Discovery of uncompetitive inhibitors of SapM that compromise intracellular survival of Mycobacterium tuberculosis

Autor: Paulina Fernández-Soto, Joshua Casulli, Danilo Solano-Castro, Pablo Rodríguez-Fernández, Thomas A. Jowitt, Mark A. Travis, Jennifer S. Cavet, Lydia Tabernero

Publikováno v: Scientific Reports, Vol 11, Iss 1, Pp 1-11 (2021)

Abstract SapM is a secreted virulence factor from Mycobacterium tuberculosis critical for pathogen survival and persistence inside the host. Its full potential as a target for tuberculosis treatment has not yet been exploited because of the lack of p

Externí odkaz: https://doaj.org/article/5135dd571c544dfd9a33769cbc83fbac

Computational and structure-guided design of phosphoinositide substrate specificity into the tyrosine specific LMW-PTP enzyme.

Autor: Eyong Egbe, Colin W Levy, Lydia Tabernero

Publikováno v: PLoS ONE, Vol 15, Iss 6, p e0235133 (2020)

We have used a combination of computational and structure-based redesign of the low molecular weight protein tyrosine phosphatase, LMW-PTP, to create new activity towards phosphoinositide substrates for which the wild-type enzyme had little or no act

Externí odkaz: https://doaj.org/article/96c1e3c4d7184914af684d85e30ef290

VSpipe, an Integrated Resource for Virtual Screening and Hit Selection: Applications to Protein Tyrosine Phospahatase Inhibition

Autor: Sandra Álvarez-Carretero, Niki Pavlopoulou, James Adams, Jane Gilsenan, Lydia Tabernero

Publikováno v: Molecules, Vol 23, Iss 2, p 353 (2018)

The use of computational tools for virtual screening provides a cost-efficient approach to select starting points for drug development. We have developed VSpipe, a user-friendly semi-automated pipeline for structure-based virtual screening. VSpipe us

Externí odkaz: https://doaj.org/article/d5c03217a7f64082a76ea6a3b9476f17

A Founder Mutation in

Autor: Naomi Issler, Sara Afonso, Irith Weissman, Katrin Jordan, Alberto Cebrian-Serrano, Katrin Meindl, Eileen Dahlke, Konstantin Tziridis, Guanhua Yan, José M. Robles-López, Lydia Tabernero, Vaksha Patel, Anne Kesselheim, Enriko D. Klootwijk, Horia C. Stanescu, Simona Dumitriu, Daniela Iancu, Mehmet Tekman, Monika Mozere, Graciana Jaureguiberry, Priya Outtandy, Claire Russell, Anna-Lena Forst, Christina Sterner, Elena-Sofia Heinl, Helga Othmen, Ines Tegtmeier, Markus Reichold, Ina Maria Schiessl, Katharina Limm, Peter Oefner, Ralph Witzgall, Lifei Fu, Franziska Theilig, Achim Schilling, Efrat Shuster Biton, Limor Kalfon, Ayalla Fedida, Elite Arnon-Sheleg, Ofer Ben Izhak, Daniella Magen, Yair Anikster, Holger Schulze, Christine Ziegler, Martin Lowe, Benjamin Davies, Detlef Böckenhauer, Robert Kleta, Tzipora C. Falik Zaccai, Richard Warth

Publikováno v: J Am Soc Nephrol
Issler, N, Afonso, S, Weissman, I, Jordan, K, Cebrian-Serrano, A, Meindl, K, Dahlke, E, Tziridis, K, Yan, G, Robles-López, J M, Tabernero, L, Patel, V, Kesselheim, A, Klootwijk, E D, Stanescu, H C, Dumitriu, S, Iancu, D, Tekman, M, Mozere, M, Jaureguiberry, G, Outtandy, P, Russell, C, Forst, A-L, Sterner, C, Heinl, E-S, Othmen, H, Tegtmeier, I, Reichold, M, Schiessl, I M, Limm, K, Oefner, P, Witzgall, R, Fu, L, Theilig, F, Schilling, A, Shuster Biton, E, Kalfon, L, Fedida, A, Arnon-Sheleg, E, Ben Izhak, O, Magen, D, Anikster, Y, Schulze, H, Ziegler, C, Lowe, M, Davies, B, Böckenhauer, D, Kleta, R, Falik Zaccai, T C & Warth, R 2022, ' A Founder Mutation in EHD1 Presents with Tubular Proteinuria and Deafness ', Journal of the American Society of Nephrology : JASN, vol. 33, no. 4, pp. 732-745 . https://doi.org/10.1681/ASN.2021101312

BACKGROUND: The endocytic reabsorption of proteins in the proximal tubule requires a complex machinery and defects can lead to tubular proteinuria. The precise mechanisms of endocytosis and processing of receptors and cargo are incompletely understoo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8d86b9e766f0d768e9b5bfddd01c006
https://pubmed.ncbi.nlm.nih.gov/35256404

Targeting Methionine Synthase in a Fungal Pathogen Causes a Metabolic Imbalance That Impacts Cell Energetics, Growth, and Virulence

Autor: Darren D. Thomson, Sean Doyle, Riba Thomas, Jorge Amich, Elaine Bignell, Benjamin P. Thornton, Monica Sueiro-Olivares, Rachael Fortune-Grant, Rebecca A. Owens, Howbeer Muhamadali, Lydia Tabernero, Katherine A. Hollywood, Royston Goodacre, Jennifer Scott

Publikováno v: mBio
Scott, J, Sueiro Olivares, M, Thornton, B, Owens, R A, Muhamadali, H, Fortune-Grant, R, Thomson, D, Thomas, R, Hollywood, K, Doyle, S, Goodacre, R, Tabernero, L, Bignell, E & Amich Elias, J 2020, ' Targeting methionine synthase in a fungal pathogen causes a metabolic imbalance that impacts cell energetics, growth and virulence ', mBio, vol. 11, no. 5, e01985-20, pp. 1-23 . https://doi.org/10.1128/mBio.01985-20
mBio, Vol 11, Iss 5 (2020)

Fungal pathogens are responsible for millions of life-threatening infections on an annual basis worldwide. The current repertoire of antifungal drugs is very limited and, worryingly, resistance has emerged and already become a serious threat to our c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed2ea1a6d5ad7b555668bceb623c0bc1
https://pubmed.ncbi.nlm.nih.gov/33051366