| Title |
Design and development of ICCA as a dual inhibitor of GPIIb/IIIa and P-selectin receptors
|
|---|---|
| Published in |
Drug Design, Development and Therapy, July 2018
|
| DOI | 10.2147/dddt.s169238 |
| Pubmed ID | |
| Authors |
Haiyan Chen, An Lu, Xiaoyi Zhang, Lin Gui, Yaonan Wang, Jianhui Wu, Hua Feng, Shiqi Peng, Ming Zhao |
| Abstract |
The impact of upregulation of platelet membrane glycoprotein (GP)IIb/IIIa and P-selectin on the onset of arterial thrombosis, venous thrombosis, and cancer encourages to hypothesize that dual inhibitor of GPIIb/IIIa and P-selectin receptors should simultaneously inhibit arterial thrombosis, block venous thrombosis, and slow tumor growth. For this reason, the structural characteristics and the CDOCKER interaction energies of 12 carbolines were analyzed. This led to the design of 1-(4-isopropyl-phenyl)-β-carboline-3-carboxylic acid (ICCA) as a promising inhibitor of GPIIb/IIIa and P-selectin receptors. The synthetic route provided ICCA in 48% total yield and 99.6% high-performance liquid chromatography purity. In vivo 5 μmol/kg oral ICCA downregulated GPIIb/IIIa and P-selectin expression thereby inhibited arterial thrombosis, blocked venous thrombosis, and slowed down tumor growth, but did not damage the kidney and the liver. Therefore, ICCA could be a promising candidate capable of downregulating GPIIb/IIIa and P-selectin receptors, inhibiting arterial thrombosis, blocking venous thrombosis, and slowing down tumor growth. |
X Demographics
The data shown below were collected from the profiles of 2 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 2 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 50% |
| Science communicators (journalists, bloggers, editors) | 1 | 50% |
Mendeley readers
The data shown below were compiled from readership statistics for 15 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 15 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Master | 3 | 20% |
| Other | 2 | 13% |
| Student > Bachelor | 2 | 13% |
| Student > Ph. D. Student | 1 | 7% |
| Student > Doctoral Student | 1 | 7% |
| Other | 2 | 13% |
| Unknown | 4 | 27% |
| Readers by discipline | Count | As % |
|---|---|---|
| Medicine and Dentistry | 3 | 20% |
| Biochemistry, Genetics and Molecular Biology | 3 | 20% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 13% |
| Environmental Science | 1 | 7% |
| Psychology | 1 | 7% |
| Other | 1 | 7% |
| Unknown | 4 | 27% |
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 20 July 2018.
All research outputs
#19,951,180
of 25,385,509 outputs
Outputs from Drug Design, Development and Therapy
#1,310
of 2,268 outputs
Outputs of similar age
#250,846
of 341,606 outputs
Outputs of similar age from Drug Design, Development and Therapy
#47
of 65 outputs
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