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Pharmaceuticals
Special Issues
New Applications and Developments in Synthetic Peptide Chemistry
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New Applications and Developments in Synthetic Peptide Chemistry

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Biopharmaceuticals".

Deadline for manuscript submissions: closed (30 May 2023) | Viewed by 30940

Printed Edition Available!
A printed edition of this Special Issue is available here.

Special Issue Editors

Dr. Giovanni N. Roviello

E-Mail Website
Guest Editor
Istituto di Biostrutture e Bioimmagini, Naples, Italy
Interests: peptide chemistry; solid phase synthesis; solution synthesis; nucleopeptides; PNA; nucleic acid chemistry; spectroscopic studies; SARS-CoV-2 and MERS-CoV coronaviruses; computational studies
Special Issues, Collections and Topics in MDPI journals
Dr. Rosanna Palumbo

E-Mail Website
Guest Editor
Istituto di Biostrutture e Bioimmagini, Naples, Italy
Interests: qualitative determination of peptides; toxicity screening; antioxidant properties; bioactive peptides; cell culture

Special Issue Information

Dear Colleagues,

Peptide-based therapeutics are of great relevance in biomedicine for the treatment of pathologies of enormous social impact, including cancer, neurodegeneration, and viral diseases, like the current COVID-19 pandemic. In this context, peptide inhibitors of SARS-CoV-2 enzymes are under investigation in the fight against the novel coronavirus. Peptides are able to interact with biomacromolecules involved in crucial biological pathways such as proteins and nucleic acids. Moreover, after functionalization by DNA nucleobases, they become powerful tools in DNA and RNA targeting, as testified by the scientific literature on peptide nucleic acids (PNAs) and nucleopeptides, with known diagnostic and therapeutic potential. Nonetheless, peptide analogues of a different nature are endowed with self-assembly properties at the origin of supramolecular assemblies and nanomaterials, which are attracting increasing attention in nanomedicine and biotechnology. In this Special Issue, we wish to focus on the novel experimental and theoretical approaches for peptide design and development, with particular attention being paid to the solid phase synthesis of natural peptides, PNA, nucleopeptides, peptoids and more general peptide analogs. However, contributions to the solution synthesis of amino acid monomers as building blocks for peptide chain elongation, as well as peptide-nucleic acid and peptide–protein interaction, peptide aggregation, nucleoamino acid and nucleopeptide chemistry, peptide–metal complexes and antimicrobial poly-amino acids are also welcome, as they could improve overall knowledge with regard to the amino acid-based chemistry at the interface between peptide design and pharmaceutical applications. Other themes of interest are inherent to the computational chemistry applied to peptide science.

This Special Issue is open to the submission of both original articles and reviews that describe research and ideas on themes treated in this issue for new applications and developments in synthetic peptide chemistry.

Dr. Giovanni N. Roviello
Dr. Rosanna Palumbo
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Peptides
  • Amyloid
  • Alzheimer’s disease
  • Parkinson’s disease
  • Neuropeptides
  • Peptide inhibitors
  • Antiviral peptides
  • Anti-COVID-19 peptides
  • Peptide aggregation
  • Polyamino acids
  • Synthetic antivirals
  • Anticancer peptides
  • Peptide synthesis
  • Peptoids
  • PNA
  • Nucleopeptides
  • Nucleoamino acids
  • Peptide supramolecular materials
  • Peptide–-metal complexes
  • Peptide characterization
  • Solid phase peptide synthesis

Published Papers (11 papers)

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Editorial

Jump to: Research, Review

3 pages, 443 KiB  
Editorial
Advances in Amino Acid-Based Chemistry
by Rosanna Palumbo, Hayarpi Simonyan and Giovanni N. Roviello
Pharmaceuticals 2023, 16(10), 1490; https://0-doi-org.brum.beds.ac.uk/10.3390/ph16101490 - 19 Oct 2023
Cited by 2 | Viewed by 1092
Abstract
Numerous applications of amino acid-based compounds and peptide derivatives in different biomedicine- and nanotechnology-related fields were described in the recent scientific literature [...] Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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Research

