Hi Kendall, in cAMP-dependent protein kinase (PKA) in complex with the bisindolyl maleimide inhibitor BIM-2, two conformations of the inhibitor are seen in the two kinase molecules of the asymmetric unit.
Gassel M, Breitenlechner CB, König N, Huber R, Engh RA, Bossemeyer D. The protein kinase C inhibitor bisindolyl maleimide 2 binds with reversed orientations to different conformations of protein kinase A. J Biol Chem. 2004 May 28;279(22):23679-90. Epub 2004 Mar 1. we only saw one conformation of the same inhibitor in complex with PDK1. Komander D, Kular GS, Schüttelkopf AW, Deak M, Prakash KR, Bain J, Elliott M, Garrido-Franco M, Kozikowski AP, Alessi DR, van Aalten DM. Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1. Structure. 2004 Feb;12(2):215-26. HTH david _______________________________________________________ David Komander, PhD Beit Memorial Fellow Section of Structural Biology Chester Beatty Laboratories The Institute of Cancer Research 237 Fulham Road London, SW3 6JB, UK Tel. : +44 (0)20 7153 5447 FAX : +44 (0)20 7153 5457 email: [EMAIL PROTECTED] On Tuesday, February 19, 2008, at 02:12AM, "Kendall Nettles" <[EMAIL PROTECTED]> wrote: >Jon, I have not had any replies. I did hear a talk at an American Chemical >Society meeting on a ligand flipping between the two estrogen receptor >subtypes, but it hasn¹t been published from what I can tell. Here¹s a link >to the abstract. > >membership.acs.org/C/COMP/pastprograms/Fall06abstracts.pdf > >Kendall > > >On 2/18/08 8:38 PM, "Read, Jon" <[EMAIL PROTECTED]> wrote: > >> Hi Kendall, >> did you get any replies about this as I would be interested in hearing about >> these. I have seen some talks of kinases which mention this but can't recall >> the targets. >>> >>> -----Original Message----- >>> From: CCP4 bulletin board [mailto:[EMAIL PROTECTED] Behalf Of Kendall >>> Nettles >>> Sent: Saturday, February 09, 2008 11:04 AM >>> To: CCP4BB@JISCMAIL.AC.UK >>> Subject: [ccp4bb] References for ligand flipping >>> >>> >>> >>> Hi, >>> Thanks to everyone for suggestions on making disulfides. I do have another >>> question. >>> >>> Can anyone suggest some references for structures showing that a small >>> molecule ligand binds differently in closely related proteins? >>> >>> >>> Thanks, >>> Kendall >>> -- >>> Kendall W. Nettles, PhD >>> Assistant Professor >>> Department of Cancer Biology >>> The Scripps Research Institute >>> 5353 Parkside Dr. >>> Jupiter Fl 33458 >>> >> > > >
