Reading the iSee version of the articles offline - first-time installation instructions.

<p>Reading the iSee version of the articles offline - first-time installation instructions.</p

Reading the iSee version of the articles on-line - first-time installation instructions.

<p>Reading the iSee version of the articles on-line - first-time installation instructions.</p

Main features of the enhanced iSee version of the articles and a quick reference guide to interact and use the graphical display window.

<p>Both on-line and offline (standalone) versions of the enhanced iSee articles have the same controls and layouts.</p

Human Pleckstrin Homology domain Interacting Protein (PHIP); A Target Enabling Package

<p>SGC Oxford has expressed, purified and crystallized the second bromodomain of PHIP as part of the probe programme. Fragment screening and X-ray crystallography identified binders, some of which optimised to uM affinity. However, molecules with probe properties were not obtained. Consequently it has been decided to put the information generated into the public domain.</p

Human Pleckstrin Homology domain Interacting Protein (PHIP); A Target Enabling Package

<p>SGC Oxford has expressed, purified and crystallized the second bromodomain of PHIP as part of the probe programme. Fragment screening and X-ray crystallography identified binders, some of which optimised to uM affinity. However, molecules with probe properties were not obtained. Consequently it has been decided to put the information generated into the public domain.</p

[1,2,4]Triazolo[4,3‑<i>a</i>]phthalazines: Inhibitors of Diverse Bromodomains

Bromodomains are gaining increasing interest as drug targets. Commercially sourced and de novo synthesized substituted [1,2,4]­triazolo­[4,3-<i>a</i>]­phthalazines are potent inhibitors of both the BET bromodomains such as BRD4 as well as bromodomains outside the BET family such as BRD9, CECR2, and CREBBP. This new series of compounds is the first example of submicromolar inhibitors of bromodomains outside the BET subfamily. Representative compounds are active in cells exhibiting potent cellular inhibition activity in a FRAP model of CREBBP and chromatin association. The compounds described are valuable starting points for discovery of selective bromodomain inhibitors and inhibitors with mixed bromodomain pharmacology