Inhibitor of fgf-5 polypeptide and its hair growth application

A peptide inhibitor, FGF-5 technology, applied in the direction of specific peptides, hair care, grooming preparations, etc., can solve the problem of no way to achieve receptor dimerization, achieve convenient purification work, high coupling efficiency, and promote The effect of hair growth

Active Publication Date: 2022-04-29
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

By analyzing the key part of the binding between FGF5 and the receptor, we found the key site of the binding between FGF5 and FGFR, and designed and synthesized a series of polypeptide substances. The obtained polypeptides can block the binding of FGF5 and the FGFR receptor, so there is no way to achieve Receptor dimerization, antagonizing FGF5, thereby blocking downstream signaling related to hair loss caused by FGF5

Method used

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  • Inhibitor of fgf-5 polypeptide and its hair growth application
  • Inhibitor of fgf-5 polypeptide and its hair growth application
  • Inhibitor of fgf-5 polypeptide and its hair growth application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Asp-Val-Gly-Ser-Tyr-Leu-Glu-Gly-Ser-Gln-Asp-Leu-Val-Ala-Gly-NH 2 (SEQ. ID NO: 2)

[0030] microwave-facilitated solid-phase synthesis

[0031] (1) Swelling of the resin

[0032] Weigh 50 mg of Fmoc-Rink amide-MBHA Resin (substitution amount 0.4mmol / g), swell with 7 mL DCM for 30 min, filter to remove DCM, then swell with 10 mL NMP for 30 min, and finally use NMP, DCM, NMP 7 mL to rinse off.

[0033] (2) Microwave promotes removal of Fmoc protecting group

[0034] Put the swollen resin into the reactor, add 7 mL of 25% piperidine / NMP (V / V) solution containing 0.1 M HOBT, react in the microwave reactor for 1 min, the microwave power is 15 W, and the reaction temperature is controlled Within 50 °C, use an air compressor to compress the air to cool, and filter the solution after the reaction; add 7 mL of 25% piperidine / NMP(V / V) solution containing 0.1 M HOBT and react in a microwave reactor for another 4 min , the microwave power was 25 W, the reaction temperature was...

Embodiment 2

[0046] Binding experiments of FGF5 and FGF5 peptide inhibitors

[0047] To determine whether FGF5 peptide inhibitors have an activating effect on FGFR, we analyzed the affinity of FGF5 peptide inhibitors and FGFR1c. We used BIAcore T200 system (GE Healthcare, NJ, USA) to carry out surface ion resonance SPR experiments, the buffer system was HBS-EP buffer (10 mM HEPES-NaOH, pH 7.4, 150 mM NaCl, 3 mM EDTA and 0.005% [ v / v] polysorbate 20), the temperature is 25 ℃.

[0048] Because the D2-D3 region of FGFR1 is sufficient to exert ligand-binding ability], we immobilized FGFR1c (D2-D3 region) on the CM5 chip by amino coupling reaction to obtain the FGFR1c chip. Solvent effects were subtracted from the control channel as a control. Flow FGF5 peptide inhibitors (25 uM, 50 uM, 100 uM, 200 uM, 400 uM) through the chip one by one (including the experimental channel and the control channel). The chip was regenerated by flowing regeneration solution (2.0 M NaCl, 10 mM sodium acetate, p...

Embodiment 3

[0051] Evaluation of the blocking effect of FGF5 inhibitors on downstream signaling pathways

[0052] In order to study the inhibitory effect of FGF5 inhibitors on FGF5, the epidermal cell Hcat was used to stimulate the relevant downstream signaling molecular mechanisms, such as figure 2 As shown, the results of Western blot showed that FGF5 can significantly enhance the expression of downstream p-FRS2, p-Erk2 and p-AKT, and after adding peptide inhibitors, the corresponding phosphorylation indicators of these signaling pathways were weakened in a dose-dependent manner. reduce. It shows that the FGF5 polypeptide inhibitor can effectively inhibit the activity of FGF5.

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Abstract

The invention relates to FGF‑5 inhibitor polypeptides and their hair growth application, and discloses a reagent for inhibiting the action of fibroblast growth factor 5 (FGF5) and its application. ) related receptor peptide analogs, and has a high degree of specificity. The reagent can be used to increase the hair length of mice, and has significant hair growth application value.

Description

technical field [0001] The invention relates to the field of biopharmaceuticals, in particular to an FGF-5 polypeptide inhibitor and its hair growth application. Background technique [0002] Hair growth has a certain periodicity, hair does not grow continuously at a certain speed, but repeats the growth period and rest period at the same time. Hair cycle control is also found in the biological activity of fibroblast growth factor 5 (FGF-5). FGF-5 has the function of inhibiting the growth of hair, making the hair cycle enter the catagen phase from the growth phase, resulting in hair loss. Studies have found that FGF-5S, a short-chain molecule that expresses a large amount of FGF-5 in hair cells in the anagen phase, exhibits an antagonistic effect on FGF-5, delays the transition of hair from the anagen phase to the catagen phase, and promotes hair growth. [0003] Through the study of the mode of action of FGF5 and receptors, it was found that the binding of FGF5 to the ext...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/50A61K38/18A61P17/14A61K8/64A61Q7/00
CPCC07K14/50A61P17/14A61K8/64A61Q7/00A61K38/00
Inventor 王璐瑶赵天阳包京京周洁黄志锋
Owner WENZHOU MEDICAL UNIV
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