- 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...
Expand abstract - Publication status:
- Published
- Publisher copy:
- 10.1021/jm501177w
-
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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
- Language:
- English
- Keywords:
- Copyright date:
- 2014
Journal article
Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
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