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Article

Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.

Journal of medicinal chemistry - 14 May 2020

Ensan Deeba, Smil David, Zepeda-Velázquez Carlos A, Panagopoulos Dimitrios, Wong Jong Fu, Williams Eleanor P, Adamson Roslin, Bullock Alex N, Kiyota Taira, Aman Ahmed, Roberts Owen G, Edwards Aled M, O'Meara Jeff A, Isaac Methvin B, Al-Awar Rima

Abstract excerpt

Diffuse intrinsic pontine glioma is an aggressive pediatric cancer for which no effective chemotherapeutic drugs exist. Analysis of the genomic landscape of this disease has led to the identification of the serine/threonine kinase ALK2 as a potential target for therapeutic intervention. In this work, we adopted an open science approach to develop a series of potent type I inhibitors of ALK2 which are orally...

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Identifiers

PMID: 32369358
DOI: 10.1021/acs.jmedchem.0c00395
PMCID: PMC8213057

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