PMID- 30060458
OWN - NLM
STAT- MEDLINE
DCOM- 20181121
LR  - 20220408
IS  - 1422-0067 (Electronic)
IS  - 1422-0067 (Linking)
VI  - 19
IP  - 8
DP  - 2018 Jul 27
TI  - The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors 
      Ligands in Clinical Drug Discovery and Development.
LID - 10.3390/ijms19082189 [doi]
LID - 2189
AB  - Peroxisome proliferator-activated receptors (PPARs) are a well-known 
      pharmacological target for the treatment of multiple diseases, including diabetes 
      mellitus, dyslipidemia, cardiovascular diseases and even primary biliary 
      cholangitis, gout, cancer, Alzheimer's disease and ulcerative colitis. The three 
      PPAR isoforms (alpha, beta/delta and gamma) have emerged as integrators of glucose and lipid 
      metabolic signaling networks. Typically, PPARalpha is activated by fibrates, which 
      are commonly used therapeutic agents in the treatment of dyslipidemia. The 
      pharmacological activators of PPARgamma include thiazolidinediones (TZDs), which are 
      insulin sensitizers used in the treatment of type 2 diabetes mellitus (T2DM), 
      despite some drawbacks. In this review, we summarize 84 types of PPAR synthetic 
      ligands introduced to date for the treatment of metabolic and other diseases and 
      provide a comprehensive analysis of the current applications and problems of 
      these ligands in clinical drug discovery and development.
FAU - Hong, Fan
AU  - Hong F
AD  - Beijing Key Laboratory of Gene Resource and Molecular Development, College of 
      Life Sciences, Beijing Normal University, Beijing 100875, China. 
      hongfanky@126.com.
AD  - Key Laboratory for Cell Proliferation and Regulation Biology of State Education 
      Ministry, College of Life Sciences, Beijing Normal University, Beijing 100875, 
      China. hongfanky@126.com.
FAU - Xu, Pengfei
AU  - Xu P
AD  - Beijing Key Laboratory of Gene Resource and Molecular Development, College of 
      Life Sciences, Beijing Normal University, Beijing 100875, China. pex9@pitt.edu.
FAU - Zhai, Yonggong
AU  - Zhai Y
AD  - Beijing Key Laboratory of Gene Resource and Molecular Development, College of 
      Life Sciences, Beijing Normal University, Beijing 100875, China. 
      ygzhai@bnu.edu.cn.
AD  - Key Laboratory for Cell Proliferation and Regulation Biology of State Education 
      Ministry, College of Life Sciences, Beijing Normal University, Beijing 100875, 
      China. ygzhai@bnu.edu.cn.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20180727
PL  - Switzerland
TA  - Int J Mol Sci
JT  - International journal of molecular sciences
JID - 101092791
RN  - 0 (Anti-Inflammatory Agents)
RN  - 0 (Hypolipidemic Agents)
RN  - 0 (Ligands)
RN  - 0 (Peroxisome Proliferator-Activated Receptors)
RN  - 0 (Protein Isoforms)
SB  - IM
MH  - Animals
MH  - Anti-Inflammatory Agents/therapeutic use
MH  - Disease Models, Animal
MH  - *Drug Discovery
MH  - Humans
MH  - Hypolipidemic Agents/therapeutic use
MH  - Ligands
MH  - Metabolic Diseases/*drug therapy
MH  - Mice
MH  - Molecular Conformation
MH  - *Molecular Targeted Therapy
MH  - Peroxisome Proliferator-Activated Receptors/*agonists/*chemistry/metabolism
MH  - Protein Isoforms/agonists/chemistry/metabolism
MH  - Rats
PMC - PMC6121873
OTO - NOTNLM
OT  - PPAR
OT  - T2DM
OT  - TZDs
OT  - dyslipidemia
OT  - ligand
COIS- The authors declare no conflict of interest.
EDAT- 2018/08/01 06:00
MHDA- 2018/11/22 06:00
PMCR- 2018/08/01
CRDT- 2018/08/01 06:00
PHST- 2018/06/22 00:00 [received]
PHST- 2018/07/16 00:00 [revised]
PHST- 2018/07/24 00:00 [accepted]
PHST- 2018/08/01 06:00 [entrez]
PHST- 2018/08/01 06:00 [pubmed]
PHST- 2018/11/22 06:00 [medline]
PHST- 2018/08/01 00:00 [pmc-release]
AID - ijms19082189 [pii]
AID - ijms-19-02189 [pii]
AID - 10.3390/ijms19082189 [doi]
PST - epublish
SO  - Int J Mol Sci. 2018 Jul 27;19(8):2189. doi: 10.3390/ijms19082189.