eprintid: 19978
rev_number: 16
userid: 1419
dir: disk0/00/01/99/78
datestamp: 2013-11-12 17:17:00
lastmod: 2019-02-02 15:56:50
status_changed: 2013-11-12 17:17:00
type: article
metadata_visibility: show
item_issues_count: 0
eprint_status: archive
creators_name: Wipf, P
creators_name: Halter, RJ
creators_email: pwipf@pitt.edu
creators_email: 
creators_id: PWIPF
creators_id: 
title: Chemistry and biology of wortmannin
ispublished: pub
divisions: sch_as_chemistry
full_text_status: public
abstract: Recent synthetic and biological studies of the viridin class of steroidal furans have revealed multiple opportunities for fundamental discoveries as well as advanced drug design. Wortmannin is a potent enzyme inhibitor that binds to the ATP site of important regulatory kinases such as PI-3 kinase and Polo-like kinase. The natural product shares a unique mechanism-based biological activation pathway with other viridins. Furthermore, while there have been several encouraging approaches toward the total synthesis of these compounds, there is still ample room for improvements in synthetic strategies and tactics, and the development of structurally simplified analogs that exert more specific biological effects and are devoid of toxicity issues that have thwarted the clinical development of the parent compounds. © The Royal Society of Chemistry 2005.
date: 2005-06-07
date_type: published
publication: Organic and Biomolecular Chemistry
volume: 3
number: 11
pagerange: 2053 - 2061
refereed: TRUE
issn: 1477-0520
id_number: 10.1039/b504418a
pmid: 15917886
mesh_headings: Adenosine Triphosphate--metabolism
mesh_headings: Androstadienes--chemistry
mesh_headings: Androstadienes--metabolism
mesh_headings: Enzyme Inhibitors--chemistry
mesh_headings: Enzyme Inhibitors--metabolism
mesh_headings: Models, Molecular
mesh_headings: Phosphatidylinositol 3-Kinases--antagonists & inhibitors
mesh_headings: Phosphatidylinositol 3-Kinases--chemistry
mesh_headings: Phosphatidylinositol 3-Kinases--metabolism
chemical_names: Androstadienes
chemical_names: Enzyme Inhibitors
chemical_names: wortmannin
chemical_names: Adenosine Triphosphate
chemical_names: Phosphatidylinositol 3-Kinases
citation:   Wipf, P and Halter, RJ  (2005) Chemistry and biology of wortmannin.  Organic and Biomolecular Chemistry, 3 (11).  2053 - 2061.  ISSN 1477-0520     
document_url: http://d-scholarship-dev.library.pitt.edu/19978/1/licence.txt