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PROTAC for targeted degradation of tyrosinase, and application thereof

A compound and structural formula technology, applied in the field of compounds targeting the degradation of tyrosinase, can solve problems such as skin damage and adverse off-target effects

Active Publication Date: 2021-12-03
CHENGDU INST OF BIOLOGY CHINESE ACAD OF S
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, in order to produce inhibition, tyrosinase inhibitors need to continuously occupy the active site of the target protein, but high doses can cause undesirable off-target effects and cause damage to the skin

Method used

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  • PROTAC for targeted degradation of tyrosinase, and application thereof
  • PROTAC for targeted degradation of tyrosinase, and application thereof
  • PROTAC for targeted degradation of tyrosinase, and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Synthetic route of small molecule targeting E3 ubiquitin ligase

[0033]

Embodiment 2

[0035] Design and synthetic route of targeting small molecules with levodopa or 3,4-dihydroxyphenylpropionic acid

[0036]

Embodiment 3

[0038] Synthetic route of alkane carbon chain compounds (L-C2—L-C10) targeting the degradation of tyrosinase

[0039]

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PUM

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Abstract

The invention relates to tyrosinase-targeted PROTAC and application thereof, and belongs to the technical field of skin whitening cosmetic new raw materials and skin disease treatment drugs. The technical problem to be solved by the invention is to provide the compound for targeted degradation of tyrosinase by using PROTAC, and a salt, a prodrug, a hydrate or a solvate thereof. The structural formula of the PROTAC molecule is shown as a formula I in the specification. A series of tyrosinase-targeted PROTAC molecules are successfully prepared by coupling tyrosinase ligands with ligands of E3 ligase through linkers of different types and different chain lengths, can effectively target a target protein and reduce the content of tyrosinase in cells, have a better effect of reducing melanin in vivo and in vitro, are lower in toxicity to normal cells, and meet the characteristics of high efficiency and low toxicity.

Description

technical field [0001] The invention relates to a compound, a technical method and an application for targeting and degrading tyrosinase (tyrosinase, TYR for short). Background technique [0002] Hyperpigmentation is the process by which melanocytes in the skin and hair follicles synthesize melanin, which protects the epidermis from UV radiation, environmental pollutants, and toxic drugs and chemicals. However, abnormal levels of melanin can lead to serious skin conditions including freckles, melasma, senile lentils and pigmented acne scars. In addition, epidermal skin pigmentation increases markedly with skin wound healing and UV exposure. Therefore, regulation of melanin production is an important avenue for the treatment of medical pigmentation disorders and safe cosmetic practice. In fact, the synthesis of melanin is determined by the main rate-limiting enzyme, tyrosinase (EC1.14.18.1, TYR for short), which catalyzes the hydroxylation of tyrosine to 3,4-dihydroxyphenyl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04A61P17/00A61K31/454A61K8/49A61Q19/02A61Q19/00
CPCC07D401/04A61P17/00A61K8/4926A61Q19/02A61Q19/00
Inventor 唐卓付丁强袁奕李光勋
Owner CHENGDU INST OF BIOLOGY CHINESE ACAD OF S
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