Special Issue "Molecular Targets and Targeting in Biomedical Sciences"

A special issue of Biology (ISSN 2079-7737).

Deadline for manuscript submissions: closed (30 September 2020).

Special Issue Editors

Prof. Dr. Carmen Burtea
E-Mail Website1 Website2
Guest Editor
Department of General, Organic and Biomedical Chemistry, NMR and Molecular Imaging Laboratory, Faculty of Medicine and Pharmacy, University of Mons, Avenue Maistriau 19, Mendeleev Building, B-7000 Mons, Belgium
Interests: bioactive peptides; cell biology; molecular targets; drug discovery; biomedicine; molecular imaging; MRI
Prof. Dr. Sven Saussez
E-Mail Website
Guest Editor
Department of Human Anatomy and Experimental Oncology, Faculty of Medicine and Pharmacy, University of Mons, Mons, Belgium
Interests: cancer; biology; head and neck; oncoimmunology; prognostic; immunotherapy
Prof. Dr. Marc Port
E-Mail Website
Guest Editor
Laboratoire de Génomique, Bioinformatique et Chimie Moléculaire (EA 7528), Equipe Chimie Moléculaire, Conservatoire National des Arts et Métiers (Cnam), HESAM Université, 75003 Paris, France
Interests: molecular targets; drug discovery; biomedicine; molecular imaging; nanopaticles; theranostic; medicinal chemistry

Special Issue Information

Dear Colleagues,

The personalized medicine endorsed by the remarkable breakthrough of genomic and proteomic technologies during the last decades will hopefully enable the fashioning of preventive, diagnostic, prognostic, and curative medicine, according to the individual’s genetic and molecular profile. Such tremendous progress in biomedical concepts will have an overwhelming impact on patient healthcare, both by preventing or limiting the medication side effects and reducing the healthcare costs as a result of an improved disease outcome.

The biomarkers represent key players in personalized medicine, and they are defined by the FDA-NIH Biomarker Working Group as a measurable molecular signature of normal or pathogenic processes, or as a therapeutic outcome of medical intervention. Among them, molecular biomarkers serve as targets for the development of molecularly targeted imaging probes and therapeutics through a wide range of library-based display technologies. But what are the real progresses, challenges, and perspectives of all of these modern tools of molecular biology for biomedical research in general and for patient care in particular?

This Special Issue welcomes the submission of original research and review manuscripts focusing on biomarkers of interest for the diagnosis, therapy, and theranostics of a wide range of pathologies, but also on the specific technologies employed in their identification and targeting, helping us to achieve a realistic overview of this exciting and interdisciplinary field of biomedical research.

Prof. Dr. Carmen Burtea
Prof. Dr. Sven Saussez
Prof. Dr. Marc Port
Guest Editors

Manuscript Submission Information

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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. Biology 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 1800 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

  • biomarkers
  • targeted therapy
  • molecular targeting
  • imaging probes
  • molecular imaging
  • theranostics
  • library-based display technologies
  • peptides
  • aptamers
  • antibodies

Published Papers (8 papers)

