| Title |
Structure-based drug design, synthesis and biological assays of P. falciparum Atg3–Atg8 protein–protein interaction inhibitors
|
|---|---|
| Published in |
Perspectives in Drug Discovery and Design, January 2018
|
| DOI | 10.1007/s10822-018-0102-5 |
| Pubmed ID | |
| Authors |
Stefania Villa, Laura Legnani, Diego Colombo, Arianna Gelain, Carmen Lammi, Daniele Bongiorno, Denise P. Ilboudo, Kellen E. McGee, Jürgen Bosch, Giovanni Grazioso |
| Abstract |
The proteins involved in the autophagy (Atg) pathway have recently been considered promising targets for the development of new antimalarial drugs. In particular, inhibitors of the protein-protein interaction (PPI) between Atg3 and Atg8 of Plasmodium falciparum retarded the blood- and liver-stages of parasite growth. In this paper, we used computational techniques to design a new class of peptidomimetics mimicking the Atg3 interaction motif, which were then synthesized by click-chemistry. Surface plasmon resonance has been employed to measure the ability of these compounds to inhibit the Atg3-Atg8 reciprocal protein-protein interaction. Moreover, P. falciparum growth inhibition in red blood cell cultures was evaluated as well as the cyto-toxicity of the compounds. |
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 % |
|---|---|---|
| United States | 1 | 50% |
| Unknown | 1 | 50% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 50% |
| Scientists | 1 | 50% |
Mendeley readers
The data shown below were compiled from readership statistics for 23 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 23 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Master | 5 | 22% |
| Researcher | 4 | 17% |
| Student > Ph. D. Student | 3 | 13% |
| Student > Bachelor | 2 | 9% |
| Student > Doctoral Student | 1 | 4% |
| Other | 1 | 4% |
| Unknown | 7 | 30% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 4 | 17% |
| Agricultural and Biological Sciences | 3 | 13% |
| Chemistry | 3 | 13% |
| Biochemistry, Genetics and Molecular Biology | 2 | 9% |
| Immunology and Microbiology | 2 | 9% |
| Other | 1 | 4% |
| Unknown | 8 | 35% |
Attention Score in Context
This research output has an Altmetric Attention Score of 2. 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 01 February 2018.
All research outputs
#16,784,715
of 25,461,852 outputs
Outputs from Perspectives in Drug Discovery and Design
#720
of 949 outputs
Outputs of similar age
#271,375
of 449,716 outputs
Outputs of similar age from Perspectives in Drug Discovery and Design
#7
of 13 outputs
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We're also able to compare this research output to 13 others from the same source and published within six weeks on either side of this one. This one is in the 46th percentile – i.e., 46% of its contemporaries scored the same or lower than it.