New Advances in Short Peptides: Looking Forward

Apostolopoulos, Vasso; Bojarska, Joanna; Chai, Tsun-Thai; Feehan, Jack; Kaczmarek, Krzysztof; Matsoukas, John; Paredes‐López, Octavio; Skwarczynski, Mariusz; Smith‐Carpenter, Jillian E.; Venanzi, Mariano; Wolf, Wojciech M.; Zielenkiewicz, Piotr; Ziora, Zyta M.

doi:10.3390/molecules27113635

Cited by 9 publications

(6 citation statements)

References 33 publications

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“…Further, in a phase 2 human clinical study with tirzepatide in conjunction with regulated nutrition and lifestyle with or without metformin, a dose-dependent impact on HbA1c and weight loss was observed, which was larger than that of the selective GLP-1 RA dulaglutide. Meanwhile, in a 12-week phase 2 trial with moderate dose-escalation regimens, gastrointestinal tolerability improved when starting with a lower dose and slowly increasing to the highest effective doses [55][56][57]. Mechanism of action of trizepatide is presented in Figure 4.…”

Section: Clinical Developmentmentioning

confidence: 99%

Tirzepatide, a New Era of Dual-Targeted Treatment for Diabetes and Obesity: A Mini-Review

Chavda¹,

Ajabiya

Teli

et al. 2022

Molecules

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The prevalence of obesity and diabetes is an increasing global problem, especially in developed countries, and is referred to as the twin epidemics. As such, advanced treatment approaches are needed. Tirzepatide, known as a ‘twincretin’, is a ‘first-in-class’ and the only dual glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) receptor agonist, that can significantly reduce glycemic levels and improve insulin sensitivity, as well as reducing body weight by more than 20% and improving lipid metabolism. This novel anti-diabetic drug is a synthetic peptide analog of the human GIP hormone with a C20 fatty-diacid portion attached which, via acylation technology, can bind to albumin in order to provide a dose of the drug, by means of subcutaneous injection, once a week, which is appropriate to its a half-life of about five days. Tirzepatide, developed by Eli Lilly, was approved, under the brand name Mounjaro, by the United States Food and Drug Administration in May 2022. This started the ‘twincretin’ era of enormously important and appealing dual therapeutic options for diabetes and obesity, as well as advanced management of closely related cardiometabolic settings, which constitute the leading cause of morbidity, disability, and mortality worldwide. Herein, we present the key characteristics of tirzepatide in terms of synthesis, structure, and activity, bearing in mind its advantages and shortcomings. Furthermore, we briefly trace the evolution of this kind of medical agent and discuss the development of clinical studies.

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Section: Clinical Developmentmentioning

confidence: 99%

Tirzepatide, a New Era of Dual-Targeted Treatment for Diabetes and Obesity: A Mini-Review

Chavda¹,

Ajabiya

Teli

et al. 2022

Molecules

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“…Research suggests that insects' proteins, after enzymatic proteolysis, may be a good source of bioactive peptides [5]. The positive impact of bioactive peptides on body functions and, thus, on human health is well acknowledged [25]. Indeed, bioactive peptides exert antioxidant, anticancer, antithrombotic, antihypertensive, antiobesity, anti-inflammatory, opioid, mineral binding, immunomodulatory, antiaging, and antimicrobial effects, with high organ specificity and low toxicity [26].…”

Section: Edible Insects and Human Healthmentioning

confidence: 99%

Bioactive Peptides Derived from Edible Insects: Effects on Human Health and Possible Applications in Dentistry

Ferrazzano,

D’Ambrosio,

Caruso

et al. 2023

Nutrients

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Novel foods, including edible insects, are emerging because of their nutritional characteristics and low environmental impacts and could represent a valid alternative source of food in a more sustainable way. Edible insects have been shown to have beneficial effects on human health. Insect-derived bioactive peptides exert antihypertensive, antioxidant, anti-inflammatory, and antimicrobial properties and have protective effects against common metabolic conditions. In this review, the roles of edible insects in human health are reported, and the possible applications of these peptides in clinical practice are discussed. A special mention is given to the role of antimicrobial peptides and their potential applications in controlling infections in orthodontic procedures. In this context, insects’ antimicrobial peptides might represent a potential tool to face the onset of infective endocarditis, with a low chance to develop resistances, and could be manipulated and optimized to replace common antibiotics used in clinical practice so far. Although some safety concerns must be taken into consideration, and the isolation and production of insect-derived proteins are far from easy, edible insects represent an interesting source of peptides, with beneficial effects that may be, in the future, integrated into clinical and orthodontic practice.

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“…Bioactive peptides may have a positive impact on body functions and thus benefit human health [ 1 , 2 ]. New information reporting their beneficial effects on the health of livestock and plants is also emerging.…”

Section: Introductionmentioning

confidence: 99%

Bioactive Peptide Discovery from Edible Insects for Potential Applications in Human Health and Agriculture

et al. 2023

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In the past decade, there has been fast-growing interest among researchers to discover bioactive peptides from edible insects and to evaluate their potential applications in the management of human, livestock, and plant health. This review summarizes current knowledge of insect-derived peptides and their potential role in tackling human health issues and solving agriculture problems by protecting crops and livestock against their pathogens. Numerous bioactive peptides have been identified from edible insect species, including peptides that were enzymatically liberated from insect proteins and endogenous peptides that occur naturally in insects. The peptides exhibited diverse bioactivities, encompassing antioxidant, anti-angiotensin-converting enzyme, anti-dipeptidyl peptidase-IV, anti-glucosidase, anti-lipase, anti-lipoxygenase, anti-cyclooxygenase, anti-obesity, and hepatoprotective activities. Such findings point to their potential contribution to solving human health problems related to inflammation, free radical damage, diabetes, hypertension, and liver damage, among others. Although most of the experiments were performed in vitro, evidence for the in vivo efficacy of some peptides is emerging. Evidence of the protective effects of insect-derived endogenous antimicrobial peptides in combating farm animal and plant pathogens is available. The ability of insect-derived endogenous neuropeptides to protect plants against herbivorous insects has been demonstrated as well. Nevertheless, the potency of peptides identified from insect protein hydrolysates in modulating livestock and plant health remains a knowledge gap to be filled.

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New Advances in Short Peptides: Looking Forward

Abstract: It is beyond doubt that short peptides hold significant promise in bio-medicine, as the most versatile molecules, both structurally and functionally [...]

Cited by 9 publications

References 33 publications

Tirzepatide, a New Era of Dual-Targeted Treatment for Diabetes and Obesity: A Mini-Review

Tirzepatide, a New Era of Dual-Targeted Treatment for Diabetes and Obesity: A Mini-Review

Bioactive Peptides Derived from Edible Insects: Effects on Human Health and Possible Applications in Dentistry

Bioactive Peptide Discovery from Edible Insects for Potential Applications in Human Health and Agriculture

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