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Research

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Open AccessEditor’s ChoiceArticle
ACE2 Protein Landscape in the Head and Neck Region: The Conundrum of SARS-CoV-2 Infection
Biology 2020, 9(8), 235; https://doi.org/10.3390/biology9080235 - 18 Aug 2020
Cited by 9 | Viewed by 1114
Abstract
The coronavirus pandemic raging worldwide since December 2019 is caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which invades human cells via the angiotensin-converting enzyme 2 (ACE2) receptor. Although it has already been identified in many organs, ACE2 expression remains largely [...] Read more.
The coronavirus pandemic raging worldwide since December 2019 is caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which invades human cells via the angiotensin-converting enzyme 2 (ACE2) receptor. Although it has already been identified in many organs, ACE2 expression remains largely unknown in the head and neck (HN) sphere. Thus, this study aims to investigate its protein expression in several sites of the upper aerodigestive tract in order to highlight potential routes of infection. We compared ACE2 immunohistochemical expression between 70 paraffin-embedded specimens with two different antibodies and reported the quantified expression in each histological location. Surprisingly, we obtained different results depending on the antibody, an absence of labeling having been observed with a monoclonal antibody raised against the extracellular domain, whereas the polyclonal, against the cytoplasmic part of the protein, revealed enriched ACE2 expression, particularly in sinuses, vocal cords, salivary glands and oral cavity epithelial cells. The interpretation of these discordant results has brought several exciting lines of reflection. In conclusion, this study provides possible routes of entry for the SARS-CoV-2 in HN region and, above all, has led us to encourage caution when studying the ACE2 expression which is currently at the center of all attention. Full article
(This article belongs to the Special Issue Molecular Targets and Targeting in Biomedical Sciences)
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Open AccessArticle
Toad Venom Antiproliferative Activities on Metastatic Melanoma: Bio-Guided Fractionation and Screening of the Compounds of Two Different Venoms
Biology 2020, 9(8), 218; https://doi.org/10.3390/biology9080218 - 10 Aug 2020
Cited by 2 | Viewed by 638
Abstract
Melanoma is the most common cancer in young adults, with a constantly increasing incidence. Metastatic melanoma is a very aggressive cancer with a 5-year survival rate of about 22−25%. This is, in most cases, due to a lack of therapies which are effective [...] Read more.
Melanoma is the most common cancer in young adults, with a constantly increasing incidence. Metastatic melanoma is a very aggressive cancer with a 5-year survival rate of about 22−25%. This is, in most cases, due to a lack of therapies which are effective on the long term. Hence, it is crucial to find new therapeutic agents to increase patient survival. Toad venoms are a rich source of potentially pharmaceutically active compounds and studies have highlighted their possible effect on cancer cells. We focused on the venoms of two different toad species: Bufo bufo and Rhinella marina. We screened the venom crude extracts, the fractions from crude extracts and isolated biomolecules by studying their antiproliferative properties on melanoma cells aiming to determine the compound or the combination of compounds with the highest antiproliferative effect. Our results indicated strong antiproliferative capacities of toad venoms on melanoma cells. We found that these effects were mainly due to bufadienolides that are cardiotonic steroids potentially acting on the Na+/K+ ATPase pump which is overexpressed in melanoma. Finally, our results indicated that bufalin alone was the most interesting compound among the isolated bufadienolides because it had the highest antiproliferative activity on melanoma cells. Full article
(This article belongs to the Special Issue Molecular Targets and Targeting in Biomedical Sciences)
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Open AccessArticle
Development of an LDL Receptor-Targeted Peptide Susceptible to Facilitate the Brain Access of Diagnostic or Therapeutic Agents
Biology 2020, 9(7), 161; https://doi.org/10.3390/biology9070161 - 11 Jul 2020
Cited by 1 | Viewed by 766
Abstract
Blood-brain barrier (BBB) crossing and brain penetration are really challenging for the delivery of therapeutic agents and imaging probes. The development of new crossing strategies is needed, and a wide range of approaches (invasive or not) have been proposed so far. The receptor-mediated [...] Read more.
Blood-brain barrier (BBB) crossing and brain penetration are really challenging for the delivery of therapeutic agents and imaging probes. The development of new crossing strategies is needed, and a wide range of approaches (invasive or not) have been proposed so far. The receptor-mediated transcytosis is an attractive mechanism, allowing the non-invasive penetration of the BBB. Among available targets, the low-density lipoprotein (LDL) receptor (LDLR) shows favorable characteristics mainly because of the lysosome-bypassed pathway of LDL delivery to the brain, allowing an intact discharge of the carried ligand to the brain targets. The phage display technology was employed to identify a dodecapeptide targeted to the extracellular domain of LDLR (ED-LDLR). This peptide was able to bind the ED-LDLR in the presence of natural ligands and dissociated at acidic pH and in the absence of calcium, in a similar manner as the LDL. In vitro, our peptide was endocytosed by endothelial cells through the caveolae-dependent pathway, proper to the LDLR route in BBB, suggesting the prevention of its lysosomal degradation. The in vivo studies performed by magnetic resonance imaging and fluorescent lifetime imaging suggested the brain penetration of this ED-LDLR-targeted peptide. Full article
