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

Literature Information

Publication Date 2020-11-13
DOI 10.1039/D0MD00310G
Impact Factor 0
Authors

Marco Catalano, Gabriele Bassi, Maria Dichiara, Patrizia Murer, Jörg Scheuermann, Montserrat Soler-Lopez, Dario Neri


View Original

Abstract

Human tyrosinase (hTYR) and tyrosinase-related protein 1 (hTYRP1) are closely-related enzymes involved in the synthesis of melanin, which are selectively expressed in melanocytes and, in a pathological context, in melanoma lesions. We used a previously described tyrosinase inhibitor (Thiamidolâ„¢) and DNA-encoded library technology for the discovery of novel hTYR and hTYRP1 ligands, that could be used as vehicles for melanoma targeting. Performing de novo selections with DNA-encoded libraries, we discovered novel ligands capable of binding to both hTYR and hTYRP1. More potent ligands were obtained by multimerizing Thiamidolâ„¢ moieties, leading to homotetrameric structures that avidly bound to melanoma cells, as revealed by flow cytometry. These findings suggest that melanoma lesions may, in the future, be targeted not only by monoclonal antibody reagents but also by small organic ligands.

Related Literature

Generation and direct EPR spectroscopic observation of triplet arylphosphinidenes: stabilisation versus internal rearrangements

Eugenii Ya. Misochko, Alexander V. Akimov, Denis V. Korchagin, Yulia S. Ganushevich, Egor A. Melnikov, Vasili A. Miluykov

2020-11-18 Paper

DOI: 10.1039/D0CP05254J

Effects of fixed charge group physicochemistry on anion exchange membrane permselectivity and ion transport

Yuanyuan Ji, Hongxi Luo, Geoffrey M. Geise

2020-03-16 Paper

DOI: 10.1039/D0CP00018C

The interaction of defects in a mayenite structure

Sergey N. Shkerin, Ekaterina S. Ulyanova, Sergey V. Naumov

2020-11-27 Paper

DOI: 10.1039/D0CP05107A

Molecular design of anti-spindle-like molecules by use of siloxanyl terminals for a thermotropic bicontinuous cubic phase

Akane Kawafuchi, Shoichi Kutsumizu, Yuki Kawase, Issei Tokiwa, Taro Udagawa, Yohei Miwa

2020-04-07 Paper

DOI: 10.1039/C9CP06831G

Nucleation in a liquid droplet

2020-04-23 Paper

DOI: 10.1039/D0CP00559B

Study of the surface species during thermal and plasma-enhanced atomic layer deposition of titanium oxide films using in situ IR-spectroscopy and in vacuo X-ray photoelectron spectroscopy

Elisabeth Levrau, Matthias M. Minjauw, Michiel Van Daele, Rita Vos, Jolien Dendooven, Christophe Detavernier

2020-04-08 Paper

DOI: 10.1039/D0CP00395F

Kinked row-induced chirality driven by molecule–substrate interactions

Yannick J. Dappe, Oleksiy L. Kapitanchuk, Delphine Coursault, Emmanuelle Lacaze

2020-02-21 Paper

DOI: 10.1039/C9CP06519A

Boron-terminated diamond (100) surfaces with promising structural and electronic properties

Zhaolong Sun, Mingchao Yang, Xueting Wang, Peng Wang, Chunling Zhang, Nan Gao, Hongdong Li

2020-03-19 Paper

DOI: 10.1039/D0CP00121J

Hierarchical phenomena in multicomponent liquids: simulation methods, analysis, chemistry

Michael J. Servis, Ernesto Martinez-Baez

2020-03-05 Perspective

DOI: 10.1039/D0CP00164C

You might also like

155412-88-71-(3-Aminophenyl)-3-...
Compound Q&A

How should waste containing 1-(D-Ribofuranosyl)-1,4-dihydro-3-pyridinecarboxamide (CAS: 19132-12-8) be handled?

Waste containing 1-(D-Ribofuranosyl)-1,4-dihydro-3-pyridinecarboxamide (CAS: 191...

19132-12-81-(D-Ribofuranosyl)-...
Compound Q&A

What regulatory guidelines apply to 2-Methyl-2-propanyl 3-bromo-3-(hydroxymethyl)-1-azetidinecarboxylate (CAS: 2007919-81-3)?

2-Methyl-2-propanyl 3-bromo-3-(hydroxymethyl)-1-azetidinecarboxylate (CAS: 20079...

2007919-81-32-Methyl-2-propanyl ...
Compound Q&A

What is N-(4-Chloro-2-pyridinyl)acetamide (CAS: 245056-66-0)?

N-(4-Chloro-2-pyridinyl)acetamide (CAS: 245056-66-0) is a chemical compound with...

245056-66-0N-(4-Chloro-2-pyridi...
Compound Q&A

What is 5-Chloro-2-hydroxybenzoic acid (CAS: 321-14-2)?

5-Chloro-2-hydroxybenzoic acid, also known as 5-chlorosalicylic acid, is an arom...

321-14-25-Chloro-2-hydroxybe...
Compound Q&A

What precautions should be taken when handling 1,1-Dichloro-1-fluoroethane (CAS: 1717-00-6)?

When handling 1,1-Dichloro-1-fluoroethane (CAS: 1717-00-6), it is important to u...

1717-00-61,1-Dichloro-1-fluor...
Compound Q&A

What are the physical and chemical properties of Fmoc-(2S,3R)-3-phenylpyrrolidine-2-carboxylic acid (CAS: 281655-32-1)?

Fmoc-(2S,3R)-3-phenylpyrrolidine-2-carboxylic acid is a white crystalline solid ...

281655-32-1Fmoc-(2S,3R)-3-pheny...
Compound Q&A

What are the main uses of 4-Amino-5-bromo-2-pyridinecarboxylic acid (CAS: 1363381-01-4)?

4-Amino-5-bromo-2-pyridinecarboxylic acid is primarily used as a precursor in th...

1363381-01-44-Amino-5-bromo-2-py...
1007881-98-2(S)-tert-butyl 2-((2...
Compound Q&A

What precautions should be taken when handling 8-bromo-2,2-dimethyl-3,4-dihydro-2H-1,4-benzoxazin-3-one (CAS: 688363-73-7)?

When handling 8-bromo-2,2-dimethyl-3,4-dihydro-2H-1,4-benzoxazin-3-one, use prop...

688363-73-78-bromo-2,2-dimethyl...
Disclaimer
This page provides academic journal information for reference and research purposes only. We are not affiliated with any journal publishers and do not handle publication submissions. For publication-related inquiries, please contact the respective journal publishers directly.
If you notice any inaccuracies in the information displayed, please contact us at support@chemtradehub.com. We will promptly review and address your concerns.