Browsing by author "Al-Lazikani, Bissan"
Now showing items 21-33 of 33
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Objective, Quantitative, Data-Driven Assessment of Chemical Probes.
Antolin, AA; Tym, JE; Komianou, A; Collins, I; Workman, P; et al. (CELL PRESS, 2018-02-15)Chemical probes are essential tools for understanding biological systems and for target validation, yet selecting probes for biomedical research is rarely based on objective assessment of all potential compounds. Here, we ... -
PDBe-KB: a community-driven resource for structural and functional annotations.
PDBe-KB consortium, (OXFORD UNIV PRESS, 2020-01-08)The Protein Data Bank in Europe-Knowledge Base (PDBe-KB, https://pdbe-kb.org) is a community-driven, collaborative resource for literature-derived, manually curated and computationally predicted structural and functional ... -
Polypharmacology in Precision Oncology: Current Applications and Future Prospects.
Antolin, AA; Workman, P; Mestres, J; Al-Lazikani, B (BENTHAM SCIENCE PUBL LTD, 2017-01-24)Over the past decade, a more comprehensive, large-scale approach to studying cancer genetics and biology has revealed the challenges of tumor heterogeneity, adaption, evolution and drug resistance, while systems-based ... -
Public resources for chemical probes: the journey so far and the road ahead.
Antolin, AA; Workman, P; Al-Lazikani, B (Future Science Ltd, 2019-11-28)High-quality small molecule chemical probes are extremely valuable for biological research and target validation. However, frequent use of flawed small-molecule inhibitors produces misleading results and diminishes the ... -
Rational design of non-resistant targeted cancer therapies.
Martínez-Jiménez, F; Overington, JP; Al-Lazikani, B; Marti-Renom, MA (NATURE PORTFOLIO, 2017-04-24)Drug resistance is one of the major problems in targeted cancer therapy. A major cause of resistance is changes in the amino acids that form the drug-target binding site. Despite of the numerous efforts made to individually ... -
Sequencing of prostate cancers identifies new cancer genes, routes of progression and drug targets.
Wedge, DC; Gundem, G; Mitchell, T; Woodcock, DJ; Martincorena, I; et al. (NATURE PUBLISHING GROUP, 2018-05-01)Prostate cancer represents a substantial clinical challenge because it is difficult to predict outcome and advanced disease is often fatal. We sequenced the whole genomes of 112 primary and metastatic prostate cancer ... -
Signalling involving MET and FAK supports cell division independent of the activity of the cell cycle-regulating CDK4/6 kinases.
Zhang, C; Stockwell, SR; Elbanna, M; Ketteler, R; Freeman, J; et al. (NATURE PUBLISHING GROUP, 2019-07-25)Deregulation of cyclin-dependent kinases 4 and 6 (CDK4/6) is highly prevalent in cancer; yet, inhibitors against these kinases are currently used only in restricted tumour contexts. The extent to which cancers depend on ... -
SiGNet: A signaling network data simulator to enable signaling network inference.
Coker, EA; Mitsopoulos, C; Workman, P; Al-Lazikani, B (PUBLIC LIBRARY SCIENCE, 2017-05-17)Network models are widely used to describe complex signaling systems. Cellular wiring varies in different cellular contexts and numerous inference techniques have been developed to infer the structure of a network from ... -
Solution structure of the Hop TPR2A domain and investigation of target druggability by NMR, biochemical and in silico approaches.
Darby, JF; Vidler, LR; Simpson, PJ; Al-Lazikani, B; Matthews, SJ; et al. (NATURE RESEARCH, 2020-09-29)Heat shock protein 90 (Hsp90) is a molecular chaperone that plays an important role in tumour biology by promoting the stabilisation and activity of oncogenic 'client' proteins. Inhibition of Hsp90 by small-molecule drugs, ... -
Target 2035 - update on the quest for a probe for every protein.
Müller, S; Ackloo, S; Al Chawaf, A; Al-Lazikani, B; Antolin, A; et al. (ROYAL SOC CHEMISTRY, 2022-01-27)Twenty years after the publication of the first draft of the human genome, our knowledge of the human proteome is still fragmented. The challenge of translating the wealth of new knowledge from genomics into new medicines ... -
The Chemical Probes Portal: an expert review-based public resource to empower chemical probe assessment, selection and use.
Antolin, AA; Sanfelice, D; Crisp, A; Villasclaras Fernandez, E; Mica, IL; et al. (OXFORD UNIV PRESS, 2023-01-06)We describe the Chemical Probes Portal (https://www.chemicalprobes.org/), an expert review-based public resource to empower chemical probe assessment, selection and use. Chemical probes are high-quality small-molecule ... -
The kinase polypharmacology landscape of clinical PARP inhibitors.
Antolin, AA; Ameratunga, M; Banerji, U; Clarke, PA; Workman, P; et al. (NATURE PUBLISHING GROUP, 2020-02-17)Polypharmacology plays an important role in defining response and adverse effects of drugs. For some mechanisms, experimentally mapping polypharmacology is commonplace, although this is typically done within the same protein ... -
Tuning Local Hydration Enables a Deeper Understanding of Protein-Ligand Binding: The PP1-Src Kinase Case.
Spitaleri, A; Zia, SR; Di Micco, P; Al-Lazikani, B; Soler, MA; et al. (AMER CHEMICAL SOC, 2021-01-14)Water plays a key role in biomolecular recognition and binding. Despite the development of several computational and experimental approaches, it is still challenging to comprehensively characterize water-mediated effects ...