(This article belongs to the Special Issue Molecular Targets and Targeting in Biomedical Sciences)
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Open AccessArticle
A Comparative Study of Rat Urine 1H-NMR Metabolome Changes Presumably Arising from Isoproterenol-Induced Heart Necrosis Versus Clarithromycin-Induced QT Interval Prolongation
Biology 2020, 9(5), 98; https://doi.org/10.3390/biology9050098 - 13 May 2020
Viewed by 1005
Abstract
Cardiotoxicity remains a challenging concern both in drug development and in the management of various clinical situations. There are a lot of examples of drugs withdrawn from the market or stopped during clinical trials due to unpredicted cardiac adverse events. Obviously, current conventional [...] Read more.
Cardiotoxicity remains a challenging concern both in drug development and in the management of various clinical situations. There are a lot of examples of drugs withdrawn from the market or stopped during clinical trials due to unpredicted cardiac adverse events. Obviously, current conventional methods for cardiotoxicity assessment suffer from a lack of predictivity and sensitivity. Therefore, there is a need for developing new tools to better identify and characterize any cardiotoxicity that can occur during the pre-clinical and clinical phases of drug development as well as after marketing in exposed patients. In this study, isoproterenol and clarithromycin were used as prototypical cardiotoxic agents in rats in order to evaluate potential biomarkers of heart toxicity at very early stages using 1H-NMR-based metabonomics. While isoproterenol is known to cause heart necrosis, clarithromycin may induce QT interval prolongation. Heart necrosis and QT prolongation were validated by histological analysis, serum measurement of lactate dehydrogenase/creatine phosphate kinase and QTc measurement by electrocardiogram (ECG). Urine samples were collected before and repeatedly during daily exposure to the drugs for 1H-NMR based-metabonomics investigations. Specific metabolic signatures, characteristic of each tested drug, were obtained from which potential predictive biomarkers for drug-induced heart necrosis and drug-induced QT prolongation were retrieved. Isoproterenol-induced heart necrosis was characterized by higher levels of taurine, creatine, glucose and by lower levels of Krebs cycle intermediates, creatinine, betaine/trimethylamine N-oxide (TMAO), dimethylamine (DMA)/sarcosine. Clarithromycin-induced QT prolongation was characterized by higher levels of creatinine, taurine, betaine/TMAO and DMA/sarcosine and by lower levels of Krebs cycle intermediates, glucose and hippurate. Full article
(This article belongs to the Special Issue Molecular Targets and Targeting in Biomedical Sciences)
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Open AccessArticle
Molecular Imaging of Galectin-1 Expression as a Biomarker of Papillary Thyroid Cancer by Using Peptide-Functionalized Imaging Probes
Biology 2020, 9(3), 53; https://doi.org/10.3390/biology9030053 - 14 Mar 2020
Viewed by 879
Abstract
Thyroid cancers are the most frequent endocrine cancers and their incidence is increasing worldwide. Thyroid nodules occur in over 19–68% of the population, but only 7–15% of them are diagnosed as malignant. Diagnosis relies on a fine needle aspiration biopsy, which is often [...] Read more.
Thyroid cancers are the most frequent endocrine cancers and their incidence is increasing worldwide. Thyroid nodules occur in over 19–68% of the population, but only 7–15% of them are diagnosed as malignant. Diagnosis relies on a fine needle aspiration biopsy, which is often inconclusive and about 90% of thyroidectomies are performed for benign lesions. Galectin-1 has been proposed as a confident biomarker for the discrimination of malignant from benign nodules. We previously identified by phage display two peptides (P1 and P7) targeting galectin-1, with the goal of developing imaging probes for non-invasive diagnosis of thyroid cancer. The peptides were coupled to ultra-small superparamagnetic particles of iron oxide (USPIO) or to a near-infrared dye (CF770) for non-invasive detection of galectin-1 expression in a mouse model of papillary thyroid cancer (PTC, as the most frequent one) by magnetic resonance imaging and fluorescence lifetime imaging. The imaging probes functionalized with the two peptides presented comparable image enhancement characteristics. However, those coupled to P7 were more favorable, and showed decreased retention by the liver and spleen (known for their galectin-1 expression) and high sensitivity (75%) and specificity (100%) of PTC detection, which confirm the aptitude of this peptide to discriminate human malignant from benign nodules (80% sensitivity, 100% specificity) previously observed by immunohistochemistry. Full article
(This article belongs to the Special Issue Molecular Targets and Targeting in Biomedical Sciences)
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Review

