Premium
Progress Towards Design of a Light Activated COX‐2 Inhibitor
Author(s) -
Paulishak Wyatt,
Armstrong Christopher,
DeBerardino Maryrose,
Rous Clarissa,
Mertz Pamela,
Streu Craig
Publication year - 2016
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.30.1_supplement.612.9
Subject(s) - cyclooxygenase , aspirin , ibuprofen , pharmacology , enzyme , arachidonic acid , inflammation , medicine , chemistry , biochemistry
Controlled inhibition of enzymes is a therapeutic mechanism that has long been sought after in medicine. Much of modern day therapeutic research has been aimed at targeting specific cell or tissue types with limited success. However, light activated molecules could provide a safe, targetable alternative to these therapeutics. This could allow for drugs with side effects deemed too harmful for use previously to be revisited and modified, allowing for new avenues of treating diseases. Cyclooxygenase‐2 (COX‐2) is an enzyme that synthesizes prostaglandins from arachidonic acid and is responsible for pain and inflammation. Ibuprofen and aspirin act as inhibitors of COX‐2, which has become a well‐understood enzyme usable for testing entirely new types of inhibitors. Previous research on other types of compounds has demonstrated photo‐switchable organic groups that could allow controlled inhibition for site‐specific therapy instead of whole body treatment. Here we discuss the replacement of key groups within known COX‐2 inhibitors and analyze their ability to perform light controlled inhibition of COX‐2.