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Structure of the Bone Morphogenetic Protein Receptor ALK2 and Implications for Fibrodysplasia Ossificans Progressiva*
Background: Mutations in the ALK2 kinase cause extraskeletal bone formation. Results: We solved the structure of ALK2 in complex with the inhibitor FKBP12. Conclusion: Disease mutations breakExpand
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A New Class of Small Molecule Inhibitor of BMP Signaling
Growth factor signaling pathways are tightly regulated by phosphorylation and include many important kinase targets of interest for drug discovery. Small molecule inhibitors of the bone morphogeneticExpand
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CIS is a potent checkpoint in NK cell–mediated tumor immunity
The detection of aberrant cells by natural killer (NK) cells is controlled by the integration of signals from activating and inhibitory ligands and from cytokines such as IL-15. We identifiedExpand
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Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases
Members of the potassium channel tetramerization domain (KCTD) family are soluble non-channel proteins that commonly function as Cullin3 (Cul3)-dependent E3 ligases. Solution studies of theExpand
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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
There are currently no effective therapies for fibrodysplasia ossificans progressiva (FOP), a debilitating and progressive heterotopic ossification disease caused by activating mutations of ACVR1Expand
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Crystal structure of the ACVRL1 (ALK1) kinase domain bound to LDN-193189
PDB ID : 3MY0 Title : Crystal structure of the ACVRL1 (ALK1) kinase domain bound to LDN193189 Authors : Chaikuad, A.; Alfano, I.; Cooper, C.; Mahajan, P.; Daga, N.; Sanvitale, C.; Fedorov, O.;Expand
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Crystal structure of human BJ-TSA-9
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Crystal structure of the ACVR1 kinase in complex with a 2-aminopyridine inhibitor
PDB ID : 3MTF Title : Crystal structure of the ACVR1 kinase in complex with a 2-aminopyridine inhibitor Authors : Chaikuad, A.; Sanvitale, C.; Cooper, C.; Mahajan, P.; Daga, N.; Petrie, K.; Alfano,Expand
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