PMID- 30259737
OWN - NLM
STAT- MEDLINE
DCOM- 20181115
LR  - 20191210
IS  - 1520-5118 (Electronic)
IS  - 0021-8561 (Linking)
VI  - 66
IP  - 44
DP  - 2018 Nov 7
TI  - Discovery of TAS2R14 Agonists from Platycodon grandiflorum Using Virtual 
      Screening and Affinity Screening Based on a Novel TAS2R14-Functionalized HEMT 
      Sensor Combined with UPLC-MS Analysis.
PG  - 11663-11671
LID - 10.1021/acs.jafc.8b04455 [doi]
AB  - TAS2R14 is of great potential as a therapeutic target against asthma, and the 
      discovery of TAS2R14 agonists can be very valuable for treating this disease. 
      Herein, we developed a strategy using virtual screening and affinity screening 
      based on a fabricated biosensor combined with UPLC-MS analysis to screen TAS2R14 
      agonists from Platycodon grandiflorum. By ligand-based virtual screening, 16 
      best-fit candidates were yielded. A novel TAS2R14-functionalized 
      high-electron-mobility transistor (HEMT) sensor was applied to detect and fish 
      out the potential TAS2R14 agonists from P. grandiflorum extracts. Those 
      components captured by the immobilized TAS2R14 were eluted and characterized on 
      UPLC-QTOF MS. As a result, six potential TAS2R14 agonists were screened out and 
      identified. Among them, platycodin L was confirmed to be a special agonist of 
      TAS2R14 for the first time and had an EC(50) of 15.03 +/- 1.15 muM via intracellular 
      calcium mobilization assay ( n = 6). The results indicated that the proposed 
      strategy was efficient to discover TAS2R14 agonists from the herb directly.
FAU - Wang, Zhi-Xin
AU  - Wang ZX
AUID- ORCID: 0000-0001-7255-6049
AD  - Key Laboratory of TCM Information Engineering of State Administration of 
      Traditional Chinese Medicine , Beijing University of Chinese Medicine , Beijing 
      102488 , P. R. China.
FAU - Zhang, Yu-Xin
AU  - Zhang YX
AD  - Key Laboratory of TCM Information Engineering of State Administration of 
      Traditional Chinese Medicine , Beijing University of Chinese Medicine , Beijing 
      102488 , P. R. China.
FAU - Zeng, Yan-Ling
AU  - Zeng YL
AD  - Key Laboratory of TCM Information Engineering of State Administration of 
      Traditional Chinese Medicine , Beijing University of Chinese Medicine , Beijing 
      102488 , P. R. China.
FAU - Li, Xi
AU  - Li X
AD  - Key Laboratory of TCM Information Engineering of State Administration of 
      Traditional Chinese Medicine , Beijing University of Chinese Medicine , Beijing 
      102488 , P. R. China.
FAU - Chen, Zhao
AU  - Chen Z
AD  - Key Laboratory of TCM Information Engineering of State Administration of 
      Traditional Chinese Medicine , Beijing University of Chinese Medicine , Beijing 
      102488 , P. R. China.
FAU - Luo, Jia-Ming
AU  - Luo JM
AD  - Key Laboratory of Semiconductor Materials Science , Chinese Academy of Sciences , 
      Beijing 100083 , P. R. China.
FAU - Zhang, Yang
AU  - Zhang Y
AD  - Key Laboratory of Semiconductor Materials Science , Chinese Academy of Sciences , 
      Beijing 100083 , P. R. China.
FAU - Zhang, Yan-Ling
AU  - Zhang YL
AD  - Key Laboratory of TCM Information Engineering of State Administration of 
      Traditional Chinese Medicine , Beijing University of Chinese Medicine , Beijing 
      102488 , P. R. China.
FAU - Qiao, Yan-Jiang
AU  - Qiao YJ
AD  - Key Laboratory of TCM Information Engineering of State Administration of 
      Traditional Chinese Medicine , Beijing University of Chinese Medicine , Beijing 
      102488 , P. R. China.
LA  - eng
PT  - Evaluation Study
PT  - Journal Article
DEP - 20181019
PL  - United States
TA  - J Agric Food Chem
JT  - Journal of agricultural and food chemistry
JID - 0374755
RN  - 0 (Plant Extracts)
RN  - 0 (Receptors, G-Protein-Coupled)
RN  - 0 (taste receptors, type 2)
SB  - IM
MH  - Chromatography, High Pressure Liquid/*methods
MH  - Drug Evaluation, Preclinical/instrumentation/*methods
MH  - Mass Spectrometry/*methods
MH  - Plant Extracts/*chemistry/isolation & purification
MH  - Plant Roots/chemistry
MH  - Platycodon/*chemistry
MH  - Receptors, G-Protein-Coupled/*agonists/metabolism
OTO - NOTNLM
OT  - Platycodon grandiflorum
OT  - agonists
OT  - high-electron-mobility transistor (HEMT)
OT  - taste type 2 receptor 14 (TAS2R14)
OT  - virtual screening
EDAT- 2018/09/28 06:00
MHDA- 2018/11/16 06:00
CRDT- 2018/09/28 06:00
PHST- 2018/09/28 06:00 [pubmed]
PHST- 2018/11/16 06:00 [medline]
PHST- 2018/09/28 06:00 [entrez]
AID - 10.1021/acs.jafc.8b04455 [doi]
PST - ppublish
SO  - J Agric Food Chem. 2018 Nov 7;66(44):11663-11671. doi: 10.1021/acs.jafc.8b04455. 
      Epub 2018 Oct 19.