Biological Chemistry and Drug Discovery

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Research Output 1972 2020

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Review article
2019

Bifunctional chemical probes inducing protein-protein interactions

Maniaci, C. & Ciulli, A., 13 Aug 2019, In : Current Opinion in Chemical Biology. 52, p. 145-156 12 p.

Research output: Contribution to journalReview article

Proteins
Ubiquitin-Protein Ligases
Molecules
Glues
Adhesives
37 Downloads (Pure)

Pore timing: the evolutionary origins of the nucleus and nuclear pore complex

Field, M. C. & Rout, M. P., 3 Apr 2019, In : F1000Research. 8, p. 1-11 11 p., 369.

Research output: Contribution to journalReview article

Open Access
File
Nuclear Pore
Eukaryota
Bacteria
Archaea
Cell Nucleus
2018
81 Downloads (Pure)

Adaptation and therapeutic exploitation of the plasma membrane of African trypanosomes

Quintana, J. F., Canavate Del Pino, R., Yamada, K., Zhang, N. & Field, M., 20 Jul 2018, In : Genes. 9, 7, 16 p., 368.

Research output: Contribution to journalReview article

Open Access
File
Immune Evasion
Trypanosomiasis
Cell Membrane
Membranes
Organelles
31 Citations (Scopus)
16 Downloads (Pure)

BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease

Prati, F., Bottegoni, G., Bolognesi, M. L. & Cavalli, A., 8 Feb 2018, In : Journal of Medicinal Chemistry. 61, 3, p. 619-637 19 p.

Research output: Contribution to journalReview article

Open Access
File
Alzheimer Disease
Drug Discovery
Amyloid
Amyloid beta-Protein Precursor
Pharmaceutical Preparations
13 Citations (Scopus)
98 Downloads (Pure)

Challenges and recent progress in drug discovery for tropical diseases

De Rycker, M., Baragaña, B., Duce, S. L. & Gilbert, I. H., 25 Jul 2018, In : Nature. 559, 7715, p. 498-506 9 p.

Research output: Contribution to journalReview article

Open Access
File
Drug Discovery
Pharmaceutical Preparations
Communicable Diseases
Economics
Morbidity
1 Citation (Scopus)

Conservation and Variation in Strategies for DNA Replication of Kinetoplastid Nuclear Genomes

Marques, C. A. & McCulloch, R., Feb 2018, In : Current Genomics. 19, 2, p. 98-109 12 p.

Research output: Contribution to journalReview article

Trypanosoma brucei brucei
DNA Replication
Origin Recognition Complex
Genome
Leishmania
55 Downloads (Pure)
Open Access
File
Nitro Compounds
Leishmaniasis
Trypanosomiasis
Parasites
Nifurtimox
4 Citations (Scopus)
58 Downloads (Pure)

Evolutionary origins and specialisation of membrane transport

Dacks, J. B. & Field, M. C., 1 Aug 2018, In : Current Opinion in Cell Biology. 53, p. 70-76 7 p.

Research output: Contribution to journalReview article

Open Access
File
Organelles
Intracellular Membranes
Membranes
Eukaryotic Cells
Cellular Structures
10 Downloads (Pure)

Evolution of protein trafficking in kinetoplastid parasites: complexity and pathogenesis

Venkatesh, D., Zhang, N., Zoltner, M., Canavate Del Pino, R. & Field, M. C., Nov 2018, In : Traffic. 19, 11, p. 803-812 10 p.

Research output: Contribution to journalReview article

Open Access
File
Protein Transport
Parasites
Kinetoplastida
Plastids
Host Specificity
12 Citations (Scopus)
58 Downloads (Pure)

Melarsoprol Resistance in African Trypanosomiasis

Fairlamb, A. & Horn, D., Jun 2018, In : Trends in Parasitology. 34, 6, p. 481-492 12 p.

Research output: Contribution to journalReview article

Open Access
File
Melarsoprol
African Trypanosomiasis
Parasites
Drug Resistance
Pharmaceutical Preparations
4 Citations (Scopus)
157 Downloads (Pure)

Using Microscale Thermophoresis to Characterize Hits from High-Throughput Screening: A European Lead Factory Perspective

Rainard, J. M., Pandarakalam, G. C. & McElroy, S. P., 1 Mar 2018, In : SLAS Discovery. 23, 3, p. 225-241 17 p.

Research output: Contribution to journalReview article

Open Access
File
Thermophoresis
Industrial plants
Screening
Throughput
Triage
2017
95 Citations (Scopus)
160 Downloads (Pure)
Open Access
File
Drug Discovery
Public Health
Neglected Diseases
Disease Eradication
African Trypanosomiasis
6 Citations (Scopus)
108 Downloads (Pure)

Does DNA replication direct locus-specific recombination during host immune evasion by antigenic variation in the African trypanosome?

