New Issue :: Current Protein & Peptide Science 19, Issue 8

Current Protein & Peptide Science publishes review articles on specific aspects involving proteins, peptides, and interactions between the enzymes, the binding interactions of hormones and their receptors; the properties of transcription factors and other molecules that regulate gene expression; the reactions leading to the immune response; the process of signal transduction; the structure and function of proteins involved in the cytoskeleton and molecular motors; the properties of membrane channels and transporters; and the generation and storage of metabolic energy. In addition, reviews of experimental studies of protein folding and design are given special emphasis. Manuscripts submitted to Current Protein and Peptide Science should cover a field by discussing research from the leading laboratories in a field and should pose questions for future studies. Original papers, research articles and letter articles/short communications are not considered for publication in Current Protein & Peptide Science.

Articles from the journal Current Protein & Peptide Science Volume 19, Issue 8:

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EDITOR’S CHOICE – Inhibitory Effects of 1,4-disubstituted Thiosemicarbazide Derivatives on Streptococcus mutans and Streptococcus sanguinis Mono-species Biofilms

Journal: Letters in Drug Design & Discovery

Author(s): Malgorzata Miazga-Karska, Maciej Wos, Agnieszka A. Kaczor, Anna Pachuta-Stec, Grazyna Ginalska, Monika Pitucha*

Graphical Abstract:



Background: Bacterial biofilms are a cause of a number of infections and are associated with specific drug resistance. In particular, dental biofilm can consist of up to 100 bacterial species and may result in the diseases in the teeth and the surrounding tissues, including dental caries and periodontal diseases. Moreover, pathogens from the dental biofilm can migrate to other organs and lead to systemic diseases. Thus, it is important to search for inhibitors of dental biofilm formation. The series of 1,4-disubstitued thiosemicarbazide derivatives were evaluated for their ability to inhibit mono-species Streptococcus mutans or Streptococcus sanguinis biofilm formation.

Methods: The Minimum Biofilm Inhibitory Concentration (MBIC) is defined as the lowest concentration of an antimicrobial agent required to inhibit the formation of biofilm. MBIC was determined spectrophotometrically. Molecular docking was performed using Glide from the Schrödinger suite of software. The grid file was generated indicating acarbose as a reference ligand. The compounds were modeled using LigPrep protocol from the Schrödinger suite of software. Molecular docking was performed using the SP (standard precision) protocol of Glide. Molecular dynamics studies of ligand-receptor complexes was performed using Desmond v.

Results: The series of 1,4-disubstituted thiosemicarbazide derivatives were synthesized and investigated for their ability to inhibit S. mutans or S. sanguinis biofilm. The most active compounds caused inhibition of S. sanguinis and S. mutans biofilm formation in the concentration of 7.81 µg/ml- 62.5 µg/ml. We showed, that growth of S. mutans and S. sanguinis biofilm was faster and higher in presence of sucrose. Additionally it was harder to inhibit the growth of biofilm in BHIbroth with the presence of sucrose, than the biofilm growing in BHI without sucrose. It seems that colonization by tested caries bacteria depends on sucrose content in medium. Based on above in vitro anti-biofilm data, we postulated that the mechanism of antibacterial activity of the investigated compounds might be connected with the inhibition of mono-species bacteria biofilm formation. In order to demonstrate that the investigated compounds may inhibit the enzyme glucansucrase and thus, biofilm formation, we performed molecular docking and molecular dynamics of the studied compounds to glucansucrase crystal structure. The obtained results reveal that the thiosemicarbazide derivatives can be used as potential inhibitors of dental biofilm formation, acting possibly through inhibition of glucansucrase.

Conclusion: In this study we showed that some of tested thiosemicarbazide derivatives can be used as potential inhibitors for mono-species cultures of S. mutans or S. sanguinis biofilm. The possible blocking mechanism of mono-species biofilm formation was proposed via molecular modelling technique. The data suggested that this mechanism may involve the glucansucrase inhibition as it was demonstrated that tested derivatives occupy the same binding pocket in this enzyme as acarbose, commonly known inhibitor of glucosylotransferases. Therefore, it is possible that tested derivatives could be used in prevention of dental caries.

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EDITOR’S CHOICE – Cytomegalovirus Infection: The Neurodevelopmental Peptide Signatures

Journal: Current Drug Discovery Technologies

Author(s): Guglielmo Lucchese, Darja Kanduc*

Graphical Abstract:



Background and Objective: HCMV infection may cause neurodevelopmental disorders, including intellectual disability, hearing loss, cortical malformations, and calcifications. Theorizing about the still unknown molecular basis of HCMV-related diseases, this study analyzes the peptide sharing between HCMV, strains AD169 and Merlin, and human proteins, searching for shared sequences that might lead to crossreactive autoimmune injuries in the brain during immune responses following HCMV infection.

Method: HCMV proteins were analyzed for peptides shared with the human proteome using the Pir Peptide Match resource.

Result: Numerous HCMV peptides (ranging from 9 to 13 mer in length) are disseminated through hundreds of human proteins. The peptide sharing mostly involves crucial neurodevelopmental antigens such as PITX3, implicated in the differentiation of meso-diencephalic dopaminergic neurons; SIX3, which controls proper anterioposterior patterning of the diencephalon and formation of the rostral diencephalon during forebrain development; and ZIC2, which plays a fundamental role in the early stage of organogenesis of the central nervous system.