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Open AccessReview
VCAM-1 Target in Non-Invasive Imaging for the Detection of Atherosclerotic Plaques
Biology 2020, 9(11), 368; https://doi.org/10.3390/biology9110368 - 29 Oct 2020
Cited by 1 | Viewed by 800
Abstract
Atherosclerosis is a progressive chronic arterial disease characterised by atheromatous plaque formation in the intima of the arterial wall. Several invasive and non-invasive imaging techniques have been developed to detect and characterise atherosclerosis in the vessel wall: anatomic/structural imaging, functional imaging and molecular [...] Read more.
Atherosclerosis is a progressive chronic arterial disease characterised by atheromatous plaque formation in the intima of the arterial wall. Several invasive and non-invasive imaging techniques have been developed to detect and characterise atherosclerosis in the vessel wall: anatomic/structural imaging, functional imaging and molecular imaging. In molecular imaging, vascular cell adhesion molecule-1 (VCAM-1) is a promising target for the non-invasive detection of atherosclerosis and for the assessment of novel antiatherogenic treatments. VCAM-1 is an adhesion molecule expressed on the activated endothelial surface that binds leucocyte ligands and therefore promotes leucocyte adhesion and transendothelial migration. Hence, for several years, there has been an increase in molecular imaging methods for detecting VCAM-1 in MRI, PET, SPECT, optical imaging and ultrasound. The use of microparticles of iron oxide (MPIO), ultrasmall superparamagnetic iron oxide (USPIO), microbubbles, echogenic immunoliposomes, peptides, nanobodies and other nanoparticles has been described. However, these approaches have been tested in animal models, and the remaining challenge is bench-to-bedside development and clinical applicability. Full article
(This article belongs to the Special Issue Molecular Targets and Targeting in Biomedical Sciences)
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Open AccessReview
Liposome-Based Bioassays
Biology 2020, 9(8), 202; https://doi.org/10.3390/biology9080202 - 01 Aug 2020
Viewed by 1122
Abstract
This review highlights the potential of using liposomes in bioassays. Liposomes consist of nano- or micro-sized, synthetically constructed phospholipid vesicles. Liposomes can be loaded with a number of reporting molecules that allow a dramatic amplification of the detection threshold in bioassays. Liposome-based sensors [...] Read more.
This review highlights the potential of using liposomes in bioassays. Liposomes consist of nano- or micro-sized, synthetically constructed phospholipid vesicles. Liposomes can be loaded with a number of reporting molecules that allow a dramatic amplification of the detection threshold in bioassays. Liposome-based sensors bind or react with the biological components of targets through the introduction of properly tailored vectors anchored on their external surface. The use of liposome-based formulations allows the set-up of bioassays that are rapid, sensitive, and often suitable for in-field applications. Selected applications in the field of immunoassays, as well as recognition/assessment of corona proteins, nucleic acids, exosomes, bacteria, and viruses are surveyed. The role of magnetoliposomes is also highlighted as an additional tool in the armory of liposome-based systems for bioassays. Full article
(This article belongs to the Special Issue Molecular Targets and Targeting in Biomedical Sciences)
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Open AccessReview
Lymphocyte-Activation Gene 3 (LAG3) Protein as a Possible Therapeutic Target for Parkinson’s Disease: Molecular Mechanisms Connecting Neuroinflammation to α-Synuclein Spreading Pathology
Biology 2020, 9(4), 86; https://doi.org/10.3390/biology9040086 - 23 Apr 2020
Cited by 4 | Viewed by 1957
Abstract
Parkinson’s disease (PD) is the most common neurodegenerative movement disorder without any objective biomarker available to date. Increasing evidence highlights the critical role of neuroinflammation, including T cell responses, and spreading of aggregated α-synuclein in PD progression. Lymphocyte-activation gene 3 (LAG3) belongs to [...] Read more.
Parkinson’s disease (PD) is the most common neurodegenerative movement disorder without any objective biomarker available to date. Increasing evidence highlights the critical role of neuroinflammation, including T cell responses, and spreading of aggregated α-synuclein in PD progression. Lymphocyte-activation gene 3 (LAG3) belongs to the immunoglobulin (Ig) superfamily expressed by peripheral immune cells, microglia and neurons and plays a key role in T cell regulation. The role of LAG3 has been extensively investigated in several human cancers, whereas until recently, the role of LAG3 in the central nervous system (CNS) has been largely unknown. Accumulating evidence highlights the potential role of LAG3 in PD pathogenesis, mainly by binding to α-synuclein fibrils and affecting its endocytosis and intercellular transmission, which sheds more light on the connection between immune dysregulation and α-synuclein spreading pathology. Serum and cerebrospinal fluid (CSF) soluble LAG3 (sLAG3) levels have been demonstrated to be potentially associated with PD development and clinical phenotype, suggesting that sLAG3 could represent an emerging PD biomarker. Specific single nucleotide polymorphisms (SNPs) of the LAG3 gene have been also related to PD occurrence especially in the female population, enlightening the pathophysiological background of gender-related PD clinical differences. Given also the ongoing clinical trials investigating various LAG3-targeting strategies in human diseases, new opportunities are being developed for PD treatment research. In this review, we discuss recent preclinical and clinical evidence on the role of LAG3 in PD pathogenesis and biomarker potential, aiming to elucidate its underlying molecular mechanisms. Full article
(This article belongs to the Special Issue Molecular Targets and Targeting in Biomedical Sciences)
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