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Compound class:
Endogenous peptide in human, mouse or rat
Comment: Histatin 1 is an endogenous cationic and histidine-rich secreted peptide. It binds to the σ2 receptor (TMEM97) on epithelial cells [8-9], and to the VEGFR2 (KDR) on endothelial cells [4]. Histatin 1 is the primary wound healing agent in saliva. It acts as a potent promoter of cell migration and angiogenesis [11], two important biological processes that contribute to the rapid rate of wound healing in the oral mucosa.
Preclinical evidence suggests that histatin 1, or more likely metabolically stablised derivatives, offer a novel therapeutic mechanism in non-oral tissues for wound healing properties [1-3,5-6,13], or for potential osteogenic activity [7,10,12,14].
Species: Human
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Arab A, Aghila Rani KG, Altell RT, Ismail AA, Alkawas S, Samsudin AR. (2022)
The efficacy of salivary Histatin-1 protein in wound closure of nicotine treated human periodontal ligament fibroblast cells - In vitro study. Arch Oral Biol, 141: 105486. [PMID:35779427] |
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2. Cheng L, Lei X, Yang Z, Kong Y, Xu P, Peng S, Wang J, Chen C, Dong Y, Hu X et al.. (2021)
Histatin 1 enhanced the speed and quality of wound healing through regulating the behaviour of fibroblast. Cell Prolif, 54 (8): e13087. [PMID:34255393] |
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3. Lei XX, Cheng LH, Lin HY, Yang Y, Lu YY, Pang MR, Dong YQ, Bikker FJ, Forouzanfar T, Cheng B et al.. (2022)
The minimal active domain of human salivary histatin 1 is efficacious in promoting acute skin wound healing. Mil Med Res, 9 (1): 41. [PMID:35841072] |
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4. Mateluna C, Torres P, Rodriguez-Peña M, Silva P, Matthies DJ, Criollo A, Bikker FJ, Bolscher JGM, Wilson CAM, Zapata-Torres G et al.. (2022)
Identification of VEGFR2 as the Histatin-1 receptor in endothelial cells. Biochem Pharmacol, 201: 115079. [PMID:35551916] |
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5. Pan L, Zhang X, Gao Q. (2021)
Effects and mechanisms of histatins as novel skin wound-healing agents. J Tissue Viability, 30 (2): 190-195. [PMID:33551241] |
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6. Pan L, Zhang X, Gao Q. (2022)
Histatin-1 alleviates high-glucose injury to skin keratinocytes through MAPK signaling pathway. J Cosmet Dermatol, 21 (11): 6281-6291. [PMID:35819887] |
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7. Shi C, Yao Y, Wang L, Sun P, Feng J, Wu G. (2021)
Human Salivary Histatin-1-Functionalized Gelatin Methacrylate Hydrogels Promote the Regeneration of Cartilage and Subchondral Bone in Temporomandibular Joints. Pharmaceuticals (Basel), 14 (5). [PMID:34069458] |
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8. Son KN, Lee H, Lee SM, Pierre-Jacques D, Shah D, Cologna SM, Aakalu VK. (2024)
Identifying the crucial binding domain of histatin-1 to recombinant TMEM97 in activating chemotactic migration in human corneal epithelial cells. Biochem Biophys Res Commun, 739: 150991. [PMID:39547121] |
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9. Son KN, Lee H, Shah D, Kalmodia S, Miller RC, Ali M, Balasubramaniam A, Cologna SM, Kong H, Shukla D et al.. (2021)
Histatin-1 is an endogenous ligand of the sigma-2 receptor. FEBS J, 288 (23): 6815-6827. [PMID:34233061] |
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10. Sun W, Ma D, Bolscher JGM, Nazmi K, Veerman ECI, Bikker FJ, Sun P, Lin H, Wu G. (2020)
Human Salivary Histatin-1 Promotes Osteogenic Cell Spreading on Both Bio-Inert Substrates and Titanium SLA Surfaces. Front Bioeng Biotechnol, 8: 584410. [PMID:33195147] |
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11. Tapia H, Torres P, Mateluna C, Cáceres M, Torres VA. (2024)
Histatins, proangiogenic molecules with therapeutic implications in regenerative medicine. iScience, 27 (12): 111309. [PMID:39634559] |
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12. Torres P, Hernández N, Mateluna C, Silva P, Reyes M, Solano L, Venegas S, Criollo A, Nazmi K, Bikker FJ et al.. (2021)
Histatin-1 is a novel osteogenic factor that promotes bone cell adhesion, migration, and differentiation. J Tissue Eng Regen Med, 15 (4): 336-346. [PMID:33480156] |
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13. Zhu S, Yu C, Zhao M, Liu N, Chen Z, Liu J, Li G, Deng Y, Sai X, Huang H et al.. (2022)
Histatin-1 loaded multifunctional, adhesive and conductive biomolecular hydrogel to treat diabetic wound. Int J Biol Macromol, 209 (Pt A): 1020-1031. [PMID:35390401] |
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14. Zhu Y, Lou Y, Zhang M, Sun J, Zhang B, Ye Y, Li Z, Lu J, Wan B, Wu G et al.. (2026)
Histatin-1 promotes bone regeneration by coordinating osteogenic and angiogenic responses in a sustained-release hydrogel system. Biomater Adv, 180: 214618. [PMID:41289946] |
