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Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.

Abstract:

There are currently no effective therapies for fibrodysplasia ossificans progressiva (FOP), a debilitating and progressive heterotopic ossification disease caused by activating mutations of ACVR1 encoding the BMP type I receptor kinase ALK2. Recently, a subset of these same mutations of ACVR1 have been identified in diffuse intrinsic pontine glioma (DIPG) tumors. Here we describe the structure-activity relationship for a series of novel ALK2 inhibitors based on the 2-aminopyridine compound K0...

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Publication status:
Published

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Publisher copy:
10.1021/jm501177w

Authors


Mohedas, AH More by this author
Sanvitale, CE More by this author
Canning, P More by this author
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Journal:
Journal of medicinal chemistry
Volume:
57
Issue:
19
Pages:
7900-7915
Publication date:
2014-10-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:f6d3956a-8f1b-41b4-9e3d-1d9efe0fc35f
Source identifiers:
479273
Local pid:
pubs:479273

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