Discovery, affinity maturation and multimerization of small molecule ligands against human tyrosinase and tyrosinase-related protein 1

Catalano, Marco; Bassi, Gabriele; Rotondi, Giulia; Khettabi, Lyna; Dichiara, Maria; Murer, Patrizia; Scheuermann, Jörg; Soler-López, Montserrat; Neri, Dario

doi:10.1039/d0md00310g

Cited by 11 publications

(2 citation statements)

References 68 publications

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“…However, many studies highlighted the differences between the AbTYR and hTYR isoforms which require diverse structural motifs for their inhibition [133]. In comparison to AbTYR, the number of reported hTYRIs is limited [134]. A study, conducted by Mann and co-workers, pointed out that some well-known TYRIs employed in topical formulations had lower affinities towards hTYR if compared to the fungal isoform [135].…”

Section: Human Tyrosinase Inhibitorsmentioning

confidence: 99%

Heterocyclic Compounds as Synthetic Tyrosinase Inhibitors: Recent Advances

Vittorio

Dank

Ielo

2023

IJMS

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Tyrosinase is a copper-containing enzyme which is widely distributed in nature (e.g., bacteria, mammals, fungi) and involved in two consecutive steps of melanin biosynthesis. In humans, an excessive production of melanin can determine hyperpigmentation disorders as well as neurodegenerative processes in Parkinson’s disease. The development of molecules able to inhibit the high activity of the enzyme remain a current topic in medicinal chemistry, because the inhibitors reported so far present several side effects. Heterocycle-bearing molecules are largely diffuse in this sense. Due to their importance as biologically active compounds, we decided to report a comprehensive review of synthetic tyrosinase inhibitors possessing heterocyclic moieties reported within the last five years. For the reader’s convenience, we classified them as inhibitors of mushroom tyrosinase (Agaricus bisporus) and human tyrosinase.

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Section: Human Tyrosinase Inhibitorsmentioning

confidence: 99%

Heterocyclic Compounds as Synthetic Tyrosinase Inhibitors: Recent Advances

Vittorio

Dank

Ielo

2023

IJMS

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“…Initially, the two BBs in a binding pair are separately decoded and their correlation is lost; thus, ESAC libraries were mostly used for affinity maturation of known ligands. 98,99,103 Recently, an elegant tag-transfer approach was developed to incorporate both sets of codes into one DNA strand (Figure 2b), 37 so that the synergistic BB pairs, instead of individual BBs, could be identified. ESAC libraries have been successfully employed to discover novel ligands against a variety of biological targets.…”

Section: Dual-pharmacophore Esac Librarymentioning

confidence: 99%

Recent advances in DNA-encoded dynamic libraries

Shi

Zhou

2022

RSC Chem. Biol.

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Recent Advances on the Selection Methods of DNA‐Encoded Libraries

Huang

2021

ChemBioChem

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DNA-encoded libraries (DEL) have come of age and become a major technology platform for ligand discovery in both academia and the pharmaceutical industry. Technological maturation in the past two decades and the recent explosive developments of DEL-compatible chemistries have greatly improved the chemical diversity of DELs and fueled its applications in drug discovery. A relatively less-covered aspect of DELs is the selection method. Typically, DEL selection is considered as a binding assay and the selection is conducted with purified protein targets immobilized on a matrix, and the binders are separated from the non-binding background via physical washes. However, the recent innovations in DEL selection methods have not only expanded the target scope of DELs, but also revealed the potential of the DEL technology as a powerful tool in exploring fundamental biology. In this Review, we first cover the "classic" DEL selection methods with purified proteins on solid phase, and then we discuss the strategies to realize DEL selections in solution phase. Finally, we focus on the emerging approaches for DELs to interrogate complex biological targets.

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Discovery, affinity maturation and multimerization of small molecule ligands against human tyrosinase and tyrosinase-related protein 1

Abstract: A series of different strategies were oriented toward the discovery of small molecule ligands binding to the human version of tyrosinase (hTYR) and tyrosinase-related protein 1 (hTYRP1), which may represent the basis for novel treatments of melanoma.

Cited by 11 publications

References 68 publications

Heterocyclic Compounds as Synthetic Tyrosinase Inhibitors: Recent Advances

Heterocyclic Compounds as Synthetic Tyrosinase Inhibitors: Recent Advances

Recent advances in DNA-encoded dynamic libraries

Recent Advances on the Selection Methods of DNA‐Encoded Libraries

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