luspatercept 
GtoPdb Ligand ID: 10538
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Synonyms: ACE-536 | ACE536 | luspatercept-aamt | Reblozyl®
luspatercept is an approved drug (FDA (2019), EMA (2020))
Compound class:
Peptide
Comment: Luspatercept (ACE-536) is a fusion protein comprising human ACVR2B (activin receptor type 2B) extracellular domain (which is mutated to reduce activin binding), fused with human immunoglobulin G1 Fc fragment [2]. Luspatercept was initially proposed as a ligand trap for growth/differentiation factor-11 (GDF11; and other TGFβ family ligands). Mechanistically, it reduces Smad2/3 activation, and promotes maturation of late-stage erythroid precursors, independently of the erythropoietin (EPO) pathway. In contrast, erythropoietin stimulates proliferation of early-stage erythrocyte precursors.
Using Gdf11 knockout, Guerra et al. (2019) disputed GDF11 as an important molecular target of luspatercept and its proposed inhibitory effect on late erythropoiesis [1]. |
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Other Similar Sequences  |
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TargetsCD80; CD86 |
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TargetsThrombopoietin receptor |
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| resokine | |
| efgartigimod alfa |
TargetsFc fragment of IgG receptor and transporter |
| MK-7110 |
Targetssialic acid binding Ig like lectin 10 |
| inbakicept | |
| sotatercept |
Targetsnull |
| efzofitimod | |
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