reactions
Research
8 Downloads (Pure)

Persistent DNA Damage Foci and DNA Replication with a Broken Chromosome in the African Trypanosome

Glover, L., Marques, C., Suska, O. & Horn, D., 9 Jul 2019, In : MBio. 10, 4, p. 1-17 17 p., e01252-19.

Research output: Contribution to journalArticle

Open Access
File
Trypanosomiasis
DNA Replication
DNA Damage
Replication Protein A
Chromosomes
75 Downloads (Pure)
Open Access
File
Leishmania donovani
Pharmacology
Parasites
Enzymes
Pharmaceutical Preparations
27 Downloads (Pure)

Phosphatidylcholine synthesis through cholinephosphate cytidylyltransferase is dispensable in Leishmania major

Moitra, S., Pawlowic, M. C., Hsu, F-F. & Zhang, K., 20 May 2019, In : Scientific Reports. 9, p. 1-13 13 p., 7602.

Research output: Contribution to journalArticle

Open Access
File
Leishmania major
Phosphatidylcholines
Parasites
Choline
Psychodidae
1 Citation (Scopus)
52 Downloads (Pure)

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition

Wyllie, S., Brand, S., Thomas, M., De Rycker, M., Chung, C-W., Peña, I., Bingham, R., Bueren-Calabuig, J., Cantizani, J., Cebrian, D., Craggs, P. D., Ferguson, L., Goswami, P., Hobrath, J., Howe, J., Jeacock, L., Ko, E. J., Korczynska, J., MacLean, L., Manthri, S. & 29 others, Santos Martinez, M., Mata-Cantero, L., Moniz, S., Nuhs, A., Osuna-Cabello, M., Pinto, E., Riley, J., Robinson, S., Rowland, P., Simeons, F., Shishikura, Y., Spinks, D., Stojanovski, L., Thomas, J., Thompson, S., Viayna Gaza, E., Wall, R., Zuccotto, F., Horn, D., Ferguson, M., Fairlamb, A., Fiandor, J. M., Martín, J., Gray, D., Miles, T. J., Gilbert, I., Read, K., Marco, M. & Wyatt, P., 7 May 2019, In : Proceedings of the National Academy of Sciences. 116, 19, p. 9318-9323 6 p., 201820175.

Research output: Contribution to journalArticle

Open Access
File
Leishmania infantum
Visceral Leishmaniasis
Proteasome Endopeptidase Complex
Leishmania donovani
Parasites

Publisher Correction: BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

Farnaby, W., Koegl, M., Roy, M. J., Whitworth, C., Diers, E., Trainor, N., Zollman, D., Steurer, S., Karolyi-oezguer, J., Riedmueller, C., Gmaschitz, T., Wachter, J., Dank, C., Galant, M., Sharps, B., Rumpel, K., Traxler, E., Gerstberger, T., Schnitzer, R., Petermann, O. & 17 others, Greb, P., Weinstabl, H., Bader, G., Zoephel, A., Weiss-Puxbaum, A., Ehrenhöfer-Wölfer, K., Wöhrle, S., Boehmelt, G., Rinnenthal, J., Arnhof, H., Wiechens, N., Wu, M-Y., Owen-Hughes, T., Ettmayer, P., Pearson, M., Mcconnell, D. B. & Ciulli, A., 2 Jul 2019, In : Nature Chemical Biology. 15, 8, p. 846 1 p.

Research output: Contribution to journalArticle

Chromatin Assembly and Disassembly
Ubiquitin-Protein Ligases
Nucleosomes
DNA Repair
Chromatin
1 Citation (Scopus)
66 Downloads (Pure)

Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader

Tovell, H., Testa, A., Maniaci, C., Zhou, H., Prescott, A., Macartney, T., Ciulli, A. & Alessi, D., 17 May 2019, In : ACS Chemical Biology. 14, 5, p. 882-892 11 p.

Research output: Contribution to journalArticle

Open Access
File
Degradation
Clustered Regularly Interspaced Short Palindromic Repeats
Proteins
Ubiquitination
Phosphorylation
5 Citations (Scopus)

Rapid and scale-independent microfluidic manufacture of liposomes entrapping protein incorporating in-line purification and at-line size monitoring

Forbes, N., Hussain, M. T., Briuglia, M. L., Edwards, D. Y., Horst, J. H. T., Szita, N. & Perrie, Y., 10 Feb 2019, In : International Journal of Pharmaceutics. 556, p. 68-81 14 p.

Research output: Contribution to journalArticle

Microfluidics
Liposomes
Proteins
Sonication
Particle Size
40 Downloads (Pure)

Reprogramming of Trypanosoma cruzi metabolism triggered by parasite interaction with the host cell extracellular matrix

Mattos, E. C., Canuto, G., Varón, N. C. M., Magalhães, R. D. M., Crozier, T. W. M., Lamont, D. J., Tavares, M. F. M., Colli, W., Ferguson, M. A. J. & Alves, M. J. M., 6 Feb 2019, In : PLoS Neglected Tropical Diseases. 13, 2, p. 1-27 27 p., e0007103.

Research output: Contribution to journalArticle

Open Access
File
Host-Parasite Interactions
Trypanosoma cruzi
Extracellular Matrix
Phosphorylation
Parasites
57 Downloads (Pure)

RNA-seq analysis of PHD and VHL inhibitors reveals differences and similarities to the hypoxia response

Frost, J., Ciulli, A. & Rocha, S., 29 Jan 2019, In : Wellcome Open Research. 4, p. 1-17 17 p., 17.

