PMID- 21694679
OWN - NLM
STAT- MEDLINE
DCOM- 20110915
LR  - 20240109
IS  - 1420-3049 (Electronic)
IS  - 1420-3049 (Linking)
VI  - 16
IP  - 6
DP  - 2011 Jun 21
TI  - Inhibitory activity of flavonoids against class I phosphatidylinositol 3-kinase 
      isoforms.
PG  - 5159-67
LID - 10.3390/molecules16065159 [doi]
AB  - Class I PI3 Kinase (PI3K) phosphorylates phosphatidylinositol 4,5-bisphophate 
      (PIP2) to generate the second messenger phosphatidylinositol 3,4,5-trisphosphate 
      (PIP3) and therefore plays an important role in fundamental cellular responses 
      such as proliferation. There are four isoforms of class I PI3K which are known to 
      have different functions and relate to various diseases such as cancer and 
      inflammation. Flavonoids are abundant in fruits, vegetables and plant-derived 
      beverages such as tea. So far, various pharmacological effects of flavonoids have 
      been reported. We previously reported that the flavonoid baicalein exhibits 
      potent PI3K-inhibitory activity. Recently we examined the inhibitory activity of 
      eighteen flavonoids against PI3Ka by using an in vitro homogenous time resolved 
      fluorescence (HTRF) kinase assay, and deduced their structure-activity 
      relationships by comparing the activities of the analogues. Our result suggests 
      that the number of hydroxyl groups in the A and B rings might promote the 
      activity, while loss of C2-C3 double bond might reduce the activity. Furthermore, 
      the activity against 4 class I PI3K isoforms of some selected flavonoids was 
      investigated, and the results indicate that the flavonoids seem to exhibit more 
      potent activity on PI3Ka and d isoforms compared with that on PI3Kb and g 
      isoforms.
FAU - Kong, Dexin
AU  - Kong D
AD  - School of Pharmaceutical Sciences and Research Center of Basic Medical Sciences, 
      Tianjin Medical University, Tianjin, China. kongdexin@tijmu.edu.cn
FAU - Zhang, Yanwen
AU  - Zhang Y
FAU - Yamori, Takao
AU  - Yamori T
FAU - Duan, Hongquan
AU  - Duan H
FAU - Jin, Meihua
AU  - Jin M
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20110621
PL  - Switzerland
TA  - Molecules
JT  - Molecules (Basel, Switzerland)
JID - 100964009
RN  - 0 (Enzyme Inhibitors)
RN  - 0 (Flavonoids)
RN  - 0 (Isoenzymes)
RN  - EC 2.7.1.137 (Class I Phosphatidylinositol 3-Kinases)
SB  - IM
MH  - Class I Phosphatidylinositol 3-Kinases/*antagonists & inhibitors
MH  - Enzyme Activation/*drug effects
MH  - Enzyme Inhibitors/chemistry/*pharmacology
MH  - Flavonoids/chemistry/*pharmacology
MH  - Isoenzymes/antagonists & inhibitors
MH  - Structure-Activity Relationship
PMC - PMC6264676
COIS- The authors declare no conflict of interest.
EDAT- 2011/06/23 06:00
MHDA- 2011/09/16 06:00
PMCR- 2011/06/21
CRDT- 2011/06/23 06:00
PHST- 2011/06/03 00:00 [received]
PHST- 2011/06/16 00:00 [revised]
PHST- 2011/06/17 00:00 [accepted]
PHST- 2011/06/23 06:00 [entrez]
PHST- 2011/06/23 06:00 [pubmed]
PHST- 2011/09/16 06:00 [medline]
PHST- 2011/06/21 00:00 [pmc-release]
AID - molecules16065159 [pii]
AID - molecules-16-05159 [pii]
AID - 10.3390/molecules16065159 [doi]
PST - epublish
SO  - Molecules. 2011 Jun 21;16(6):5159-67. doi: 10.3390/molecules16065159.