13th IIS (UK group) symposium

✍ Scribed by Stephen Caddick; Sharon Stone-Elander; Simon G. Patching; Richard B. Herbert; Peter J. F. Henderson; Adrian R. Brough; David A. Middleton; Gregory S. Coumbarides; Jason Eames; Stephanos Ghilagaber; Michael J. Suggate; Neluka Weerasooriya; Alan C. Spivey; Chris Diaper; Ratnasothy Srikaran; Teyrnon Jones; Catherine Noban; George J. Ellames; Andrew Kohler; Harry Wadsworth; Ian S. Blagbrough; James R. Ballinger; Gary Shemilt; R Gordon Reid; Philip D Wilde; Andrew Mangion; Julian G. Knight; Neil J. Geach; Mark F. Oldfield; Jens Atzrodt; Claudia Loewe; Michael R. Chappelle; Calvin R. Hawes; Michael R. Chappelle; Alan D. Morgan; Anthony T. Rees; Sean L. Kitson; Helen Booth; John R. Harding; David P. Woodhouse; Julie A. Bergin; Helen Booth; Nicholas Bushby; John R. Harding; David A. Killick; Clare D. King; David J. Wilkinson; Michael J. Hickey; Lee P. Kingston; John R. Jones; William J.S. Lockley; Andrew N. Mather; David J. Wilkinson; Michael J. Hickey; Lee P. Kingston; John R. Jones; William J.S. Lockley; Andrew N. Mather; Barry McAuley; David J. Wilkinson; Crist N. Filer; Giliyar Ullas; Terry Kelly; Cindy Lloyd; Jeannette Potwin; Christopher Wright; Stuart L. v Adelman; Jane C. Bowden v Adelman; Göran N. Nilsson; Roger Simonsson; David J. Wilkinson; Teyrnon Jones; Alan C Spivey; Andrew Kohler; George Ellames; Marcel C. Cleij; Franklin I. Aigbirhio; Jean-Claude Baron; John C. Clark; Peter Johnström; Tim D. Fryer; Hugh K. Richards; Olivier Barret; John C. Clark; John D. Pickard; Anthony P. Davenport

• Publisher: John Wiley and Sons
• Year: 2004
• Tongue: French
• Weight: 231 KB
• Volume: 47
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.819

✦ Synopsis

The enediyne chromoproteins are a fascinating class of naturally occurring antibiotic, which exhibit potent anti-cancer activity. These substances are isolated from soil bacteria and comprise a highly reactive enediyne chromophore, a ligand, which is non-covalently bound to an apo-protein. It is believed that the biological activity resides with the chromophore, with the apo-protein responsible for stabilisation of the ligand.

This talk will focus on our studies directed toward Neocarzinostatin (NCS). Recent work has enabled the production of isotopically labelled recombinant apoNCS, which has been used to probe the structural requirements for recruiting small drug-like substances into the protein binding site. The use of high field NMR techniques has enabled the level of promiscuity in small molecule binding to be assessed. Further work has examined the potential for the apo-NCS system to stabilize novel nitrogen mustard derivatives. The ability of apoNCS to enter cells will also be discussed.