Jump to: Editorial, Review

23 pages, 5844 KiB  
Article
A Peptide Vaccine Design Targeting KIT Mutations in Acute Myeloid Leukemia
by Minji Kim, Kush Savsani and Sivanesan Dakshanamurthy
Pharmaceuticals 2023, 16(7), 932; https://0-doi-org.brum.beds.ac.uk/10.3390/ph16070932 - 27 Jun 2023
Cited by 2 | Viewed by 1724
Abstract
Acute myeloid leukemia (AML) is a leading blood cancer subtype that can be caused by 27 gene mutations. Previous studies have explored potential vaccine and drug treatments against AML, but many were proven immunologically insignificant. Here, we targeted this issue and applied various [...] Read more.
Acute myeloid leukemia (AML) is a leading blood cancer subtype that can be caused by 27 gene mutations. Previous studies have explored potential vaccine and drug treatments against AML, but many were proven immunologically insignificant. Here, we targeted this issue and applied various clinical filters to improve immune response. KIT is an oncogenic gene that can cause AML when mutated and is predicted to be a promising vaccine target because of its immunogenic responses when activated. We designed a multi-epitope vaccine targeting mutations in the KIT oncogene using CD8+ and CD4+ epitopes. We selected the most viable vaccine epitopes based on thresholds for percentile rank, immunogenicity, antigenicity, half-life, toxicity, IFNγ release, allergenicity, and stability. The efficacy of data was observed through world and regional population coverage of our vaccine design. Then, we obtained epitopes for optimized population coverage from PCOptim-CD, a modified version of our original Java-based program code PCOptim. Using 24 mutations on the KIT gene, 12 CD8+ epitopes and 21 CD4+ epitopes were obtained. The CD8+ dataset had a 98.55% world population coverage, while the CD4+ dataset had a 65.14% world population coverage. There were five CD4+ epitopes that overlapped with the top CD8+ epitopes. Strong binding to murine MHC molecules was found in four CD8+ and six CD4+ epitopes, demonstrating the feasibility of our results in preclinical murine vaccine trials. We then created three-dimensional (3D) models to visualize epitope–MHC complexes and TCR interactions. The final candidate is a non-toxic and non-allergenic multi-epitope vaccine against KIT mutations that cause AML. Further research would involve murine trials of the vaccine candidates on tumor cells causing AML. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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16 pages, 2770 KiB  
Article
Anti-Inflammatory Effects of Ang-(1-7) Bone-Targeting Conjugate in an Adjuvant-Induced Arthritis Rat Model
by Sana Khajeh pour, Arina Ranjit, Emma L. Summerill and Ali Aghazadeh-Habashi
Pharmaceuticals 2022, 15(9), 1157; https://0-doi-org.brum.beds.ac.uk/10.3390/ph15091157 - 17 Sep 2022
Cited by 3 | Viewed by 1685
Abstract
Rheumatoid arthritis (RA) is a chronic inflammatory condition of synovial joints that causes disability and systemic complications. Ang-(1-7), one of the main peptides in the renin-angiotensin (Ang) system (RAS), imposes its protective effects through Mas receptor (MasR) signaling. It has a short half-life, [...] Read more.
Rheumatoid arthritis (RA) is a chronic inflammatory condition of synovial joints that causes disability and systemic complications. Ang-(1-7), one of the main peptides in the renin-angiotensin (Ang) system (RAS), imposes its protective effects through Mas receptor (MasR) signaling. It has a short half-life, limiting its feasibility as a therapeutic agent. In this study, we evaluated the anti-inflammatory effects of Ang-(1-7)’s novel and stable conjugate (Ang. Conj.) by utilizing its affinity for bone through bisphosphonate (BP) moiety in an adjuvant-induced arthritis (AIA) rat model. The rats received subcutaneous injections of vehicle, plain Ang-(1-7), or an equivalent dose of Ang. Conj. The rats’ body weights, paws, and joints’ diameters were measured thrice weekly. After 14 days, the rats were euthanized, and the blood and tissue samples were harvested for further analysis of nitric oxide (NO) and RAS components’ gene and protein expression. The administration of Ang. Conj. reduced body weight loss, joint edema, and serum NO. Moreover, the Ang. Conj. treatment significantly reduced the classical arm components at peptide, enzyme, and receptor levels while augmenting them for the protective arm. The results of this study introduce a novel class of bone-targeting natural peptides for RA caused by an inflammation-induced imbalance in the activated RAS. Our results indicate that extending the half-life of Ang-(1-7) augments the RAS protective arm and exerts enhanced therapeutic effects in the AIA model in rats. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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19 pages, 5862 KiB  
Article
Synthesis, Neuroprotective Effect and Physicochemical Studies of Novel Peptide and Nootropic Analogues of Alzheimer Disease Drug
