Summary

High potency, specificity and a good safety profile are the main strengths of bioactive peptides as new and promising therapies that may fill the gap between small molecules and protein drugs. These positive attributes of peptides, along with advances in drug delivery technologies, have contributed to a renewed interest in the discovery, optimization and development of peptides as pharmacological therapy. The entry collection aims to cover all aspects of peptide research in relation to health promotion.

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Entries
Topic Review
Pharmacodynamics of the Main Bioactive Peptides
Bioactive peptides (BPs) are a heterogeneous class of molecules found in a wide range of plant and animal sources. The first bioactive peptide was identified circa 1900 by Mellander, who isolated BPs from casein and demonstrated its ability to improve bone calcification in rachitic children. BPs can be defined as peptides between 2 and 20 amino acids able to modulate physiological functions. In general, BP consist of an inactive precursor molecule that becomes active after release of the active site by enzymatic or chemical hydrolysis in the gastrointestinal tract, thus allowing BP to be absorbed through specific peptide transporters. Thus, BP can be classified into exogenous and endogenous molecules, obtained via gastrointestinal digestion or artificially, respectively.
  • 804
  • 14 Dec 2022
Topic Review
Insulin/Insulin-like Growth Factor 1
Insulin (MW: 5.8 kDa) and insulin-like growth factor-1 (IGF1; also known as somatostatin C; MW: 7.65 kDa) are peptide hormones sharing significant structural homology with significant contributions to the regulation of whole-body metabolism and promotion of growth/cell renewal.
  • 407
  • 09 Dec 2022
Topic Review
Synthetic Hemorphin Analogs Containing Non-Natural Amino Acids
The endogenous hemorphins are bioactive peptides with activity on opioid receptors. Several research teams have synthesized, characterized, and pharmacologically evaluated synthetic hemorphin analogs containing unusual amino acids, D-amino acids, α-aminophosphonic acids, and their derivatives. Research focuses on the structure-activity relationship analysis, details on specific methods for their characterization, and the advantage of synthetic hemorphin analogs compared to endogenous peptides as potent biologically active compounds with a complex mechanism of action.
  • 679
  • 05 Dec 2022
Topic Review
Physical Exercise-Induced FGF-21 to Fight Obesity
Fibroblast growth factor 21 (FGF-21) is a protein that is involved in the regulation of glucose, lipids, and energy metabolism. To act on target tissues, endocrine FGF-21 binds preferably to FGF receptor 1 (FGFR1) in the presence of the coreceptor named β-klotho (KLB). Some of the effects of FGF-21 include increased fatty acid oxidation, glucose uptake, insulin sensitivity, and thermogenesis, which can regulate body weight and glycemia control. By exerting such metabolic effects, the therapeutic potential of FGF-21 for the treatment of obesity and diabetes has been investigated. Physical exercise has been widely used for the prevention and treatment of obesity. Several mechanisms mediate the effects of physical exercise, including the FGF-21 pathway. Studies have shown that physical exercise increases the concentration of circulating and tissue FGF-21 in animals, while contradictory results are still observed in humans.
  • 680
  • 29 Nov 2022
Topic Review
Plant- and Food-Derived Health-Beneficial Bioactive Peptides
Natural bioactives can be classified into micronutrients (i.e., vitamins and minerals); phytonutrients (e.g., phenolics, alkaloids, and terpenes); pre- and probiotics; and bioactive peptides. In particular, bioactive peptides have remained largely underappreciated as molecular deliverers of health promotion, mainly due to: (assumedly) poor bioavailability after oral consumption due to proteolysis along the gastrointestinal tract; limited transport from the gut lumen to the bloodstream; and, importantly, insufficient discovery and translation based on serendipitous research and/or high-throughput screening.
  • 503
  • 22 Nov 2022
Topic Review
TGFβ Signalling in Helminths
There has been little interaction between parasitologists and oncologists, some helminth infections predispose to the development of tumours. In addition, both parasites and tumours need to survive immune attack. The research suggests that both tumours and parasites suppress the immune response to increase their chances of survival. They both co-opt the transforming growth factor beta (TGFβ) signalling pathway to modulate the immune response to their benefit.
  • 465
  • 21 Nov 2022
Topic Review
Strategies for Improving Cell-Penetrating Peptides Stability and Delivery
Peptides play an important role in many fields, including immunology, medical diagnostics, and drug discovery, due to their high specificity and positive safety profile. However, for their delivery as active pharmaceutical ingredients, delivery vectors, or diagnostic imaging molecules, they suffer from two serious shortcomings: their poor metabolic stability and short half-life. Major research efforts are being invested to tackle those drawbacks, where structural modifications and novel delivery tactics have been developed to boost their ability to reach their targets as fully functional species.
  • 746
  • 04 Nov 2022
Topic Review
Research Trends on Exercise-Induced Muscle Damage
Exercise-induced muscle damage (EIMD) is a phenomenon that occurs following novel or unaccustomed exercise, particularly if the exercise includes a high number of eccentric contractions. The damage process is normally accompanied by a temporary decrease in muscle function (both muscle force and range of motion), increased swelling of the involved muscle group, increased circulation of muscle-specific proteins, and delayed-onset muscle soreness (DOMS). Most of the symptoms and signs of EIMD are present immediately after the initial exercise bout and persist for up to 14 days. 
  • 539
  • 03 Nov 2022
Topic Review
The Insulin-like Growth Factor System and Colorectal Cancer
Insulin-like growth factors (IGFs) are peptides which exert mitogenic, endocrine and cytokine activities. Together with their receptors, binding proteins and associated molecules, they participate in numerous pathophysiological processes, including cancer development. Colorectal cancer (CRC) is a disease with high incidence and mortality rates worldwide, whose etiology usually represents a combination of the environmental and genetic factors. IGFs are most often increased in CRC, enabling excessive autocrine/paracrine stimulation of the cell growth. Overexpression or increased activation/accessibility of IGF receptors is a coinciding step which transmits IGF-related signals. A number of molecules and biochemical mechanisms exert modulatory effects shaping the final outcome of the IGF-stimulated processes, frequently leading to neoplastic transformation in the case of irreparable disbalance.
  • 449
  • 24 Oct 2022
Topic Review
Sortilin/Neurotensin Receptor-3 in Cancer
The multifunctional role of sortilin in cancers development The development of cancerous tumors is known to be the consequence of the overexpression of growth factors. Unfortunately, when treated with radiotherapy or chemical therapy, some tumors can metastasize as a result of the weakening of cancer cell–cell interactions in the tumor tissue, leading to the dissemination of cancer cells in the circulation. Both mechanisms of cancer growth and metastasis are regulated by a large panel of circulating activators from several neuropeptides to membrane-bound factors released by matrix metalloprotease (MMP)-dependent shedding, such as Epidermal Growth Factor Receptor (EGFR) ligands. One of the most studied neuropeptides involved in cancer progression is neurotensin (NTS), the three known receptors of which (two G-protein coupled receptors, NTSR1 and NTSR2, and a type I receptor, NTSR3) are expressed in numerous cancers and particularly in digestive cancers. Interestingly, NTSR3, also previously identified as Sortilin, is shed from the plasma membrane, leading to the release of a soluble form of sortilin (sSortilin). However, growing evidence indicates the emerging role of membrane-bound Sortilin/NTSR3 and its soluble counterpart in cancer cell proliferation and dissemination.
  • 555
  • 21 Oct 2022
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