Open AccessDiscovery and Development of a Novel mPGES-1/5-LOX Dual Inhibitor LFA-9 for Prevention and Treatment of Chronic Inflammatory Diseases
Author(s) -
Nagendra Sastri Yarla,
Gopal Pathuri,
Hariprasad Gali,
Simon Terzyan,
Janani Panneerselvam,
Parthasarathy Chandrakesan,
Marcus Tullius Scotti,
Courtney W. Houchen,
Venkateshwar Madka,
Chinthalapally V. Rao
Publication year - 2020
Publication title -
journal of inflammation research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.656
H-Index - 33
ISSN - 1178-7031
DOI - 10.2147/jir.s286110
Subject(s) - pharmacology , cyclooxygenase , arachidonate 5 lipoxygenase , prostaglandin e2 , inflammation , chemistry , medicine , immunology , enzyme , biochemistry , arachidonic acid
Non-steroidal anti-inflammatory drugs, cyclooxygenase (COX)-2 selective inhibitors, have been explored for prevention and treatment of several inflammatory chronic conditions including arthritis, and cancer. However, the long-term use of these drugs is associated with gastrointestinal, renal, and cardiovascular side effects. Later, COX/5-lipoxygenase (5-LOX) dual inhibitors (eg, licofelone) have been developed but did not enter into the market from the clinical trails due to COX-1/2 inhibition-associated side effects. Hence, targeting microsomal prostaglandin E synthase-1 (mPGES-1) and 5-LOX can be an ideal approach while sparing COX-1/2 activities for development of the next generation of anti-inflammatory drugs with better efficacy and safety.