by Radoslav Chayrov, Tatyana Volkova, German Perlovich, Li Zeng, Zhuorong Li, Martin Štícha, Rui Liu and Ivanka Stankova
Pharmaceuticals 2022, 15(9), 1108; https://0-doi-org.brum.beds.ac.uk/10.3390/ph15091108 - 05 Sep 2022
Cited by 2 | Viewed by 2235
Abstract
Glutamate is an excitatory neurotransmitter in the nervous system. Excessive glutamate transmission can lead to increased calcium ion expression, related to increased neurotoxicity. Memantine is used for treating patients with Alzheimer’s disease (AD) due to its protective action on the neurons against toxicity [...] Read more.
Glutamate is an excitatory neurotransmitter in the nervous system. Excessive glutamate transmission can lead to increased calcium ion expression, related to increased neurotoxicity. Memantine is used for treating patients with Alzheimer’s disease (AD) due to its protective action on the neurons against toxicity caused by over activation of N-methyl-D-aspartate receptors. Nootropics, also called “smart drugs”, are used for the treatment of cognitive deficits. In this work, we evaluate the neuroprotective action of four memantine analogues of glycine derivatives, including glycyl-glycine, glycyl-glycyl-glycine, sarcosine, dimethylglycine and three conjugates with nootropics, modafinil, piracetam and picamilon. The new structural memantine derivatives improved cell viability against copper-induced neurotoxicity in APPswe cells and glutamate-induced neurotoxicity in SH-SY5Y cells. Among these novel compounds, modafinil-memantine, piracetam-memantine, sarcosine-memantine, dimethylglycine-memantine, and glycyl-glycine-memantine were demonstrated with good EC50 values of the protective effects on APPswe cells, accompanied with moderate amelioration from glutamate-induced neurotoxicity. In conclusion, our study demonstrated that novel structural derivatives of memantine might have the potential to develop promising lead compounds for the treatment of AD. The solubility of memantine analogues with nootropics and memantine analogues with glycine derivatives in buffer solutions at pH 2.0 and pH 7.4 simulating the biological media at 298.15 K was determined and the mutual influence of the structural fragments in the molecules on the solubility behavior was analyzed. The significative correlation equations relating the solubility and biological properties with the structural HYBOT (Hydrogen Bond Thermodynamics) descriptors were derived. These equations would greatly simplify the task of the directed design of the memantine analogues with improved solubility and enhanced bioavailability. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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20 pages, 2772 KiB  
Article
Cu and Zn Interactions with Peptides Revealed by High-Resolution Mass Spectrometry
by Monica Iavorschi, Ancuța-Veronica Lupăescu, Laura Darie-Ion, Maria Indeykina, Gabriela Elena Hitruc and Brîndușa Alina Petre
Pharmaceuticals 2022, 15(9), 1096; https://0-doi-org.brum.beds.ac.uk/10.3390/ph15091096 - 31 Aug 2022
Cited by 2 | Viewed by 2824
Abstract
Alzheimer’s disease (AD) is a progressive neurodegenerative disease characterized by abnormal extracellular amyloid-beta (Aβ) peptide depositions in the brain. Among amorphous aggregates, altered metal homeostasis is considered a common risk factor for neurodegeneration known to accelerate plaque formation. Recently, peptide-based drugs capable of [...] Read more.
Alzheimer’s disease (AD) is a progressive neurodegenerative disease characterized by abnormal extracellular amyloid-beta (Aβ) peptide depositions in the brain. Among amorphous aggregates, altered metal homeostasis is considered a common risk factor for neurodegeneration known to accelerate plaque formation. Recently, peptide-based drugs capable of inhibiting amyloid aggregation have achieved unprecedented scientific and pharmaceutical interest. In response to metal ions binding to Aβ peptide, metal chelation was also proposed as a therapy in AD. The present study analyzes the interactions formed between NAP octapeptide, derived from activity-dependent neuroprotective protein (ADNP), amyloid Aβ(9–16) fragment and divalent metal ions such as Cu and Zn. The binding affinity studies for Cu and Zn ions of synthetic NAP peptide and Aβ(9–16) fragment were investigated by matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS), electrospray ion trap mass spectrometry (ESI-MS) and atomic force microscopy (AFM). Both mass spectrometric methods confirmed the formation of metal–peptide complexes while the AFM technique provided morphological and topographic information regarding the influence of metal ions upon peptide crystallization. Our findings showed that due to a rich histidine center, the Aβ(9–16) fragment is capable of binding metal ions, thus becoming stiff and promoting aggregation of the entire amyloid peptide. Apart from this, the protective effect of the NAP peptide was found to rely on the ability of this octapeptide to generate both chelating properties with metals and interactions with Aβ peptide, thus stopping its folding process. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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21 pages, 6907 KiB  