Conclusion: This study describes a HCMV vs human peptide overlap that may represent a crossreactive platform linking the pathologic sequelae of HCMV infection to the immune anti-HCMV response. The data could inform development of effective and safe immune therapeutic/preventive approaches against HCMV infections.

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EDITOR’S CHOICE – N-3 (Omega-3) Fatty Acids: Effects on Brain Dopamine Systems and Potential Role in the Etiology and Treatment of Neuropsychiatric Disorders

Journal: CNS & Neurological Disorders – Drug Targets

Author(s): Michelle Healy-Stoffel, Beth Levant

Graphical Abstract:



Background & Objective: A number of neuropsychiatric disorders, including Parkinson’s disease, schizophrenia, attention deficit hyperactivity disorder, and, to some extent, depression, involve dysregulation of the brain dopamine systems. The etiology of these diseases is multifactorial, involving genetic and environmental factors. Evidence suggests that inadequate levels of n-3 (omega- 3) polyunsaturated fatty acids (PUFA) in the brain may represent a risk factor for these disorders. These fatty acids, which are derived from the diet, are a major component of neuronal membranes and are of particular importance in brain development and function. Low levels of n-3 PUFAs in the brain affect the brain dopamine systems and, when combined with appropriate genetic and other factors, increase the risk of developing these disorders and/or the severity of the disease. This article reviews the neurobiology of n-3 PUFAs and their effects on dopaminergic function.

Conclusion: Clinical studies supporting their role in the etiologies of diseases involving the brain dopamine systems and the potential of n-3 PUFAs in the treatment of these disorders are discussed.

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OPEN ACCESS ARTICLE – Hyperglycemic Hyperosmolar State

Journal: Current Diabetes Reviews

Author(s): Marco Baldrighi, Pier Paolo Sainaghi, Mattia Bellan, Ettore Bartoli, Luigi Mario Castello*


Introduction: Although hypovolemia remains the most relevant problem during acute decompensated diabetes in its clinical manifestations (diabetic ketoacidosis, DKA, and hyperglycemic hyperosmolar state, HHS), the electrolyte derangements caused by the global hydroelectrolytic imbalance usually complicate the clinical picture at presentation and may be worsened by the treatment itself.

Aim: This review article is focused on the management of dysnatremias during hyperglycemic hyperosmolar state with the aim of providing clinicians a useful tool to early identify the sodium derangement in order to address properly its treatment.

Discussion: The plasma sodium concentration is modified by most of the therapeutic measures commonly required in such patients and the physician needs to consider these interactions when treating HHS. Moreover, an improper management of plasma sodium concentration (PNa+) and plasma osmolality during treatment has been associated with two rare potentially life-threatening complications (cerebral edema and osmotic demyelination syndrome). Identifying the correct composition of the fluids that need to be infused to restore volume losses is crucial to prevent complications.

Conclusion: A quantitative approach based on the comparison between the measured PNa+ (PNa+M) and the PNa+ expected in the presence of an exclusive water shift (PNa+G) may provide more thorough information about the true hydroelectrolytic status of the patient and may therefore, guide the physician in the initial management of HHS. On the basis of data derived from our previous studies, we propose a 7-step algorithm to compute an accurate estimate of PNa+G.

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New Issue :: Current Medicinal Chemistry Volume 25, Issue 20

Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews and guest edited thematic issues written by leaders in the field covering a range of the current topics in medicinal chemistry. The journal also publishes reviews on recent patents. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

Articles from the journal Medicinal Chemistry Volume 25, Issue 20:

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EDITOR’S CHOICE – Regulation of the Unfolded Protein Response in Disease

Journal: Current Immunology Reviews

Author(s): Samuel Lara-Reyna, Thomas Scambler, Jonathan Holbrook, Heledd H. Jarosz-Griffiths, Daniel Peckham, Michael F. McDermott

Graphical Abstract:



Background: The Unfolded Protein Response (UPR) is a well conserved mechanism that mammalian cells use to cope with stress and infections. This mechanism is exquisitely regulated at several levels, including post-transcriptional modifications by microRNAs. These small non-coding RNAs are mainly involved in the degradation of mRNA, thereby blocking protein translation. The finely balanced interplay between the UPR and microRNAs is altered in several disorders, contributing to both disease aetiology and pathology.

Methods: We review and explore alterations in the UPR and microRNAs in several inflammatory conditions, including bone, lung, and neurodegenerative diseases. We also evaluate the impact of these alterations on the disruption of cellular homeostasis and suggest possible therapeutic options to restore this balance.

Results: Several components of the UPR, including IRE1, ATF6, and PERK, are clearly dysregulated in inflammatory bone, lung, and neurodegenerative diseases, contributing to the inflammatory process in these disorders. XBP1s, which is downstream of IRE1, is shown to be dysregulated in several diseases, and significantly contributes to the inflammatory process. MicroRNAs show unique dysregulated signatures in each individual tissue and disorder, suggesting that these small transcripts may regulate different pathways in a cell-dependent manner. Finally, there are functional connections between these dysregulated microRNAs and the UPR, which may underlie important pathological aspects of these disorders.

Conclusion: It is evident that microRNAs regulate several components of the UPR and that these small non-coding RNAs, or other molecules that restore the UPR balance, may represent possible therapeutic options to normalise intracellular homeostasis.

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