Publications


Publications
The first wide-scale drug repurposing screen using the Prestwick Chemical Library (1200 bioactive molecules) against Neisseria gonorrhoeae identifies high in vitro activity of auranofin and many additional drugs

Journal of Pathology, Microbiology and Immunology

Foerster S, Gustafsson TN, Brochado AR, Desilvestro V, Typas A, Unemo M
Journal of Pathology, Microbiology and Immunology - vol. 128 242-250 (2020)

Treatment options for gonorrhoea are scarce. Drug repurposing of bioactive molecules approved for other conditions might therefore be of value. We developed a method for wide-scale, systematic drug repurposing screen to identify molecules with activity against Neisseria gonorrhoeae and screened the Prestwick Chemical Library (1200 FDA-approved drugs). As a proof-of-concept, we further examined one promising […]

Publications
Evaluation of a library of FDA-approved drugs for their ability to potentiate antibiotics against multidrug-resistant gram-negative pathogens

Antimicrobial Agents and Chemotherapy

Hind CK, Dowson CG, Sutton JM, Jackson T, Clifford M, Garner RC, Czaplewski L
Antimicrobial Agents and Chemotherapy - vol. 63 1-6 (2019)

The Prestwick library was screened for antibacterial activity or « antibiotic resistance breaker » (ARB) potential against four species of Gram-negative pathogens. Discounting known antibacterials, the screen identified very few ARB hits, which were strain/drug specific. These ARB hits included antimetabolites (zidovudine, floxuridine, didanosine, and gemcitabine), anthracyclines (daunorubicin, mitoxantrone, and epirubicin), and psychoactive drugs (gabapentin, fluspirilene, and […]

Publications
The 2019 Garrod Lecture: MDR efflux in Gram-negative bacteria – How understanding resistance led to a new tool for drug discovery

Journal of Antimicrobial Chemotherapy

Piddock LJ
Journal of Antimicrobial Chemotherapy - vol. 74 3128-3134 (2019)

The AcrAB-TolC MDR efflux system confers intrinsic MDR and overproduction confers clinically relevant resistance to some antibiotics active against Gram-negative bacteria. The system is made up of three components, namely AcrA, AcrB and TolC, otherwise known as the AcrAB-TolC tripartite system. Inactivation or deletion of a gene encoding one of the constituent proteins, or substitution […]

Publications
A Small Molecule Targeting Mutagenic Translesion

Cell

Wojtaszek JL, Chatterjee N, Najeeb J, Hong J, Walker GC, Zhou P
Cell - vol. 178 152-159.e11 (2019)

Publications
Utilisation of the Prestwick Chemical Library to identify drugs that inhibit the growth of mycobacteria

PLoS ONE

Kanvatirth P JR
PLoS ONE - vol. 14 1-40 (2019)

Publications
Chlorambucil targets BRCA 1/2‐deficient tumours and counteracts PARP inhibitor resistance

EMBO Molecular Medicine

Tacconi EM, Badie S, De Gregoriis G, Reisländer T, Lai X, Porru M, Folio C, Moore J, Kopp A, Baguña Torres J, Sneddon D, Green M, Dedic S, Lee JW, Batra AS, Rueda OM, Bruna A, Leonetti C, Caldas C, Cornelissen B, Brino L, Ryan A, Biroccio A, Tarsounas M
EMBO Molecular Medicine - vol. 11 1-16 (2019)

© 2019 The Authors. Published under the terms of the CC BY 4.0 license Due to compromised homologous recombination (HR) repair, BRCA1- and BRCA2-mutated tumours accumulate DNA damage and genomic rearrangements conducive of tumour progression. To identify drugs that target specifically BRCA2-deficient cells, we screened a chemical library containing compounds in clinical use. The top […]

Publications
Repurposing of ribavirin as an adjunct therapy against invasive Candida strains in an in vitro study

Antimicrobial Agents and Chemotherapy

Yousfi H, Cassagne C, Ranque S, Rolain JM, Bittar F
Antimicrobial Agents and Chemotherapy - vol. 63 1-8 (2019)

The use of antifungal agents in clinical settings is limited by the appearance of drug resistance and adverse side effects. There is, therefore, an urgent need to develop new drugs to strengthen the treatment of invasive fungal diseases. The aim of this study is to describe the potential repurposing of ribavirin as an adjunct therapy […]

Publications
Novel drug candidates for treating esophageal carcinoma: A study on differentially expressed genes, using connectivity mapping and molecular docking

International Journal of Oncology

Chen YT, Xie JY, Sun Q, Mo WJ
International Journal of Oncology - vol. 54 152-166 (2019)

Patients with esophageal carcinoma (ESCA) have a poor prognosis and high mortality rate. Although standard therapies have had effect, there is an urgent requirement to develop novel options, as increasing drug tolerance has been identifiedinclinicalpractice.Inthepresentstudy,differentially expressedgenes(DEGs)ofESCAwereidentifiedinTheCancer Genome Atlas and Genotype-Tissue Expression databases. Functional and protein-protein interaction (PPI) analyses were performed. The Connectivity Map (CMAP) was […]

Publications
Utilisation of the Prestwick Chemical Library to identify drugs that inhibit the growth of mycobacteria

PLoS ONE

Kanvatirth P, Jeeves RE, Bacon J, Besra GS, Alderwick LJ
PLoS ONE - vol. 14 (2019)

Tuberculosis (TB) is an infectious bacterial disease that kills approximately 1.3 million people every year. Despite global efforts to reduce both the incidence and mortality associated with TB, the emergence of drug resistant strains has slowed any progress made towards combating the spread of this deadly disease. The current TB drug regimen is inadequate, takes […]

Publications
Identification and characterization of menadione and benzethonium chloride as potential treatments of Pierce’s disease of grapevines

Phytopathology

Zhang S, Jain M, Fleites LA, Rayside PA, Gabriel DW
Phytopathology - vol. 109 233-239 (2019)

Xylella fastidiosa infects a wide range of plant hosts and causes Pierce’s disease (PD) of grapevines. The type 1 multidrug resistance (MDR) efflux system is essential for pathogenicity and survival of bacterial pathogens in planta. X. fastidiosa, with a single MDR system, is significantly more vulnerable to inhibition by small-molecule treatments than most bacterial pathogens […]