A comprehensive review on tyrosinase inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, Journal Year: 2019, Volume and Issue: 34(1), P. 279 - 309

Published: Jan. 1, 2019

Tyrosinase is a multi-copper enzyme which widely distributed in different organisms and plays an important role the melanogenesis enzymatic browning. Therefore, its inhibitors can be attractive cosmetics medicinal industries as depigmentation agents also food agriculture antibrowning compounds. For this purpose, many natural, semi-synthetic synthetic have been developed by screening methods to date. This review has focused on tyrosinase discovered from all sources biochemically characterised last four decades.

Language: Английский

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Targeting Metalloenzymes for Therapeutic Intervention

Chemical Reviews, Journal Year: 2018, Volume and Issue: 119(2), P. 1323 - 1455

Published: Sept. 7, 2018

Metalloenzymes are central to a wide range of essential biological activities, including nucleic acid modification, protein degradation, and many others. The role metalloenzymes in these processes also makes them for the progression diseases and, as such, attractive targets therapeutic intervention. Increasing awareness play disease their importance class has amplified interest development new strategies develop inhibitors ultimately useful drugs. In this Review, we provide broad overview several drug discovery efforts focused on attempt map out current landscape high-value metalloenzyme targets.

Language: Английский

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Structure and Function of Human Tyrosinase and Tyrosinase‐Related Proteins

Chemistry - A European Journal, Journal Year: 2017, Volume and Issue: 24(1), P. 47 - 55

Published: Oct. 20, 2017

Melanin is the main pigment responsible for color of human skin, hair and eye. Its biosynthesis requires three melanogenic enzymes, tyrosinase (TYR), tyrosinase-related proteins TYRP1 TYRP2. The difficulty isolating pure homogeneous from endogenous sources has hampered their study, resulted in many contradictory findings regarding physiological functions. In this review, we summarize recent advances on structure function TYR TYRPs by virtue crystal TYRP1, which first available a mammalian enzyme. This structure, combined with structures other lower eukaryotes mutagenesis studies key active site residues, sheds light mechanism TYRPs. Furthermore, TYRP1-based homology model provides high-quality platform to map analyze albinism-related mutations, as well design specific antimelanogenic compounds. Finally, provide perspectives future structure/function

Language: Английский

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Structure of Human Tyrosinase Related Protein 1 Reveals a Binuclear Zinc Active Site Important for Melanogenesis

Angewandte Chemie International Edition, Journal Year: 2017, Volume and Issue: 56(33), P. 9812 - 9815

Published: June 29, 2017

Abstract Tyrosinase‐related protein 1 (TYRP1) is one of three tyrosinase‐like glycoenzymes in human melanocytes that are key to the production melanin, compound responsible for pigmentation skin, eye, and hair. Difficulties with producing these enzymes pure form have hampered understanding their activity effect mutations cause albinism disorders. Herein we show typical subdomain TYRP1 contains two zinc ions active site instead copper as found tyrosinases, which explains why does not exhibit tyrosinase redox activity. In addition, structures reveal first time Cys‐rich subdomain, unique vertebrate melanogenic proteins, has an epidermal growth factor‐like fold tightly associated subdomain. Our suggest most albinism‐related affect its stability or

Language: Английский

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Tyrosinase Inhibitors Naturally Present in Plants and Synthetic Modifications of These Natural Products as Anti-Melanogenic Agents: A Review

Molecules, Journal Year: 2023, Volume and Issue: 28(1), P. 378 - 378

Published: Jan. 2, 2023

Tyrosinase is a key enzyme target to design new chemical ligands against melanogenesis. In the current review, different derivatives are explored which have been used as anti-melanogenic compounds. These compounds naturally present in plants and semi-synthetic synthetic inspired by these natural products, such kojic acid produced several species of fungi; arbutin—a glycosylated hydroquinone extracted from bearberry plant; vanillin—a phenolic aldehyde vanilla bean, etc. After inhibition screening, various showed therapeutic effects tyrosinase inhibitors with values constant IC50. We show how appropriately designed scaffolds structures develop novel inhibitors. review results numerous studies, could lead development effective anti-tyrosinase agents increased efficiency safety near future, many applications food, pharmaceutical cosmetics industries.

Language: Английский

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A medicinal chemistry perspective of drug repositioning: Recent advances and challenges in drug discovery

European Journal of Medicinal Chemistry, Journal Year: 2020, Volume and Issue: 195, P. 112275 - 112275

Published: April 2, 2020

Language: Английский

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Tyrosinase inhibition by some flavonoids: Inhibitory activity, mechanism by in vitro and in silico studies

Bioorganic Chemistry, Journal Year: 2018, Volume and Issue: 81, P. 168 - 174

Published: Aug. 14, 2018

Language: Английский

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Advances in the Design of Genuine Human Tyrosinase Inhibitors for Targeting Melanogenesis and Related Pigmentations

Journal of Medicinal Chemistry, Journal Year: 2020, Volume and Issue: 63(22), P. 13428 - 13443

Published: July 31, 2020

Human tyrosinase (hsTYR) is the key enzyme ensuring conversion of l-tyrosine to dopaquinone, thereby initiating melanin synthesis, i.e., melanogenesis. Although protein has long been familiar, knowledge about its three-dimensional structure and efficient overexpression protocols emerged only recently. Consequently, for decades medicinal chemistry studies aiming at developing skin depigmenting agents relied almost exclusively on biological assays performed using mushroom (abTYR), producing a plethoric literature, often little useful purpose. Indeed, several recent reports have pointed out spectacular differences in terms interaction patterns inhibition values between hsTYR abTYR, including widely used standard inhibitors. In this review, we summarize last developments regarding potential role human pathologies, advances recombinant expression systems structural data retrieving, pioneer generation true Finally, present suggestions design future inhibitors highly attractive target pharmacology dermocosmetics.

Language: Английский

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Review on the Use of Kojic Acid—A Skin-Lightening Ingredient

Cosmetics, Journal Year: 2022, Volume and Issue: 9(3), P. 64 - 64

Published: June 15, 2022

This article reviews the use of Kojic Acid (KA) as a skin-lightening ingredient in cosmetics industry. In 1907, Saito discovered KA, natural product; it has since become one most investigated agents. paper highlights findings research conducted on this agent. It been found that KA certain disadvantages, and researchers have attempted to mitigate these disadvantages by designing new equivalents are more efficient tyrosinase inhibition. These also safe improved properties solubility. The Cosmeceutical Ingredient Review (CIR) indicates can be safely used at concentration not higher than 1% due its cytotoxicity. Other scientific data support safety 2% or less. was shown helpful treatment hyper pigmentary disorders, such freckles, age spots, post-inflammatory hyperpigmentation, melasma, which proven clinically.

Language: Английский

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Synthesis and biological evaluation of new kojic acid-1,3,4-oxadiazole hybrids as tyrosinase inhibitors and their application in the anti-browning of fresh-cut mushrooms

Food Chemistry, Journal Year: 2022, Volume and Issue: 409, P. 135275 - 135275

Published: Dec. 22, 2022

Language: Английский

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