Devlin, R., Marques, C. A. & McCulloch, R., Jun 2017, In : Current Genetics. 63, 3, p. 441-449 9 p.

Research output: Contribution to journalReview article

Open Access
File
Immune Evasion
Antigenic Variation
Trypanosomiasis
Membrane Glycoproteins
Gene Conversion
36 Citations (Scopus)
88 Downloads (Pure)

Endogenously produced nonclassical vitamin D hydroxy-metabolites act as "biased" agonists on VDR and inverse agonists on RORα and RORγ

Slominski, A. T., Kim, T-K., Hobrath, J. V., Oak, A. S. W., Tang, E. K. Y., Tieu, E. W., Li, W., Tuckey, R. C. & Jetten, A. M., Oct 2017, In : Journal of Steroid Biochemistry and Molecular Biology. 173, p. 42-56 15 p.

Research output: Contribution to journalReview article

Open Access
File
Metabolites
Vitamin D
Secosteroids
Molecular modeling
Ligands
13 Citations (Scopus)
197 Downloads (Pure)

Fragment library design, synthesis and expansion: nurturing a synthesis and training platform

Ray, P. C., Kiczun, M., Huggett, M., Lim, A., Prati, F., Gilbert, I. H. & Wyatt, P. G., Jan 2017, In : Drug Discovery Today. 22, 1, p. 43-56 14 p.

Research output: Contribution to journalReview article

Open Access
File
Libraries
Drug Discovery
Space Flight
Pharmaceutical Preparations
Costs and Cost Analysis
2 Citations (Scopus)

Management of plantar keratodermas: Lessons from pachyonychia congenita

Porter, R. M., Bravo, A. A. & Smith, F. J. D., Sep 2017, In : Journal of the American Podiatric Medical Association. 107, 5, p. 428-435 8 p.

Research output: Contribution to journalReview article

Pachyonychia Congenita
Bony Callus
Nails
Keratolytic Agents
Exfoliative Dermatitis
27 Citations (Scopus)
112 Downloads (Pure)
Open Access
File
Molecular recognition
Drug Design
Proteins
Cell signaling
Adhesives
6 Citations (Scopus)
84 Downloads (Pure)

Nuclear DNA Replication in Trypanosomatids: There Are No Easy Methods for Solving Difficult Problems

da Silva, M. S., Pavani, R. S., Damasceno, J. D., Marques, C. A., McCulloch, R., Tosi, L. R. O. & Elias, M. C., Nov 2017, In : Trends in Parasitology. 33, 11, p. 858-874 17 p.

Research output: Contribution to journalReview article

Open Access
File
DNA Replication
Eukaryota
Parasites
Origin Recognition Complex
Disease Eradication
27 Citations (Scopus)
279 Downloads (Pure)

Recognition of substrate degrons by E3 ubiquitin ligases and modulation by small-molecule mimicry strategies

Lucas, X. & Ciulli, A., Jun 2017, In : Current Opinion in Structural Biology. 44, p. 101-110 10 p.

Research output: Contribution to journalReview article

Open Access
File
Ubiquitin-Protein Ligases
Proteasome Endopeptidase Complex
Proteolysis
Proteins
Ubiquitination
30 Citations (Scopus)

The Evolution of Organellar Coat Complexes and Organization of the Eukaryotic Cell

Rout, M. P. & Field, M. C., Jun 2017, In : Annual Review of Biochemistry. 86, p. 637-657 21 p.

Research output: Contribution to journalReview article

Eukaryotic Cells
Organelles
Biochemistry
Proteins
Monomeric GTP-Binding Proteins
2016
11 Citations (Scopus)
94 Downloads (Pure)

Chemical genetics approaches for selective intervention in epigenetics

Runcie, A. C., Chan, K. H., Zengerle, M. & Ciulli, A., Aug 2016, In : Current Opinion in Chemical Biology. 33, p. 186-194 9 p.

Research output: Contribution to journalReview article

Open Access
File
Epigenomics
Genetics
Genes
Modulation
Molecules
38 Citations (Scopus)
107 Downloads (Pure)

Drug Resistance in Eukaryotic Microorganisms

Fairlamb, A. H., Gow, N. A. R., Matthews, K. R. & P. Waters, A., Jul 2016, In : Nature Microbiology. 1, p. 1-14 14 p., 16092.

Research output: Contribution to journalReview article

Open Access
File
Drug Resistance
Drug Therapy
Therapeutics
Microbial Drug Resistance
Technology
18 Citations (Scopus)
68 Downloads (Pure)

Epigenetic Regulation of Virulence Gene Expression in Parasitic Protozoa

Duraisingh, M. T. & Horn, D., 11 May 2016, In : Cell Host & Microbe. 19, 5, p. 629-640 12 p.

