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Open Targets: a platform for therapeutic target identification and validation

Gautier Koscielny, Peter An, Denise Carvalho-Silva, Jennifer A. Cham, Luca Fumis, Rippa Gasparyan, Samiul Hasan, Nikiforos Karamanis, Michael Maguire, Eliseo Papa, Andrea Pierleoni, Miguel Pignatelli (+44 others)
2016 Nucleic Acids Research  
We have designed and developed a data integration and visualization platform that provides evidence about the association of known and potential drug targets with diseases.  ...  ACKNOWLEDGEMENTS We thank Guilherme Viteri, Florian Korninger, Elisabet Barrera Casanova, Laura Huerta Martinez, Anja Fullgrabe and Nuno Fonseca for additional contributions to the data sources used here  ...  Overall, Open Targets is committed to a program of work that we believe will have a transformational effect on the science of therapeutic target validation including generating new experimental data.  ... 
doi:10.1093/nar/gkw1055 pmid:27899665 pmcid:PMC5210543 fatcat:f6a6uglkuvdh3k26jmu4wf6kxi

Open Targets Platform: supporting systematic drug–target identification and prioritisation

David Ochoa, Andrew Hercules, Miguel Carmona, Daniel Suveges, Asier Gonzalez-Uriarte, Cinzia Malangone, Alfredo Miranda, Luca Fumis, Denise Carvalho-Silva, Michaela Spitzer, Jarrod Baker, Javier Ferrer (+20 others)
2020 Nucleic Acids Research  
The Open Targets Platform (https://www.targetvalidation.org/) provides users with a queryable knowledgebase and user interface to aid systematic target identification and prioritisation for drug discovery  ...  To aid the prioritisation of targets and inform on the potential impact of modulating a given target, we have added evaluation of post-marketing adverse drug reactions and new curated information on target  ...  The Open Targets Platform, therefore, aims to provide a comprehensive characterisation of targets, diseases or phenotypes and, more recently, known drugs that can help inform target identification and  ... 
doi:10.1093/nar/gkaa1027 pmid:33196847 fatcat:3qrm5q5turgulbvyj2kj6oy5c4

Targeted Strategies for Henipavirus Therapeutics

Katharine N. Bossart, John Bingham, Deborah Middleton
2007 Open Virology Journal  
In recent years henipavirus research has revealed a more complete understanding of pathogenesis and, as a consequence, viable approaches towards vaccines and therapeutics have emerged.  ...  Animal models have been developed, some of which may prove more valuable than others for evaluating the efficacy of therapeutic agents and regimes.  ...  This study was supported in part by a Geelong Research Award to KNB (AAHL DR59F), in part by a grant to KNB from the Jack Brockhoff Foundation (AAHL KW96B), and the AB-CRC grant 1.013RE.  ... 
doi:10.2174/187435790701011409 fatcat:yeevc2qagnhivf6hjctzv4danm

Targeted Strategies for Henipavirus Therapeutics

Katharine N. Bossart, John Bingham, Deborah Middleton
2007 Open Virology Journal  
In recent years henipavirus research has revealed a more complete understanding of pathogenesis and, as a consequence, viable approaches towards vaccines and therapeutics have emerged.  ...  Animal models have been developed, some of which may prove more valuable than others for evaluating the efficacy of therapeutic agents and regimes.  ...  This study was supported in part by a Geelong Research Award to KNB (AAHL DR59F), in part by a grant to KNB from the Jack Brockhoff Foundation (AAHL KW96B), and the AB-CRC grant 1.013RE.  ... 
doi:10.2174/1874357900701010014 pmid:19440455 pmcid:PMC2675550 fatcat:suahdzumsvadbijxox5b7ks2zq

Practical issues of biomarker-assisted targeted therapy in precision medicine and immuno-oncology era

Dae Ho Lee
2018 ESMO Open  
advent of new therapeutic agents and new diagnostic methods.  ...  This review will briefly touch on these issues, hoping to provide a better understanding and application of targeted therapy in cancer treatment in the era of precision medicine and immuno-oncology.  ...  standardisation, validation, and quality control and assurance. 15 16 redIsCovery of meanIngs of bIomarker To date, we usually try to identify a molecular target or oncogenic driver for matched targeted  ... 
doi:10.1136/esmoopen-2018-000370 pmid:29942670 pmcid:PMC6012567 fatcat:5s6h3r5vgzg7djnsflycapivaa