Research output: Contribution to journalArticle

File
Prolyl Hydroxylases
Genes
RNA
Prolyl-Hydroxylase Inhibitors
Chemical activation
5 Citations (Scopus)
107 Downloads (Pure)

SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate

Roy, M., Winkler, S., Hughes, S. J., Whitworth, C., Galant, M., Farnaby, W., Rumpel, K. & Ciulli, A., 15 Mar 2019, In : ACS Chemical Biology. 14, 3, p. 361-368 8 p.

Research output: Contribution to journalArticle

Open Access
File
Proteolysis
Enzyme kinetics
Degradation
Ubiquitin-Protein Ligases
Assays
2 Citations (Scopus)
23 Downloads (Pure)

Spy vs. Spy: Selecting the best reporter for 19F NMR competition experiment

Castro, G. V. D. & Ciulli, A., 4 Feb 2019, In : Chemical Communications. 55, 10, p. 1482-1485 4 p.

Research output: Contribution to journalArticle

Open Access
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Assays
Screening
Ligands
Nuclear magnetic resonance
Molecules
1 Citation (Scopus)
22 Downloads (Pure)

Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase

Kung, W-W., Ramachandran, S., Makukhin, N., Bruno, E. & Ciulli, A., 10 Jun 2019, In : Nature Communications. 10, 1, p. 1-14 14 p., 2534.

Research output: Contribution to journalArticle

Open Access
File
suppressors
Ubiquitin-Protein Ligases
Cytokines
Substrates
Erythropoietin Receptors
3 Citations (Scopus)

Studies on the inhibition of AmpC and other β-lactamases by cyclic boronates

Cahill, S. T., Tyrrell, J. M., Navratilova, I. H., Calvopiña, K., Robinson, S. W., Lohans, C. T., McDonough, M. A., Cain, R., Fishwick, C. W. G., Avison, M. B., Walsh, T. R., Schofield, C. J. & Brem, J., 1 Apr 2019, In : Biochimica et Biophysica Acta: General Subjects. 1863, 4, p. 742-748 7 p.

Research output: Contribution to journalArticle

meropenem
Lactams
Enterobacteriaceae
Catalysis
Bacterial Infections
13 Downloads (Pure)

Substituted Aminoacetamides as Novel Leads for Malaria Treatment

Norcross, N., Wilson, C., Baragana, B., Hallyburton, I., Osuna-Cabello, M., Norval, S., Riley, J., Fletcher, D., Sinden, R., Delves, M. J., Ruecker, A., Duffy, S., Meister, S., Antonova-Koch, Y., Crespo, B., de Cózar, C., Sanz, L., Gamo, F-J., Avery, V. M., Frearson, J. A. & 8 others, Gray, D., Fairlamb, A., Winzeler, E. A., Waterson, D., Campbell, S. F., Willis, P., Read, K. & Gilbert, I., 17 Jul 2019, In : ChemMedChem. 14, 14, p. 1329-1335 7 p.

Research output: Contribution to journalArticle

Pharmacokinetics
Antimalarials
Germ Cells
Scaffolds
Malaria
4 Downloads (Pure)

Systematic analysis of Plasmodium myosins reveals differential expression, localisation, and function in invasive and proliferative parasite stages

Wall, R. J., Zeeshan, M., Katris, N. J., Limenitakis, R., Rea, E., Stock, J., Brady, D., Waller, R. F., Holder, A. A. & Tewari, R., 23 Jul 2019, In : Cellular Microbiology. e13082.

Research output: Contribution to journalArticle

Open Access
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Plasmodium
Myosins
Parasites
Apicomplexa
Actomyosin
59 Downloads (Pure)
Open Access
File
Burkholderia pseudomallei
Lipopolysaccharides
Lipid A
Carrier Proteins
lipids
4 Citations (Scopus)
35 Downloads (Pure)

TP53 mutation status divides myelodysplastic syndromes with complex karyotypes into distinct prognostic subgroups

Haase, D., Stevenson, K. E., Neuberg, D., Maciejewski, J. P., Nazha, A., Sekeres, M. A., Ebert, B. L., Garcia-Manero, G., Haferlach, C., Haferlach, T., Kern, W., Ogawa, S., Nagata, Y., Yoshida, K., Graubert, T. A., Walter, M. J., List, A. F., Komrokji, R. S., Padron, E., Sallman, D. & 30 others, Papaemmanuil, E., Campbell, P. J., Savona, M. R., Seegmiller, A., Adès, L., Fenaux, P., Shih, L. Y., Bowen, D., Groves, M. J., Tauro, S., Fontenay, M., Kosmider, O., Bar-Natan, M., Steensma, D., Stone, R., Heuser, M., Thol, F., Cazzola, M., Malcovati, L., Karsan, A., Ganster, C., Hellström-Lindberg, E., Boultwood, J., Pellagatti, A., Santini, V., Quek, L., Vyas, P., Tüchler, H., Greenberg, P. L. & Bejar, R., Jul 2019, In : Leukemia. 33, 7, p. 1747-1758 12 p.

Research output: Contribution to journalArticle

Open Access
File
Myelodysplastic Syndromes
Karyotype
Mutation
Chromosome Aberrations
Critical Care