Prodomain processing controls BMP-10 bioactivity and targeting to fibrillin-1 in latent conformation
(2025) In FASEB Journal 39(3).- Abstract
Bone morphogenetic protein 10 (BMP-10) is crucial for endothelial cell signaling via activin receptor-like kinase 1 (ALK1), a pathway central to vascular homeostasis and angiogenesis. Dysregulated BMP-10 signaling contributes to cardiovascular diseases and cancer, highlighting the need to control ALK1-mediated endothelial responses to BMP-10 for therapeutic development. BMP-10 biosynthesis involves processing by proprotein convertases (PPCs) resulting in a non-covalently associated prodomain–growth factor (PD–GF) complex (CPLX), similar to other TGF-β superfamily ligands. However, the molecular requirements for BMP-10 bioactivity remain unclear. We investigated how PPC processing impacts BMP-10 structure, bioactivity, and its... (More)
Bone morphogenetic protein 10 (BMP-10) is crucial for endothelial cell signaling via activin receptor-like kinase 1 (ALK1), a pathway central to vascular homeostasis and angiogenesis. Dysregulated BMP-10 signaling contributes to cardiovascular diseases and cancer, highlighting the need to control ALK1-mediated endothelial responses to BMP-10 for therapeutic development. BMP-10 biosynthesis involves processing by proprotein convertases (PPCs) resulting in a non-covalently associated prodomain–growth factor (PD–GF) complex (CPLX), similar to other TGF-β superfamily ligands. However, the molecular requirements for BMP-10 bioactivity remain unclear. We investigated how PPC processing impacts BMP-10 structure, bioactivity, and its interaction with the extracellular matrix (ECM) protein fibrillin-1. Molecular dynamics simulations post-in silico cleavage of the BMP-10 dimer model as well as negative staining and transmission electron microscopy (TEM) revealed that PD processing increases BMP-10 flexibility converting it from a latent wide-angle conformation to a bioactive CPLX which can adopt a V-shape with tighter angle. Only processed BMP-10 demonstrated high potency in HUVEC and C2C12 cells and robust binding to immobilized BMP receptors. Circular dichroism and interaction studies revealed that the N-terminal region of the BMP-10 PD is rich in alpha-helical content, which is essential for efficient complexation with the BMP-10 GF. Binding studies and TEM analyses showed that only the processed BMP-10 CPLX interacts with the N-terminal region of fibrillin-1, causing a conformational change that renders it into a closed ring-shaped conformation. These findings suggest that PD processing induces specific folding events at the PD–GF interface, which is critical for BMP-10 bioactivity and its targeting to the ECM.
(Less)
- author
- organization
- publishing date
- 2025-02
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- bone morphogenetic protein, complex, conformational change, electron microscopy, furin, growth factor, molecular dynamics, molecular modeling, proprotein convertases (PPCs), single particle analysis
- in
- FASEB Journal
- volume
- 39
- issue
- 3
- article number
- e70373
- publisher
- Wiley
- external identifiers
-
- pmid:39921464
- scopus:85217412945
- ISSN
- 0892-6638
- DOI
- 10.1096/fj.202401694R
- language
- English
- LU publication?
- yes
- id
- 04bf4b0b-4c89-41d9-8190-506d4dd8ec24
- date added to LUP
- 2025-03-17 15:12:42
- date last changed
- 2025-07-08 01:18:44
@article{04bf4b0b-4c89-41d9-8190-506d4dd8ec24, abstract = {{<p>Bone morphogenetic protein 10 (BMP-10) is crucial for endothelial cell signaling via activin receptor-like kinase 1 (ALK1), a pathway central to vascular homeostasis and angiogenesis. Dysregulated BMP-10 signaling contributes to cardiovascular diseases and cancer, highlighting the need to control ALK1-mediated endothelial responses to BMP-10 for therapeutic development. BMP-10 biosynthesis involves processing by proprotein convertases (PPCs) resulting in a non-covalently associated prodomain–growth factor (PD–GF) complex (CPLX), similar to other TGF-β superfamily ligands. However, the molecular requirements for BMP-10 bioactivity remain unclear. We investigated how PPC processing impacts BMP-10 structure, bioactivity, and its interaction with the extracellular matrix (ECM) protein fibrillin-1. Molecular dynamics simulations post-in silico cleavage of the BMP-10 dimer model as well as negative staining and transmission electron microscopy (TEM) revealed that PD processing increases BMP-10 flexibility converting it from a latent wide-angle conformation to a bioactive CPLX which can adopt a V-shape with tighter angle. Only processed BMP-10 demonstrated high potency in HUVEC and C2C12 cells and robust binding to immobilized BMP receptors. Circular dichroism and interaction studies revealed that the N-terminal region of the BMP-10 PD is rich in alpha-helical content, which is essential for efficient complexation with the BMP-10 GF. Binding studies and TEM analyses showed that only the processed BMP-10 CPLX interacts with the N-terminal region of fibrillin-1, causing a conformational change that renders it into a closed ring-shaped conformation. These findings suggest that PD processing induces specific folding events at the PD–GF interface, which is critical for BMP-10 bioactivity and its targeting to the ECM.</p>}}, author = {{Spanou, Chara E.S. and Yang, Chengeng and Godwin, Alan R.F. and Morosky, Stefanie and Anbalagan, Arulselvi and Lütke, Steffen and Mörgelin, Matthias and Marcous, Fady and Aziz, Ubair and Wohl, Alexander P. and Jabeen, Ishrat and Koch, Manuel and Jowitt, Thomas A. and Roman, Beth L. and Tarakanova, Anna and Baldock, Clair and Sengle, Gerhard}}, issn = {{0892-6638}}, keywords = {{bone morphogenetic protein; complex; conformational change; electron microscopy; furin; growth factor; molecular dynamics; molecular modeling; proprotein convertases (PPCs); single particle analysis}}, language = {{eng}}, number = {{3}}, publisher = {{Wiley}}, series = {{FASEB Journal}}, title = {{Prodomain processing controls BMP-10 bioactivity and targeting to fibrillin-1 in latent conformation}}, url = {{http://dx.doi.org/10.1096/fj.202401694R}}, doi = {{10.1096/fj.202401694R}}, volume = {{39}}, year = {{2025}}, }