Journal ArticleDOI
Synthesis, computational molecular docking analysis and effectiveness on tyrosinase inhibition of kojic acid derivatives
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TLDR
It is suggested that Mannich bases of kojic acid bearing substituted benzyl piperazine groups (compounds 1, 3, 4, 11, 13, 14, 23, 24, 28, and 29) could be promising antityrosinase agents.About:
This article is published in Bioorganic Chemistry.The article was published on 2019-04-27. It has received 42 citations till now. The article focuses on the topics: Kojic acid & Tyrosinase.read more
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Natural and synthetic flavonoid derivatives as new potential tyrosinase inhibitors: a systematic review
Rami J. Obaid,Ehsan Ullah Mughal,Nafeesa Naeem,Amina Sadiq,Reem I. Alsantali,Rabab S. Jassas,Ziad Moussa,Saleh A. Ahmed,Saleh A. Ahmed +8 more
TL;DR: This review article is oriented to provide an insight and a deeper understanding of the tyrosinase inhibitory activity of an array of natural and bioinspired phenolic compounds with special emphasis on flavonoids to demonstrate how the position of ring substituents and their interaction with tyosinase could be correlated with their effectiveness or lack thereof against inhibiting the enzyme.
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Comparing the inhibitory abilities of epigallocatechin-3-gallate and gallocatechin gallate against tyrosinase and their combined effects with kojic acid.
TL;DR: In this article, the inhibitory mechanism of epigallocatechin-3-gallate (EGCG) and gallocatechin gallate (GCG) on tyrosinase was investigated.
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A systematic review of synthetic tyrosinase inhibitors and their structure-activity relationship.
TL;DR: In this paper, the authors systematically summarized the advances of synthetic tyrosinase inhibitors in the literatures, including their inhibitory activity, cytotoxicity, structure-activity relationship (SAR), inhibition kinetics, and interaction mechanisms with the enzyme.
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Piperazine skeleton in the structural modification of natural products: a review.
TL;DR: Piperazine is a cyclic molecule containing two nitrogen atoms in positions 1 and 4, as well as four carbon atoms as discussed by the authors and is one of the most sought heterocyclics for the development of new drug candidates with a wide range of applications.
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Design, synthesis, and anticancer activity of novel 4-thiazolidinone-phenylaminopyrimidine hybrids
TL;DR: A novel series of 5-benzylidene-2-arylimino-4-thiazolidinone derivatives containing phenylaminopyrimidine core were designed, synthesized, and tested for their anticancer activity on K562, PC3, and SHSY-5Y cells and their promising anticancer activities were reported.
References
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Journal ArticleDOI
Sulforhodamine B colorimetric assay for cytotoxicity screening
TL;DR: The sulforhodamine B (SRB) assay is used for cell density determination, based on the measurement of cellular protein content, which is an efficient and highly cost-effective method for screening.
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An Updated Review of Tyrosinase Inhibitors
TL;DR: This article surveys tyrosinase inhibitors newly discovered from natural and synthetic sources and the inhibitory strength is compared with that of a standard inhibitor, kojic acid, and their inhibitory mechanisms are discussed.
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Crystal structure of Agaricus bisporus mushroom tyrosinase: identity of the tetramer subunits and interaction with tropolone.
Wangsa T. Ismaya,Henriëtte J. Rozeboom,A. Weijn,Jurriaan J. Mes,Fabrizia Fusetti,Harry J. Wichers,Bauke W. Dijkstra +6 more
TL;DR: The first structure of the full fungal tyrosinase complex from the mushroom Agaricus bisporus is presented, explaining how calcium ions stabilize the tetrameric state of the enzyme.
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Kinetics of mushroom tyrosinase inhibition by quercetin
Qing-Xi Chen,Isao Kubo +1 more
TL;DR: The inhibition mechanism obtained from Lineweaver-Burk plots show that quercetin is a competitive inhibitor, and the microscopic rate constants were determined for the reaction of quercETin with the enzyme.
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First structures of an active bacterial tyrosinase reveal copper plasticity
TL;DR: It is suggested that residues R209 and V218, situated in a second shell of residues surrounding the active site, play a role in substrate binding orientation based on their flexibility and position, which lends further support to a previously suggested mechanism by which monophenolic substrates dock mainly to CuA.