by EPS Pool of Writers
Small peptide and amino acid derivatives in the search for SARS-CoV2 main protease inhibitors
In times of COVID-19 pandemic, science is advancing very fast, faster than ever. The first vaccines and various diagnosis probes are already in the market. There is an approved drug, remdesivir, and intensive work is being done on drug repurposing, with massive studies in clinical trials. In this…
Peptide Therapeutics for COVID-19
As the world struggles to cope with the current COVID-19 pandemic, in this edition of “Peptide Highlights” we present a survey of peptide drugs which are being investigated as potential therapies for the disease. For more please download PDF file. Contributed by Susan J. Tzotzos Susan…
Imine-derived macrocyclic peptides
In recent years, macrocyclic peptides are attracting a growing attention of pharmaceutical/biotech companies and academic groups. Their intermediate size, in-between small-molecule drugs and biotherapeutics, enable their utility as modulators of therapeutically relevant protein-protein interactions…
Life imitates cookery: lysinoalanine crosslinks in peptides and proteins
The lysinoalanine crosslink – a type of protein post-translational modification – was initially discovered in vitro and later found to occur in cooked and processed food. Curiously, the same kind of crosslink occurs in certain peptide antibiotics; and there is evidence to suggest that it also…
The hitchhiker´s guide to chemoselectivity in chemical protein synthesis
Posttranslational modifications (PTMs) allow proteins to perform a variety of physiological functions. Thus, it is of prime importance to elucidate their role on proteins in physiological and/or pathophysiological processes. However, molecular biological methods to generate proteins either does not…
Peptide Drugs of the Decade
The approaching end of another decade prompted this short review of peptide drugs that successfully reached the European market from 2010 to the present. The article also gives a comparison of numbers of marketing authorisations granted to peptide drugs in Europe and the US over the last two…
“Sweet” Peptides
Naturally occurring glycopeptides (GPs, peptide + sugar) and glycoproteins are crucial players in many biological processes. N- and O-glycosylation is in fact one of the most important post-translational modifications in vivo. Glycoproteins are fundamental in cell-cell communications, recognition…
The Other Sanger Sequencing
Inspired by a recent celebration of the work of Martin and Synge, this article examines the role of chromatography in efforts to elucidate the primary structures of proteins. It touches on, as I have referred to it, ‘the other Sanger sequencing’ – the method by which the first protein…
Why protein chemist chose phosphorus for protein bioconjugation?
In the last two decades, phosphorus-mediated chemoselective ligation reactions acquired the “gold” status for in vivo labeling of biomolecules. However, some drawbacks of phosphines, such as directing non-canonical amino acids (e.g. azides) as their reaction partners limits the scope of these…
Conjugates of Vancomycin and Cell-penetrating Peptides – New Weapons in the Armoury against Drug Resistant Bacteria
Staying one step ahead in the arms race against antibiotic resistant pathogenic bacteria is an ongoing challenge to the ingenuity of medicinal chemists. Multidrug-resistance has become a menacing threat to the antibiotic armoury used by clinicians to treat nosocomial and community-acquired…
Bioactive peptides from food protein degradation: Legume peptides
Animal and plant proteins, upon in vitro or in vivo digestion, have not only a nutritional role but are a rich source of bioactive peptides initially encrypted in the native protein sequences. The activities of these peptides range from antioxidant, antihypertensive or anti-obesity to antimicrobial…
Nature’s Shotgun Proteomics
The mammalian immune system, as part of its response to a viral infection, does something akin to a shotgun proteomics experiment. Viral proteins are digested, and the resulting peptides are presented—as a mixture—in a form that can be recognised by circulating T cells. In this article, I…
Thanatin – an Insect-derived Antimicrobial Peptide Active against Pathogenic Gram-negative Bacteria
Swiss researchers have recently revealed the mechanism by which the insect-derived antimicrobial peptide thanatin targets the intermembrane protein complex required for lipopolysaccharide (LPS) transport in Escherichia coli. Employing a series of elegant techniques directed at increasing levels of…
Peptide vaccines: the future of immunotherapy?
It is widely accepted that vaccines are valuable preparations for prevention against life-threatening diseases such as polio, measles and smallpox and their utilization led to control and/or eradication of aforementioned infectious diseases. Common drawbacks in classical vaccine formulations led to…
Targeted protein degradation as a new paradigm in drug discovery. Is there a role for peptides?
Despite the large number of new, therapeutically relevant proteins discovered in recent years, classical drug discovery strategies have not been particularly successful in finding suitable small-molecule modulators. Targeted protein degradation has raised considerable interest from…
Small Proteins, Big Data
The possibility that a subset of biological molecules has been overlooked, and is waiting to be discovered, is always intriguing. For small proteins (proteins of around 100 amino acid residues or fewer) there is evidence to suggest that this is indeed the case. In this article, I examine the…
Inhibition of Amyloidogenesis by Synthetic Enantiomeric Peptides
A synthetic peptide composed of alternating L- and D-amino acid residues has been recently shown to inhibit aggregation and reduce toxic effects in neuroblastoma cells, of the beta-amyloid peptide, Aβ, implicated in Alzheimer’s disease. In contrast, a “twin” peptide with the same sequence,…
New enzymatic approaches for the generation of peptide and protein conjugates
Enzymatic conjugation of peptides and their analogues to other peptides or proteins is considered to be an exciting field in protein chemistry. Besides Sortase A, Butelase and Transglutaminase, the field offers attractive possibilities with respect to its broad spectrum and simplicity.…
Peptides as invaluable tools in the search for innovative analgesics
Pain is a quite frequent complaint after injuries and accompanying different pathologies, which remains poorly treated for a number of patients. Pain involves extremely complex/interrelated series of signaling and modulatory pathways of the nervous system. Within them, the contribution to pain…
Thiol additive-free native chemical ligation
Native chemical ligation (NCL) commonly facilitates a peptide thioester with an N-terminal β-thiol peptide to form a native amide bond. Though many peptide thioester preparation strategies have been developed, it generally requires a large excess of exogenous thiol additives. Here I will discuss…
