| Title |
Covalent fusion inhibitors targeting HIV-1 gp41 deep pocket
|
|---|---|
| Published in |
Amino Acids, September 2012
|
| DOI | 10.1007/s00726-012-1394-8 |
| Pubmed ID | |
| Authors |
Yu Bai, Huifang Xue, Kun Wang, Lifeng Cai, Jiayin Qiu, Shuangyu Bi, Luhua Lai, Maosheng Cheng, Shuwen Liu, Keliang Liu |
| Abstract |
Covalent inhibitors form covalent adducts with their target, thus permanently inhibiting a physiological process. Peptide fusion inhibitors, such as T20 (Fuzeon, enfuvirtide) and C34, interact with the N-terminal heptad repeat of human immunodeficiency virus type 1 (HIV-1) gp41 glycoprotein to form an inactive hetero six-helix bundle (6-HB) to prevent HIV-1 infection of host cells. A covalent strategy was applied to peptide fusion inhibitor design by introducing a thioester group into C34-like peptide. The modified peptide maintains the specific interaction with its target N36. After the 6-HB formation, a covalent bond between C- and N-peptides was formed by an inter-helical acyl transfer reaction, as characterized by various biophysical and biochemical methods. The covalent reaction between the reactive C-peptide fusion inhibitor and its N-peptide target is highly selective, and the reaction greatly increases the thermostability of the 6-HB. The modified peptide maintains high potency against HIV-1-mediated cell-cell fusion and infection. |
Mendeley readers
The data shown below were compiled from readership statistics for 40 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 1 | 3% |
| Austria | 1 | 3% |
| Unknown | 38 | 95% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 9 | 23% |
| Student > Bachelor | 5 | 13% |
| Student > Doctoral Student | 4 | 10% |
| Student > Master | 3 | 8% |
| Professor | 2 | 5% |
| Other | 8 | 20% |
| Unknown | 9 | 23% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 7 | 18% |
| Agricultural and Biological Sciences | 7 | 18% |
| Medicine and Dentistry | 5 | 13% |
| Biochemistry, Genetics and Molecular Biology | 4 | 10% |
| Pharmacology, Toxicology and Pharmaceutical Science | 3 | 8% |
| Other | 4 | 10% |
| Unknown | 10 | 25% |
Attention Score in Context
This research output has an Altmetric Attention Score of 3. 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 25 May 2021.
All research outputs
#7,451,942
of 22,782,096 outputs
Outputs from Amino Acids
#495
of 1,517 outputs
Outputs of similar age
#55,894
of 168,946 outputs
Outputs of similar age from Amino Acids
#8
of 25 outputs
Altmetric has tracked 22,782,096 research outputs across all sources so far. This one is in the 44th percentile – i.e., 44% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,517 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.7. This one is in the 41st percentile – i.e., 41% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 168,946 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 48th percentile – i.e., 48% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 25 others from the same source and published within six weeks on either side of this one. This one is in the 32nd percentile – i.e., 32% of its contemporaries scored the same or lower than it.