| Title |
Synthesis, activity, and docking study of phenylthiazole acids as potential agonists of PPARγ
|
|---|---|
| Published in |
Drug Design, Development and Therapy, May 2016
|
| DOI | 10.2147/dddt.s106406 |
| Pubmed ID | |
| Authors |
Liang Ma, Taijin Wang, Min Shi, Haoyu Ye |
| Abstract |
Peroxisome proliferator-activated receptor gamma (PPARγ) is a ligand-mediated transcription factor playing key roles in glucose and lipid homeostasis, and PPARγ ligands possess therapeutic potential in these as well as other areas. In this study, a series of phenylthiazole acids have been synthesized and evaluated for agonistic activity by a convenient fluorescence polarization-based PPARγ ligand screening assay. Compound 4t, as a potential PPARγ agonist with half maximal effective concentration (EC50) 0.75±0.20 μM, exhibited in vitro potency comparable with a 0.83±0.14 μM of the positive control rosiglitazone. Molecular docking and molecular dynamics simulations indicated that phenylthiazole acid 4t interacted with the amino acid residues of the active site of the PPARγ complex in a stable manner, consistent with the result of the in vitro ligand assay. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Practitioners (doctors, other healthcare professionals) | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 12 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 12 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Postgraduate | 3 | 25% |
| Student > Ph. D. Student | 2 | 17% |
| Student > Bachelor | 1 | 8% |
| Other | 1 | 8% |
| Researcher | 1 | 8% |
| Other | 1 | 8% |
| Unknown | 3 | 25% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 3 | 25% |
| Medicine and Dentistry | 2 | 17% |
| Biochemistry, Genetics and Molecular Biology | 1 | 8% |
| Neuroscience | 1 | 8% |
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 8% |
| Other | 0 | 0% |
| Unknown | 4 | 33% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 31 May 2016.
All research outputs
#22,758,309
of 25,373,627 outputs
Outputs from Drug Design, Development and Therapy
#1,754
of 2,268 outputs
Outputs of similar age
#269,271
of 311,866 outputs
Outputs of similar age from Drug Design, Development and Therapy
#44
of 63 outputs
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