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Journal article

Structural basis for the potent and selective binding of LDN-212854 to the BMP receptor kinase ALK2

Abstract:

Individuals with the rare developmental disorder fibrodysplasia ossificans progressiva (FOP) experience disabling heterotopic ossification caused by a gain of function mutation in the intracellular region of the BMP type I receptor kinase ALK2, encoded by the gene ACVR1. Small molecule BMP type I receptor inhibitors that block this ossification in FOP mouse models have been derived from the pyrazolo[1,5-a]pyrimidine scaffold of dorsomorphin. While the first derivative LDN-193189 exhibited pan...

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Publication status:
Published
Peer review status:
Peer reviewed
Version:
Publisher's version

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Publisher copy:
10.1016/j.bone.2017.09.004

Authors


More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM; Structural Genomics Consortium
Role:
Author
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
NDM; Structural Genomics Consortium
Role:
Author
Publisher:
Elsevier Publisher's website
Journal:
Bone Journal website
Volume:
109
Pages:
251-258
Publication date:
2017-09-12
Acceptance date:
2017-09-11
DOI:
EISSN:
1873-2763
ISSN:
8756-3282
Pubs id:
pubs:730169
URN:
uri:0a77cc92-4c73-45e9-a2bf-68f21ff8285b
UUID:
uuid:0a77cc92-4c73-45e9-a2bf-68f21ff8285b
Local pid:
pubs:730169

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