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Short peptide-based inhibition of fusion remains an attractive goal in anti-human immunodeficiency virus (HIV) research based on its potential for the development of technically and economically desirable antiviral agents. Herein, we report use of the dithiol bis-alkylation reaction to generate a series of m-xylene thioether-stapled 22-residue α-helical peptides that have been identified as fusion inhibitors targeting HIV-1 glycoprotein 41 (gp41). The peptide sequence is based on the helix-zone binding domain (HBD) of the gp41 C-terminal heptad repeat (CHR) region. We found that one of these stapled peptides, named hCS6ERE, showed promising inhibitory potency against HIV-1 Env-mediated cell-cell fusion and viral replication at a level comparable to the clinically used 36-mer peptide T20. Furthermore, combining hCS6ERE with a fusion inhibitor having a different target site, such as HP23, produced synergistic anti-HIV-1 activity. Collectively, our study offers new insight into the design of anti-HIV peptides with short sequences.
This article was published in the following journal.
Name: Journal of medicinal chemistry
Hydrocarbon stapled (HCS) peptides are a class of cross-linked α-helix mimetics. The technology relies on the use of α,α'-disubstituted alkenyl amino acids, which fully contrain the helical region ...
Compared to small molecule drugs, peptide therapeutics provide greater efficacy, selectivity, and safety. The intrinsic disadvantages of peptides are their sensitivity to proteases. To overcome this, ...
The toxic effects of p-xylene, 4-methylbenzyl alcohol, p-methyl benzaldehyde, and p-toluic acid on two marine microalgae (Phaeodactylum tricornutum Bohlin, and Skeletonema costatum) were investigated....
A new filter was developed to collect harmful algae colonies by adapting the cross-step filtration structures and mechanisms discovered recently in filter-feeding fish. Extending beyond previously pub...
The design of chiral chromophores that lead to self-assembly of higher order helical structures is a powerful tool to understand the hierarchical helical structures of molecules of nature. In this wor...
Carcinoma esophagus is a common cause of dysphagia. Once dysphagia occurs, a majority of the tumours are advanced. Most of them would require some form of treatments for control of dysphag...
The aim of this study is to determine the role of stapled anopexy in the treatment of haemorrhoids by comparing it to the current gold standard treatment, which is excisional haemorrhoidec...
To assess the safety and efficacy of a single fraction of radiotherapy using helical tomotherapy to treat bone metastases.
Neonatal intestinal atresia is the most difficult disease to apply stapled anastomosis. However, there are no high-quality clinical trial to verify its effectiveness. Therefore, the invest...
The stapled transanal rectal resection (STARR procedure) is an effective treatment for obstructed defecation syndrome (ODS) caused by intussusception and rectocele. Recently a new techniqu...
A family of non-fibrillar collagens that interact with FIBRILLAR COLLAGENS. They contain short triple helical domains interrupted by short non-helical domains and do not form into collagen fibrils.
A field of biological research combining engineering in the formulation, design, and building (synthesis) of novel biological structures, functions, and systems.
An approach, process, or methodology which emphasizes credible evidence and the best available scientific knowledge, judiciously integrated to achieve the best possible outcomes in structural design. For example, the design of a new OUTPATIENT CLINIC might incorporate a review of published research on outpatient clinic design, decisions on similar past projects, along with interviews with staff and consumers.
Architecture, exterior and interior design, and construction of facilities other than hospitals, e.g., dental schools, medical schools, ambulatory care clinics, and specified units of health care facilities. The concept also includes architecture, design, and construction of specialized contained, controlled, or closed research environments including those of space labs and stations.
The architecture, functional design, and construction of hospitals.
Biological therapy involves the use of living organisms, substances derived from living organisms, or laboratory-produced versions of such substances to treat disease. Some biological therapies for cancer use vaccines or bacteria to stimulate the body&rs...
Human Immuno Deficiency Virus (HIV)
Human Immunodeficiency Virus (HIV), the causative agent of AIDS. The Human Immunodeficiency Virus, more commonly known as HIV, is a member of the lentivirus sub-set of the retrovirus family of pathogens. It causes AIDS, or Acquired Immuno Deficiency Sy...