title: Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.
abstract: The Class II PI3 kinases are emerging from the shadows of their Class I cousins. The data emerging from PIK3C2 genetic modification studies and from siRNA knockdown suggest important roles in physiology and pathology. With some well-studied Class I isoform inhibitors showing strong Class II activity and a wealth of crystallographic information available, the structural similarity of these isoforms to Class I provides both the opportunity and the challenge in design of selective pharmacological inhibitors.
authors.affiliation: Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
authors.forename: Simon J
authors.initials: SJ
authors.lastname: Mountford
authors.affiliation: Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia ; Australian Centre for Blood Diseases and Department of Clinical Haematology, L6, Monash University , 89 Commerical Road , Prahran, Victoria 3181, Australia.
authors.forename: Zhaohua
authors.initials: Z
authors.lastname: Zheng
authors.affiliation: Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
authors.forename: Krithika
authors.initials: K
authors.lastname: Sundaram
authors.affiliation: Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
authors.forename: Ian G
authors.initials: IG
authors.lastname: Jennings
authors.affiliation: Australian Centre for Blood Diseases and Department of Clinical Haematology, L6, Monash University , 89 Commerical Road , Prahran, Victoria 3181, Australia.
authors.forename: Justin R
authors.initials: JR
authors.lastname: Hamilton
authors.affiliation: Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.
authors.forename: Philip E
authors.initials: PE
authors.lastname: Thompson
keywords: Class II; PI3 kinase; isoform selectivity