Molecular target: pan-AKT in gastric cancer

Byung Woog Kang, Ian Chau
2020 ESMO Open  
Accordingly, as an attractive therapeutic target for cancer treatment, several AKT inhibitors are currently under development and in multiple stages of clinical trials for various types of malignancy,  ...  AKT activation subsequently leads to a number of potential downstream effects, and its aberrant activation results in the pathogenesis of cancer.  ...  to the PI3K/AKT/mammalian target of rapamycin (mTOR) pathway inhibitors. 18 Therefore, cumulative evidence indicates a promising potential for targeting AKT for the effective treatment of GC.  ... 
doi:10.1136/esmoopen-2020-000728 pmid:32948630 pmcid:PMC7511610 fatcat:cme5wlzii5hqlh5xleblm7ayjy

Open Access Target Validation Is a More Efficient Way to Accelerate Drug Discovery

Wen Hwa Lee
2015 PLoS Biology  
Industry and academia are finally coming to terms with the fact that the prevalent models and incentives for innovation in early stage drug discovery are failing to promote progress quickly enough.  ...  There is a scarcity of novel treatments to address many unmet medical needs.  ...  , Toronto, Stockholm, and Campinas for their friendly support, and our network of collaborators for their unabated enthusiasm in supporting open access.  ... 
doi:10.1371/journal.pbio.1002164 pmid:26042736 pmcid:PMC4456377 fatcat:o2l3izxbavebxp5he4c3be3tja

New emerging targets in cancer immunotherapy: the role of neoantigens

Leticia De Mattos-Arruda, Juan Blanco-Heredia, Carmen Aguilar-Gurrieri, Jorge Carrillo, Julià Blanco
2020 ESMO Open  
In this mini review, we discuss the promises and challenges for using neoantigens as emergent targets to personalise and guide cancer immunotherapy in a broader set of cancers.  ...  Therapies that target immune checkpoint inhibitors have shown unprecedented rates of durable long-lasting responses in patients with various cancer types, but only in a fraction of patients.  ...  Here, we review an emerging tool for cancer immunotherapy, the so-called neoantigens and discuss their role as targets for cancer vaccines and adoptive T-cell therapies. neoantigens as targets for personalised  ... 
doi:10.1136/esmoopen-2020-000684 pmid:32269031 pmcid:PMC7326255 fatcat:fl3ay4nbrnfkpnahpk2my6sypy

Recent Trends in Collaborative, Open Source Drug Discovery

Anuradha Roy
2011 Open Conference Proceedings Journal  
The pharmaceutical sector has traditionally played a predominant role in screening compounds against a molecular target and optimizing chemistry to develop drugs.  ...  The pharmaacademia sectors are collaborating on several mutually beneficial alliances and the changing landscape at pharmaacademiainterface necessitates an urgent need for a better understanding of the  ...  ACKNOWLEDGEMENTS KU-HTSL is a KU Cancer Center Shared Resource, and is funded In part by NIH/NCRR, COBRE grant P20 RR015563.  ... 
doi:10.2174/2210289201102010130 fatcat:nkdgcnr2eracjcoaj7bkj5hqye

OCTAD: an open workplace for virtually screening therapeutics targeting precise cancer patient groups using gene expression features [article]

Billy Zeng, Benjamin S Glicksberg, Patrick Newbury, Jing Xing, Ke Liu, Anita Wen, Caven Chow, Bin Chen
2019 bioRxiv   pre-print
Therefore, we present OCTAD: an open workplace for virtually screening compounds targeting precise cancer patient groups using gene expression features.  ...  We release OCTAD as a web portal and standalone R workflow to allow experimental and computational scientists to easily navigate the tool.  ...  Acknowledgements The research is supported by R01GM134307, R21 TR001743 and K01 ES028047 and the MSU Global Impact Initiative.  ... 
doi:10.1101/821546 fatcat:feicwwe2evcileqbonea22zwai

New target prediction and visualization tools incorporating open source molecular fingerprints for TB Mobile 2.0

