2uzi

From Proteopedia

Revision as of 09:15, 30 October 2007

CRYSTAL STRUCTURE OF HRAS(G12V)- ANTI-RAS FV COMPLEX

Overview

Many disease-related processes occur via protein complexes that are, considered undruggable with small molecules. An example is RAS, which is, frequently mutated in cancer and contributes to initiation and maintenance, of the disease by constitutive signal transduction through protein, interaction with effector proteins, like PI3K, RAF and RALGDS. Such, protein interactions are therefore significant targets for therapy. We, describe a single immunoglobulin variable region domain that specifically, binds to activated GTP-bound RAS and prevents RAS-dependent tumorigenesis, in a mouse model. The crystal structure of the immunoglobulin-RAS complex, shows that the variable region competitively binds to the conformationally, variant regions of RAS, where its signalling effector molecules ... [(full description)]

About this Structure

2UZI is a [Protein complex] structure of sequences from [Homo sapiens] with ZN, MG and GTP as [ligands]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].

Reference

Tumour prevention by a single antibody domain targeting the interaction of signal transduction proteins with RAS., Tanaka T, Williams RL, Rabbitts TH, EMBO J. 2007 Jul 11;26(13):3250-9. Epub 2007 Jun 14. PMID:17568777

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