Research output: Contribution to journalReview article

Open Access
File
Gene Expression Regulation
Epigenomics
Virulence
Parasites
Genetic Epigenesis
25 Citations (Scopus)
116 Downloads (Pure)

Filaggrin failure - from ichthyosis vulgaris to atopic eczema and beyond

McLean, W., 26 Sep 2016, In : British Journal of Dermatology. 175, 52, p. 4-7 4 p.

Research output: Contribution to journalReview article

Open Access
File
Ichthyosis Vulgaris
Atopic Dermatitis
Cornea
Polyproteins
Mutation
19 Citations (Scopus)
102 Downloads (Pure)

From Companion Diagnostics to Theranostics: A New Avenue for Alzheimer's Disease?

Bolognesi, M. L., Gandini, A., Prati, F. & Uliassi, E., 8 Sep 2016, In : Journal of Medicinal Chemistry. 59, 17, p. 7759-7770 12 p.

Research output: Contribution to journalReview article

Open Access
File
Alzheimer Disease
Industry
Research Personnel
Theranostic Nanomedicine
Therapeutics
12 Citations (Scopus)
66 Downloads (Pure)

The ELF Honest Data Broker: Informatics enabling public-private collaboration in a precompetitive arena

Paillard, G., Cochrane, P., Jones, P. S., Van Hoorn, W. P., Caracoti, A., Van Vlijmen, H. & Pannifer, A. D., 1 Jan 2016, In : Drug Discovery Today. 21, 1, p. 97-102 6 p.

Research output: Contribution to journalReview article

Open Access
File
Informatics
Workflow
Triage
Intellectual Property
Drug Industry
2015
19 Citations (Scopus)
46 Downloads (Pure)

Parasite Glycobiology: A Bittersweet Symphony

Rodrigues, J. A., Acosta-Serrano, A., Aebi, M., Ferguson, M. A. J., Routier, F. H., Schiller, I., Soares, S., Spencer, D., Titz, A., Wilson, I. B. H. & Izquierdo, L., 12 Nov 2015, In : PLoS Pathogens. 11, 11, e1005169.

Research output: Contribution to journalReview article

Open Access
File
2013
117 Citations (Scopus)

Drug resistance in African trypanosomiasis: the melarsoprol and pentamidine story

Baker, N., de Koning, H. P., Maeser, P. & Horn, D., Mar 2013, In : Trends in Parasitology. 29, 3, p. 110-118 9 p.

Research output: Contribution to journalReview article

27 Citations (Scopus)

Proteomic analysis of clathrin interactions in trypanosomes reveals dynamic evolution of endocytosis

Adung'a, V. O., Gadelha, C. & Field, M. C., Apr 2013, In : Traffic. 14, 4, p. 440-457 18 p.

Research output: Contribution to journalReview article

20 Citations (Scopus)

Receptor-mediated endocytosis for drug delivery in African trypanosomes: Fulfilling Paul Ehrlich's vision of chemotherapy

Alsford, S., Field, M. C. & Horn, D., May 2013, In : Trends in Parasitology. 29, 5, p. 207-212 6 p.

Research output: Contribution to journalReview article

Trypanosomiasis
Membrane Glycoproteins
Endocytosis
Suramin
Drug Therapy
2012
19 Citations (Scopus)

Epigenetic mechanisms, nuclear architecture and the control of gene expression in trypanosomes

Alsford, S., duBois, K., Horn, D. & Field, M. C., 29 May 2012, In : Expert reviews in molecular medicine. 14, 20 p., ARTN e13.

Research output: Contribution to journalReview article

2011
45 Citations (Scopus)

Emerging role of surface plasmon resonance in fragment-based drug discovery

Navratilova, I. & Hopkins, A. L., Oct 2011, In : Future Medicinal Chemistry. 3, 14, p. 1809-1820 12 p.

Research output: Contribution to journalReview article

27 Citations (Scopus)

Finding New Hits in Neglected Disease Projects: Target or Phenotypic Based Screening?

Gilbert, I. H., Leroy, D. & Frearson, J. A., May 2011, In : Current Topics in Medicinal Chemistry. 11, 10, p. 1284-1291 8 p.

Research output: Contribution to journalReview article

15 Citations (Scopus)
23 Citations (Scopus)

Methylglyoxal metabolism in trypanosomes and leishmania

Wyllie, S. & Fairlamb, A. H., May 2011, In : Seminars in Cell & Developmental Biology. 22, 3, p. 271-277 7 p.