Alex M Clark, Malabika Sarker, Sean Ekins
2014 Journal of Cheminformatics  
We recently developed a freely available mobile app (TB Mobile) for both iOS and Android platforms that displays Mycobacterium tuberculosis (Mtb) active molecule structures and their targets with links  ...  We have curated an additional 60 new compounds and their targets for Mtb and added these to the original set of 745 compounds.  ...  Carolyn Talcott (SRI) for their comments on this work. S.E. also gratefully acknowledges Dr. Joel S. Freundlich and Dr. Peter Madrid for many discussions on TB targets and molecules.  ... 
doi:10.1186/s13321-014-0038-2 pmid:25302078 pmcid:PMC4190048 fatcat:kpsebi2sknelvb22t52fxeieta

Discovery of New Class of Trypanocidal Compounds Targeting the Energy Metabolism of African Trypanosomes

Emmanuel Oluwadare Balogun, Daniel Ken Inaoka, Tomoo Shiba, Yoh-Ichi Watanabe, Anthony Moore, Shigeharu Harada, Kiyoshi Kita
2017 Open Forum Infectious Diseases  
There is no vaccine and the available therapeutic options are few and with limited efficacy, prompting the search for new drug candidates.  ...  The complex structures of both enzymes with the inhibitors have been determined, providing a platform for further refinement of the trypanocidal potencies by structure-activity relationship studies.  ...  A retrospective chart review was performed in all patients with ICD-9 or ICD-10 diagnostic codes for Ehrlichiosis or Anaplasmosis between 2014 and 2016 at Southampton Hospital (a major community hospital  ... 
doi:10.1093/ofid/ofx163.154 fatcat:g3uaz7kocvbtlh45uqsspunipa

The role of open innovation in biomarker discovery

Lilla Landeck, Monika Lessl, Andreas Busch, Matthias Gottwald, Khusru Asadullah
2016 Advances in Precision Medicine  
In this article we de-scribe the first examples of open-innovation models, such as the 'grants for targets' (G4T) and biomarkers initiative 'InnoCentive' (innovation/incentive) platform.  ...  However, the identification and validation of appropriate BMs is challenging. Close col-laboration between different partners seems to be a key success factor.  ...  Acknowledgements The authors thank Stefanie Schoepe and Heidrun Dorsch (both from Berlin, Germany) for their valuable contributions in the G4T program and Johnny Grace (San Francisco Bay, USA) for critical  ... 
doi:10.18063/apm.2016.02.007. fatcat:pumwx6opsvffdpts7pe7r2ftmy

Autophagy protease ATG4B as a drug target in cancer

Robin Ketteler
2017 Biological Systems Open Access  
This enabled identification of positively selected events, and the first demonstration of negative selection of mutations that may be deleterious to tumor development indicating novel avenues for therapy  ...  driver mutations and yielding a high-resolution, genome wide map of the selective forces surrounding cancer gene loci.  ...  a resource to prioritize the study of human cancer drivers and potential therapeutic targets.  ... 
doi:10.4172/2329-6577-c1-008 fatcat:3iafcjw4g5d27omgjm2so2fq6y

The Application of the Open Pharmacological Concepts Triple Store (Open PHACTS) to Support Drug Discovery Research

Joseline Ratnam, Barbara Zdrazil, Daniela Digles, Emiliano Cuadrado-Rodriguez, Jean-Marc Neefs, Hannah Tipney, Ronald Siebes, Andra Waagmeester, Glyn Bradley, Chau Han Chau, Lars Richter, Jose Brea (+7 others)
2014 PLoS ONE  
Use cases presented herein cover 1) the comprehensive identification of chemical matter for a OPEN ACCESS dopamine receptor drug discovery program 2) the identification of compounds active against all  ...  targets in the Epidermal growth factor receptor (ErbB) signaling pathway that have a relevance to disease and 3) the evaluation of established targets in the Vitamin D metabolism pathway to aid novel Vitamin  ...  Acknowledgments The authors would like to acknowledge the contribution of the many Open PHACTS Consortium members for their various critical inputs to scientific discussions, manuscript preparation and  ... 
doi:10.1371/journal.pone.0115460 pmid:25522365 pmcid:PMC4270790 fatcat:blfev3l7bvcelfozho2y7cyrsa
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