| ECM-Derived Peptides |
| PepGen P-15 (P-15) [385−388] |
15 |
Type I collagen binding sites |
Upregulated: ALP, BMP-2, BMP-7; Runx2,
COL1, OSTRX BSP, and integrin a2 |
Promoted: extracellular matrix production; proliferation and osteogenic differentiation;
cell attachment, migration, and survival |
| Arginine-glycine-aspartic
acid (RGD) [389−392] |
3 |
Integrin binding
sites |
Upregulated: ALP, RUNX2, osteocalcin, osteopontin,
BSP, Sox9, Aggrecan, fibronectin,
and collagen II |
Promoted: Proliferation,
mineralization, and osteogenic differentiation; cell
attachment and survival |
| Ser-Val-Val-Tyr-Gly-Leu-Arg (SVVYGLR) [393−395] |
7 |
RGD binding sites |
Upregulated: integrin avb3 |
Promoted: proliferation and neovascularization; angiogenesis
and osteogenesis;
adhesion, migration; tube formation of endothelial cells |
| |
|
|
Suppressed: NFAT, osteoclastogenesis-related mRNAs |
|
| Glycine-phenylalanine-hydroxyproline-arginine
(GFOGER) [396−399] |
4 |
integrin a2b1
binding sites |
Upregulated: integrin a2b1 binding |
Promoted: differentiation, bone regeneration, and osseointegration |
| Collagen binding motif
(CBM) [400, 401] |
28 |
Collagen binding
sites |
Induced sustained
activation
of ERK; induced transactivation of SRE, CRE, and AP-1; induced expression of type X collagen |
Promoted: bone-related cell adhesion and growth; osteogenic differentiation |
| Fibronectin-derived
peptides
(FN-derived peptides) [402−404] |
7 |
– |
– |
Promoted: bone-related cell spreading; adhesion and mineralization |
| BMP-Derived Peptides |
| P17-BMP-2 [405] |
17 |
– |
– |
Promoted: bone repair; osteoblast differentiation and bone regeneration |
| P20-BMP-2 and P24-BMP-2 [406] |
20 and 24, respectively |
– |
Upregulated: OCN, Runx2, and collagen I |
Promoted: osteogenesis
and differentiation of MSCs into osteoblasts |
| BMP-7-derived peptide BFP-1 [407] |
15 |
– |
Upregulated: expression of CD44, CD47 and CD51 |
Enhanced: Ca2p content in cells; ALP activity; bone regeneration |
| Other Peptides |
| Calcitonin gene-related
peptides (CGRPs) [61, 408−410] |
37 |
Pathways: cAMP, Wnt, and AMPK-eNOS |
Upregulated: expression
of IGF-1, IGF-1 receptor and BMP-2 receptor; ALP,
OC, and COLLA1 |
Promoted: cell proliferation, osteogenic differentiation,
and angiogenesis |
| |
|
|
|
Downregulated: apoptosis
and inflammation |
| Parathyroid hormone (1-34) (PTH 1-34) [411, 412] |
34 |
Pathways: G(q)-signaling, b-arrestin recruitment, ERK 1/2 phosphorylation
and phospholipase C |
Upregulated: expression of Runx2 and COL2A1 |
Promoted: cell proliferation
and chondrogenesis |
| |
|
|
Downregulated: expression of ALP and BMP-2 |
|
| Osteogenic growth peptides
(OGPs) [413−415] |
14 |
Pathways: G1 protein-MAPK and RhoA/ROCK |
Upregulated: osteocalcin, collagen, BMP-2, ALP
and mineralization TGF b1, TGF b2, TGF b3, FGF-2, IGF-I |
Promoted: cell proliferation and osteogenic differentiation; cartilage-to-bone
transition |
| |
|
|
|
Downregulated: adipogenic differentiation |
| Thrombin peptide
508 (TP508) [389, 416] |
23 |
Pathways: JAK/STAT, NF-κB, PDGF, PI3K/AKT, PTEN, and ERK/MAPK; cell cycle-G1/S checkpoint |
Upregulated: expression of Runx2 and OPN |
Promoted: cell proliferation
and osteogenic differentiation; chemotaxis, angiogenesis
and revascularization |
| |
|
|
|
Downregulated: apoptosis,
the effect of hypoxia |
| NEMO-binding domain peptide
(NBD) [417, 418] |
6 |
Pathway: NF-κB |
Downregulated: TRAP activity, actin rings; RANKL-induced c-Src kinase activity |
Promoted: osteogenic
differentiation of cells |
| |
|
|
|
Downregulated: bone
resorption |
| Cell-penetrating peptide
(CPP) [419, 420] |
30 |
– |
– |
Transcription factor delivery
of bone regeneration-related proteins or factors into cells |
| AcN-RADARADARAD-ARADA-CONH2 (RADA16-I 16) [421] |
16 |
– |
Upregulated: expression
of Runx2 genes, ALP, and osteocalcin |
Transcription factor delivery
of bone-regeneration-related proteins or factors into cells |