Article
C16 Peptide and Ang-1 Improve Functional Disability and Pathological Changes in an Alzheimer’s Disease Model Associated with Vascular Dysfunction
by Xiaoxiao Fu, Jing Wang, Huaying Cai, Hong Jiang and Shu Han
Pharmaceuticals 2022, 15(4), 471; https://0-doi-org.brum.beds.ac.uk/10.3390/ph15040471 - 13 Apr 2022
Cited by 1 | Viewed by 2108
Abstract
Alzheimer’s disease (AD) is a neurological disorder characterized by neuronal cell death, tau pathology, and excessive inflammatory responses. Several vascular risk factors contribute to damage of the blood–brain barrier (BBB), secondary leak-out of blood vessels, and infiltration of inflammatory cells, which aggravate the [...] Read more.
Alzheimer’s disease (AD) is a neurological disorder characterized by neuronal cell death, tau pathology, and excessive inflammatory responses. Several vascular risk factors contribute to damage of the blood–brain barrier (BBB), secondary leak-out of blood vessels, and infiltration of inflammatory cells, which aggravate the functional disability and pathological changes in AD. Growth factor angiopoietin-1 (Ang-1) can stabilize the endothelium and reduce endothelial permeability by binding to receptor tyrosine kinase 2 (Tie2). C16 peptide (KAFDITYVRLKF) selectively binds to integrin ανβ3 and competitively inhibits leukocyte transmigration into the central nervous system by interfering with leukocyte ligands. In the present study, 45 male Sprague-Dawley (SD) rats were randomly divided into three groups: vehicle group, C16 peptide + Ang1 (C + A) group, and sham control group. The vehicle and C + A groups were subjected to two-vessel occlusion (2-VO) with artery ligation followed by Aβ1-42 injection into the hippocampus. The sham control group underwent sham surgery and injection with an equal amount of phosphate-buffered saline (PBS) instead of Aβ1-42. The C + A group was administered 1 mL of drug containing 2 mg of C16 and 400 µg of Ang-1 daily for 2 weeks. The sham control and vehicle groups were administered 1 mL of PBS for 2 weeks. Our results showed that treatment with Ang-1 plus C16 improved functional disability and reduced neuronal death by inhibiting inflammatory cell infiltration, protecting vascular endothelial cells, and maintaining BBB permeability. The results suggest that these compounds may be potential therapeutic agents for AD and warrant further investigation. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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15 pages, 3132 KiB  
Article
Structure-Activity Relationship Investigations of Novel Constrained Chimeric Peptidomimetics of SOCS3 Protein Targeting JAK2
by Sara La Manna, Marilisa Leone, Flavia Anna Mercurio, Daniele Florio and Daniela Marasco
Pharmaceuticals 2022, 15(4), 458; https://0-doi-org.brum.beds.ac.uk/10.3390/ph15040458 - 09 Apr 2022
Cited by 1 | Viewed by 1812
Abstract
SOCS3 (suppressor of cytokine signaling 3) protein suppresses cytokine-induced inflammation and its deletion in neurons or immune cells increases the pathological growth of blood vessels. Recently, we designed several SOCS3 peptidomimetics by assuming as template structures the interfacing regions of the ternary complex [...] Read more.
SOCS3 (suppressor of cytokine signaling 3) protein suppresses cytokine-induced inflammation and its deletion in neurons or immune cells increases the pathological growth of blood vessels. Recently, we designed several SOCS3 peptidomimetics by assuming as template structures the interfacing regions of the ternary complex constituted by SOCS3, JAK2 (Janus Kinase 2) and gp130 (glycoprotein 130) proteins. A chimeric peptide named KIRCONG chim, including non-contiguous regions demonstrated able to bind to JAK2 and anti-inflammatory and antioxidant properties in VSMCs (vascular smooth muscle cells). With the aim to improve drug-like features of KIRCONG, herein we reported novel cyclic analogues bearing different linkages. In detail, in two of them hydrocarbon cycles of different lengths were inserted at positions i/i+5 and i/i+7 to improve helical conformations of mimetics. Structural features of cyclic compounds were investigated by CD (Circular Dichroism) and NMR (Nuclear Magnetic Resonance) spectroscopies while their ability to bind to catalytic domain of JAK2 was assessed through MST (MicroScale Thermophoresis) assay as well as their stability in biological serum. Overall data indicate a crucial role exerted by the length and the position of the cycle within the chimeric structure and could pave the way to the miniaturization of SOCS3 protein for therapeutic aims. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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Review

