Hereditary hypo/de‐pigmented dermatoses: An overview

Sehgal, Virendra; Srivastava, Govind

doi:10.1111/j.1365-4632.2008.03105.x

Cited by 11 publications

(5 citation statements)

References 114 publications

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“…18 However, a robust homology model built using structural data from TyB2 and Ipomea batatas catechol oxidase has recently been published. 19 In humans, melanin-related disorders are known to cause cutaneous hyperpigmentation, 20 skin lesions, 21 or melanoma resistance to conventional therapies. 22 As Ty inhibition is a well-established strategy for controlling melanin production in vivo, as demonstrated again recently, 23 the development of TyH inhibitors raises considerable interest in dermocosmetics 24 and cancer therapies 25 fields.…”

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confidence: 99%

2-Hydroxypyridine-N-oxide-Embedded Aurones as Potent Human Tyrosinase Inhibitors

Haudecoeur

Carotti

Gouron

et al. 2016

ACS Med. Chem. Lett.

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With the aim to develop effective and selective human tyrosinase inhibitors, we investigated aurone derivatives whose B-ring was replaced by a non-oxidizable 2-hydroxypyridine-N-oxide (HOPNO) moiety. These aurones were synthesized and evaluated as inhibitors of purified human tyrosinase. Excellent inhibition activity was revealed and rationalized by theoretical calculations. The aurone backbone was especially found to play a crucial role, as the HOPNO moiety alone provided very modest activity on human tyrosinase. Furthermore, the in vitro activity was confirmed by measuring the melanogenesis suppression ability of the compounds in melanoma cell lysates and whole cells. Our study reveals that HOPNO-embedded 6-hydroxyaurone is to date the most effective inhibitor of isolated human tyrosinase. Owing to its low toxicity and its high inhibition activity, it could represent a milestone on the path toward new valuable agents in dermocosmetics, as well as in medical fields where it was recently suggested that tyrosinase could play key roles.

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confidence: 99%

2-Hydroxypyridine-N-oxide-Embedded Aurones as Potent Human Tyrosinase Inhibitors

Haudecoeur

Carotti

Gouron

et al. 2016

ACS Med. Chem. Lett.

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“…1 In mammals, Ty is involved in the twostep oxidation of L-tyrosine into dopaquinone, which is the key product for melanin pigment biosynthesis. Melaninrelated disorders are known to cause serious skin lesions, 2 Parkinson's disease, 3 and melanoma. 4 Because Ty inhibition is now a well-known approach against increased production and accumulation of melanin, 5,6 the development of Ty inhibitors has a huge economical and industrial impact.…”

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confidence: 99%

Binding of 2-Hydroxypyridine-N-oxide on Dicopper(II) Centers: Insights into Tyrosinase Inhibition Mechanism by Transition-State Analogs

et al. 2009

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2-Hydroxypyridine-N-oxide (HOPNO) is described as a new and efficient transition-state analog (TS-analog) inhibitor for the mushroom tyrosinase with an IC(50) = 1.16 microM and a K(I) = 1.8 microM. Using the binuclear copper(II) complex [Cu(2)(BPMP)(mu-OH)](ClO(4))(2) (2) known as a functional model for the tyrosinase catecholase activity, we isolated and fully characterized a 1:1 (2)/OPNO adduct in which the HOPNO is deprotonated and chelates only one Cu-atom of the binuclear site in a bidentate mode. On the basis of these results, a structural model for the tyrosinase inhibition by HOPNO is proposed.

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“…The present case had facial angio-fibroma, shagreen patch, and hypo-melanotic, confetti-like[ 9 10 ] skin lesions, a few of its salient cutaneous manifestations, adequate to consider the diagnosis of TSC, conforming to the major features ( vide supra ).…”

Section: Discussionmentioning

confidence: 87%

Tuberous sclerosis complex: Diagnostic role of magnetic resonance imaging

Sehgal¹,

Singh

Sharma

et al. 2015

Indian J Dermatol

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Tuberous sclerosis complex (TSC) is a well-known clinical entity, characterized by facial angio-fibroma, shagreen patch, and hypo-melanotic, and confetti-like skin lesions. An exquisite fresh case is being narrated, emphasizing its microscopic pathology. The role of magnetic resonance imaging of the brain, in particular, is highlighted to define the large variety of neurological abrasions for determining its future progression.

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Hereditary hypo/de‐pigmented dermatoses: An overview

Cited by 11 publications

References 114 publications

2-Hydroxypyridine-N-oxide-Embedded Aurones as Potent Human Tyrosinase Inhibitors

2-Hydroxypyridine-N-oxide-Embedded Aurones as Potent Human Tyrosinase Inhibitors

Binding of 2-Hydroxypyridine-N-oxide on Dicopper(II) Centers: Insights into Tyrosinase Inhibition Mechanism by Transition-State Analogs

Tuberous sclerosis complex: Diagnostic role of magnetic resonance imaging

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