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Open Targets Platform 23.12 has been released!

The Open Targets Blog

Target prioritisation A major new feature of this release is the Target Prioritisation view, which provides an assessment of target-specific properties of interest when evaluating the suitability of a target for a drug discovery programme. It is presented here with an additional layer of analysis with a drug discovery focus.

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Preclinical systemic pharmacokinetics, dose-proportionality, and CNS distribution of the ATM inhibitor WSD0628, a novel radiosensitizer for the treatment of brain tumors [Metabolism, Transport, and Pharmacogenetics]

ASPET

Radiation therapy, a standard treatment option for many cancer patients, induces DNA double strand breaks (DSBs), leading to cell death. Efficacy of radiosensitizers for brain tumors may be influenced by a lack of effective drug delivery across the blood-brain barrier (BBB).

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A personal touch: the role of bioprinting in drug discovery

Drug Discovery World

DDW Editor, Reece Armstrong, sits down with Brinter CEO Tomi Kalpio to learn about the company’s approach to bioprinting and how it can be used throughout drug discovery. . RA: How can bioprinting be used to shorten drug discovery timelines? . This allows researchers to identify the best individual drugs to treat the disease. .

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Pharmacokinetics of panobinostat: Inter-species difference in metabolic stability [Metabolism, Transport, and Pharmacogenetics]

ASPET

Panobinostat is a potent pan-HDAC inhibitor that has been tested in multiple studies for the treatment of brain tumors. There have been contrasting views surrounding its efficacy for the treatment of tumors in the CNS following systemic administration when examined in different models or species.

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The use-case for NGS

Drug Discovery World

DDW Editor Reece Armstrong speaks to Dr Darrell Green , Lecturer in RNA Biology Biomedical Research Centre Norwich Medical School University of East Anglia, about his work using next generation sequencing (NGS) and the areas the technology is impacting within drug discovery and development. DG : For sure!

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Humanization of SLCO2B1 in rats increases rCYP3A1 protein expression but not the metabolism of erlotinib to OSI-420 [Metabolism, Transport, and Pharmacogenetics]

ASPET

A first pharmacological phenotyping with the OATP2B1 substrate-drug atorvastatin revealed reduced hepatic content and increased expression of rCYP3A1 in the humanized animals. The contrary was observed, when microsomes isolated from treatment naive animals were assessed for the OSI-420 formation after erlotinib exposure.