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26 pages, 2099 KiB  
Review
Peptide-Based Vaccine against Breast Cancer: Recent Advances and Prospects
by Muhammad Luqman Nordin, Ahmad Khusairi Azemi, Abu Hassan Nordin, Walid Nabgan, Pei Yuen Ng, Khatijah Yusoff, Nadiah Abu, Kue Peng Lim, Zainul Amiruddin Zakaria, Noraznawati Ismail and Fazren Azmi
Pharmaceuticals 2023, 16(7), 923; https://0-doi-org.brum.beds.ac.uk/10.3390/ph16070923 - 25 Jun 2023
Cited by 1 | Viewed by 1908
Abstract
Breast cancer is considered the second-leading cancer after lung cancer and is the most prevalent cancer among women globally. Currently, cancer immunotherapy via vaccine has gained great attention due to specific and targeted immune cell activity that creates a potent immune response, thus [...] Read more.
Breast cancer is considered the second-leading cancer after lung cancer and is the most prevalent cancer among women globally. Currently, cancer immunotherapy via vaccine has gained great attention due to specific and targeted immune cell activity that creates a potent immune response, thus providing long-lasting protection against the disease. Despite peptides being very susceptible to enzymatic degradation and poor immunogenicity, they can be easily customized with selected epitopes to induce a specific immune response and particulate with carriers to improve their delivery and thus overcome their weaknesses. With advances in nanotechnology, the peptide-based vaccine could incorporate other components, thereby modulating the immune system response against breast cancer. Considering that peptide-based vaccines seem to show remarkably promising outcomes against cancer, this review focuses on and provides a specific view of peptide-based vaccines used against breast cancer. Here, we discuss the benefits associated with a peptide-based vaccine, which can be a mainstay in the prevention and recurrence of breast cancer. Additionally, we also report the results of recent trials as well as plausible prospects for nanotechnology against breast cancer. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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16 pages, 1633 KiB  
Review
Willardiine and Its Synthetic Analogues: Biological Aspects and Implications in Peptide Chemistry of This Nucleobase Amino Acid
by Rosanna Palumbo, Daniela Omodei, Caterina Vicidomini and Giovanni N. Roviello
Pharmaceuticals 2022, 15(10), 1243; https://0-doi-org.brum.beds.ac.uk/10.3390/ph15101243 - 10 Oct 2022
Cited by 4 | Viewed by 1723
Abstract
Willardiine is a nonprotein amino acid containing uracil, and thus classified as nucleobase amino acid or nucleoamino acid, that together with isowillardiine forms the family of uracilylalanines isolated more than six decades ago in higher plants. Willardiine acts as a partial agonist of [...] Read more.
Willardiine is a nonprotein amino acid containing uracil, and thus classified as nucleobase amino acid or nucleoamino acid, that together with isowillardiine forms the family of uracilylalanines isolated more than six decades ago in higher plants. Willardiine acts as a partial agonist of ionotropic glutamate receptors and more in particular it agonizes the non-N-methyl-D-aspartate (non-NMDA) receptors of L-glutamate: ie. the α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) and kainate receptors. Several analogues and derivatives of willardiine have been synthesised in the laboratory in the last decades and these compounds show different binding affinities for the non-NMDA receptors. More in detail, the willardiine analogues have been employed not only in the investigation of the structure of AMPA and kainate receptors, but also to evaluate the effects of receptor activation in the various brain regions. Remarkably, there are a number of neurological diseases determined by alterations in glutamate signaling, and thus, ligands for AMPA and kainate receptors deserve attention as potential neurodrugs. In fact, similar to willardiine its analogues often act as agonists of AMPA and kainate receptors. A particular importance should be recognized to willardiine and its thymine-based analogue AlaT also in the peptide chemistry field. In fact, besides the naturally-occurring short nucleopeptides isolated from plant sources, there are different examples in which this class of nucleoamino acids was investigated for nucleopeptide development. The applications are various ranging from the realization of nucleopeptide/DNA chimeras for diagnostic applications, and nucleoamino acid derivatization of proteins for facilitating protein-nucleic acid interaction, to nucleopeptide-nucleopeptide molecular recognition for nanotechnological applications. All the above aspects on both chemistry and biotechnological applications of willardine/willardine-analogues and nucleopeptide will be reviewed in this work. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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14 pages, 3853 KiB  
