Targeting the tubulin C-terminal tail by charged small molecules

Author:

Li Shuo1ORCID,Mori Mattia2,Yang Mingyan1ORCID,Elfazazi Soumia3ORCID,Hortigüela Rafael3,Chan Peter4,Feng Xinyue5,Risinger April4ORCID,Yang Zhiyou5,Oliva María Ángela3,Fernando Díaz J.3ORCID,Fang Wei-Shuo1ORCID

Affiliation:

1. State Key Laboratory of Bioactive Substances and Functions of Natural Medicines & MHC Key Laboratory of Biosynthesis of Natural Products, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, 2A Nan Wei Road, Beijing 100050, China

2. Department of Biotechnology, Chemistry and Pharmacy, University of Siena, via Aldo Moro 2, Siena 53100, Italy

3. Centro de Investigaciones Biológicas Margarita Salas, Consejo Superior de Investigaciones Científicas, Ramiro de Maeztu 9, Madrid 28040, Spain

4. Department of Pharmacology, University of Texas Health Science Center at San Antonio, San Antonio, Texas 78229, USA

5. College of Food Science and Technology, Guangdong Ocean University, Guangdong Provincial Key Laboratory of Aquatic Product Processing and Safety, Guangdong Province Engineering Laboratory for Marine Biological Products, Guangdong Provincial Engineering Technology Research Center of Seafood, Key Laboratory of Advanced Processing of Aquatic Product of Guangdong Higher Education Institution, Zhanjiang 524088, China

Abstract

A series of linear and cyclic peptides bearing triple arginines were synthesized to bind to the tubulin C-terminal tail, providing a starting point to target this versatile yet undruggable site.

Funder

Ministerio de Ciencia e Innovación

Natural Science Foundation of Guangdong Province

Max and Minnie Tomerlin Voelcker Fund

European Commission

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry

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