Histatin 5 TFA 抑制宿主基质金属蛋白酶 MMP-2 和 MMP-9 活性,IC50s 分别为 0.57 和 0.25 μM。
生物活性 |
Histatin 5 TFA inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively.
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IC50 Target |
IC50: 0.57 μM (MMP-2), 0.25 μM (MMP-9)
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体外研究 (In Vitro) |
Histatin 5 is a member of a family of low-molecular-weight salivary proteins secreted by parotid, submandibular, and sublingual glands. Using biotinylated gelatin as a substrate, Histatin 5 is found to inhibit the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively. To localize the domain responsible for this inhibition, three peptides containing different regions of Histatin 5 are synthesized and tested as inhibitors of MMP-9. Peptides comprising residues 1 to 14 and residues 4 to 15 of Histatin 5 show much lower inhibitory activities (IC50s, 21.4 and 20.5 μM, respectively), while a peptide comprising residues 9 to 22 showed identical activity to Histatin 5 against MMP-9. Kinetic analysis of the inhibition of the Arg-gingipain reveals that Histatin 5 is a competitive inhibitor, affecting only the Km with a Ki of 15 μM [1]. Histatin 5 is an inhibitor of mitochondrial respiration.The human salivary antifungal peptide Histatin 5 is taken up by Candida albicans cells and associates intracellularly with mitochondria. Histatin 5 inhibits respiration of isolated C. albicans mitochondria as well as the respiration of intact blastoconidia in a dose and time-dependent manner. Histatin 5 at a concentration of 33 uM inhibits state 2 respiration[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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分子量 |
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Formula |
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Sequence |
Asp-Ser-His-Ala-Lys-Arg-His-His-Gly-Tyr-Lys-Arg-Lys-Phe-His-Glu-Lys-His-His-Ser-His-Arg-Gly-Tyr
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Sequence Shortening |
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中文名称 |
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Sealed storage, away from moisture
Powder |
-80deg;C |
2 years |
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-20deg;C |
1 year |
*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
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Solvent Solubility |
In Vitro:;
H2O
Peptide Solubility and Storage Guidelines:
1.;;Calculate the length of the peptide.
2.;;Calculate the overall charge of the entire peptide according to the following table:
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Contents |
Assign value |
Acidic amino acid |
Asp (D), Glu (E), and the C-terminal -COOH. |
-1 |
Basic amino acid |
Arg (R), Lys (K), His (H), and the N-terminal -NH2 |
+1 |
Neutral amino acid |
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) |
0 |
3.;;Recommended solution:
Overall charge of peptide |
Details |
Negative (lt;0) |
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. |
Positive (gt;0) |
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. |
Zero (=0) |
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
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参考文献 |
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[1]. Gusman H, et al. Salivary histatin 5 is an inhibitor of both host and bacterial enzymes implicated in periodontaldisease. Infect Immun. 2001 Mar;69(3):1402-8.
[2]. Helmerhorst EJ, et al. The human salivary peptide histatin 5 exerts its antifungal activity through the formation ofreactive oxygen species. Proc Natl Acad Sci U S A. 2001 Dec 4;98(25):14637-42.
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