Review
Fmoc-Diphenylalanine Hydrogels: Optimization of Preparation Methods and Structural Insights
by Carlo Diaferia, Elisabetta Rosa, Giancarlo Morelli and Antonella Accardo
Pharmaceuticals 2022, 15(9), 1048; https://0-doi-org.brum.beds.ac.uk/10.3390/ph15091048 - 25 Aug 2022
Cited by 17 | Viewed by 2842
Abstract
Hydrogels (HGs) are tri-dimensional materials with a non-Newtonian flow behaviour formed by networks able to encapsulate high amounts of water or other biological fluids. They can be prepared using both synthetic or natural polymers and their mechanical and functional properties may change according [...] Read more.
Hydrogels (HGs) are tri-dimensional materials with a non-Newtonian flow behaviour formed by networks able to encapsulate high amounts of water or other biological fluids. They can be prepared using both synthetic or natural polymers and their mechanical and functional properties may change according to the preparation method, the solvent, the pH, and to others experimental parameters. Recently, many short and ultra-short peptides have been investigated as building blocks for the formulation of biocompatible hydrogels suitable for different biomedical applications. Due to its simplicity and capability to gel in physiological conditions, Fmoc-FF dipeptide is one of the most studied peptide hydrogelators. Although its identification dates to 15 ago, its behaviour is currently studied because of the observation that the final material obtained is deeply dependent on the preparation method. To collect information about their formulation, here are reported some different strategies adopted until now for the Fmoc-FF HG preparation, noting the changes in the structural arrangement and behaviour in terms of stiffness, matrix porosity, and stability induced by the different formulation strategy on the final material. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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22 pages, 2024 KiB  
Review
Usage of Synthetic Peptides in Cosmetics for Sensitive Skin
by Diana I. S. P. Resende, Marta Salvador Ferreira, José Manuel Sousa-Lobo, Emília Sousa and Isabel Filipa Almeida
Pharmaceuticals 2021, 14(8), 702; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14080702 - 21 Jul 2021
Cited by 10 | Viewed by 9318
Abstract
Sensitive skin is characterized by symptoms of discomfort when exposed to environmental factors. Peptides are used in cosmetics for sensitive skin and stand out as active ingredients for their ability to interact with skin cells by multiple mechanisms, high potency at low dosage [...] Read more.
Sensitive skin is characterized by symptoms of discomfort when exposed to environmental factors. Peptides are used in cosmetics for sensitive skin and stand out as active ingredients for their ability to interact with skin cells by multiple mechanisms, high potency at low dosage and the ability to penetrate the stratum corneum. This study aimed to analyze the composition of 88 facial cosmetics for sensitive skin from multinational brands regarding usage of peptides, reviewing their synthetic pathways and the scientific evidence that supports their efficacy. Peptides were found in 17% of the products analyzed, namely: acetyl dipeptide-1 cetyl ester, palmitoyl tripeptide-8, acetyl tetrapeptide-15, palmitoyl tripeptide-5, acetyl hexapeptide-49, palmitoyl tetrapeptide-7 and palmitoyl oligopeptide. Three out of seven peptides have a neurotransmitter-inhibiting mechanism of action, while another three are signal peptides. Only five peptides present evidence supporting their use in sensitive skin, with only one clinical study including volunteers having this condition. Noteworthy, the available data is mostly found in patents and supplier brochures, and not in randomized placebo-controlled studies. Peptides are useful active ingredients in cosmetics for sensitive skin. Knowing their efficacy and synthetic pathways provides meaningful insight for the development of new and more effective ingredients. Full article
(This article belongs to the Special Issue New Applications and Developments in Synthetic Peptide Chemistry)
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