Research output: Contribution to journalReview article

62 Citations (Scopus)

Minimum information about a bioactive entity (MIABE)

Orchard, S., Al-Lazikani, B., Bryant, S., Clark, D., Calder, E., Dix, I., Engkvist, O., Forster, M., Gaulton, A., Gilson, M., Glen, R., Grigorov, M., Hammond-Kosack, K., Harland, L., Hopkins, A., Larminie, C., Lynch, N., Mann, R. K., Murray-Rust, P., Lo Piparo, E. & 6 others, Southan, C., Steinbeck, C., Wishart, D., Hermjakob, H., Overington, J. & Thornton, J., Sep 2011, In : Nature Reviews Drug Discovery. 10, 9, p. 661-669 9 p.

Research output: Contribution to journalReview article

14 Citations (Scopus)

Rapid Analysis of Pharmacology for Infectious Diseases

Hopkins, A. L., Bickerton, G. R., Carruthers, I. M., Boyer, S. K., Rubin, H. & Overington, J. P., May 2011, In : Current Topics in Medicinal Chemistry. 11, 10, p. 1292-1300 9 p.

Research output: Contribution to journalReview article

26 Citations (Scopus)

Synthetic glycosylphosphatidylinositol (GPI) anchors: how these complex molecules have been made

Nikolaev, A. V. & Al-Maharik, N., 2011, In : Natural Product Reports. 28, 5, p. 970-1020 51 p.

Research output: Contribution to journalReview article

6 Citations (Scopus)

Synthetic Neoglycoconjugates of Cell-Surface Phosphoglycans of Leishmania as Potential Anti-parasite Carbohydrate Vaccines

Nikolaev, A. V. & Sizova, O. V., Jul 2011, In : Biochemistry-Moscow. 76, 7, p. 761-773 13 p.

Research output: Contribution to journalReview article

54 Citations (Scopus)
32 Citations (Scopus)

The capture of phosphoproteins by 14-3-3 proteins mediates actions of insulin

Chen, S., Synowsky, S., Tinti, M. & MacKintosh, C., Nov 2011, In : Trends in Endocrinology and Metabolism. 22, 11, p. 429-436 8 p.

Research output: Contribution to journalReview article

30 Citations (Scopus)
97 Downloads (Pure)

Virtual screening strategies in drug design – methods and applications

Bielska, E., Lucas, X., Czerwoniec, A., Kasprzak, J. M., Kaminska, K. H. & Bujnicki, J. M., 2011, In : BioTechnologia. 92, 3, p. 249-264 16 p.

Research output: Contribution to journalReview article

Open Access
File
Drug Design
Drug Discovery
Ligands
screening
drugs
2010
52 Citations (Scopus)

Assessing brain free fraction in early drug discovery

Read, K. D. & Braggio, S., Mar 2010, In : Expert Opinion on Drug Metabolism & Toxicology. 6, 3, p. 337-344 8 p.

Research output: Contribution to journalReview article

27 Citations (Scopus)

Drug discovery in academia: the third way?

Frearson, J. & Wyatt, P., Oct 2010, In : Expert Opinion on Drug Discovery. 5, 10, p. 909-919 11 p.

Research output: Contribution to journalReview article

88 Citations (Scopus)

Molecular mechanisms underlying the control of antigenic variation in African trypanosomes

Horn, D. & McCulloch, R., Dec 2010, In : Current Opinion in Microbiology. 13, 6, p. 700-705 6 p.

Research output: Contribution to journalReview article

8 Citations (Scopus)

The tetrahydrobiopterin pathway and pain

Naylor, A. M., Pojasek, K. R., Hopkins, A. L. & Blagg, J., Jan 2010, In : Current Opinion in Investigational Drugs. 11, 1, p. 19-30 12 p.

Research output: Contribution to journalReview article

49 Citations (Scopus)

Visualization of multiple alignments, phylogenies and gene family evolution

Procter, J. B., Thompson, J., Letunic, I., Creevey, C., Jossinet, F. & Barton, G. J., 1 Mar 2010, In : Nature Methods. 7, 3, p. S16-S25 10 p.

Research output: Contribution to journalReview article

2009
3 Citations (Scopus)

DNA breaks as triggers for antigenic variation in African trypanosomes

Alsford, S., Horn, D. & Glover, L., 2009, In : Genome Biology. 10, 6, 4 p., ARTN 223.

Research output: Contribution to journalReview article

39 Citations (Scopus)

Structure-based ligand design and the promise held for antiprotozoan drug discovery

Hunter, W. N., 1 May 2009, In : Journal of Biological Chemistry. 284, 18, p. 11749-11753 5 p.

Research output: Contribution to journalReview article

2008
328 Citations (Scopus)
160 Downloads (Pure)

Kinetoplastids: related protozoan pathogens, different diseases

Stuart, K., Brun, R., Croft, S., Fairlamb, A., Guertler, R. E., McKerrow, J., Reed, S. & Tarleton, R., 2008, In : Journal of Clinical Investigation. 118, 4, p. 1301-1310 10 p.

Research output: Contribution to journalReview article

Open Access
File