Special Issue "EPH and Ephrins in Pathogenesis and as Drug Target"

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

Deadline for manuscript submissions: 30 April 2023 | Viewed by 1179

Special Issue Editors

Dr. Massimiliano Tognolini
E-Mail Website
Guest Editor
Department of Food and Drug, University of Parma, 43124 Parma, Italy
Interests: drug discovery; Eph; ephrin; protein–protein interaction inhibitors (PPI-is); polyphenols; cancer; platelets
Prof. Dr. Jiangping Wu
E-Mail Website
Guest Editor
Centre Hospitalier de L'Universite de Montreal, University of Montreal, Montreal, QC, Canada
Interests: Eph; ephrin; hypertension; heart rhythm; diabetes; ubiquitin ligase; RNA polymerase II; neural tube defects
Dr. Carmine Giorgio
E-Mail Website
Guest Editor
Department of Food and Drug, University of Parma, 43124 Parma, Italy
Interests: pharmacology; drug discovery; Eph–ephrin system; cancer; intestinal inflammation

Special Issue Information

Dear Colleagues,

Thirty-five years after the discovery of the first EPH gene by Takaku’s group, Eph receptors and the ephrin ligands are known to constitute a complex and redundant cellular communication network that is mainly involved in adhesion/repulsion responses; these are key processes during embryogenesis, angiogenesis, in the organized cell renewal of the epithelial tissues and in the regeneration/remodeling after injuries. Therefore, it is not surprising that members of this system were shown to be involved in many pathophysiological conditions such as inflammation and atherosclerosis, neurological disorders and cancer, making Eph receptors and ephrin ligands new attractive targets for pharmacologists and pharmaceutical chemists.

At present a plethora of biological techniques and pharmacological tools are available to investigate the roles and the potential benefits of Eph/ephrin targeting in several diseases. Small molecules, peptides and antibodies have shown promising and convincing results in vitro and in preclinical animal models, and some of them have reached clinical trials. Unfortunately, despite these research efforts, drugs targeting this system have not yet reached the market, and the gap between bench and bed still exists.

Taking advantage of the third congress on the Eph/ephrin system (www.ephrins.org), which we recently organized in Montreal after four years of absence due to the pandemic, the present Special Issue of Pharmaceuticals aims to be not only a synthesis of this meeting, but also an opportunity for all scientists in this field. This Special Issue aims to collect the most updated works and to be a valid source of inspiration for future research in the field of Eph/ephrin targeting.

We sincerely hope that you will be able to submit your original contributions to this Special Issue, which aims to be a valuable collection of state-of-the-art works on the Eph/ephrin targeting puzzle.

Dr. Massimiliano Tognolini
Prof. Dr. Jiangping Wu
Dr. Carmine Giorgio
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 2200 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

  • Eph–ephrin
  • drug discovery
  • pharmacokinetic
  • kinases
  • signaling
  • PPI inhibitors
  • peptides
  • antibodies
  • small molecules
  • targeting

Published Papers (2 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Review

Jump to: Other

Review
EPHB4-RASA1-Mediated Negative Regulation of Ras-MAPK Signaling in the Vasculature: Implications for the Treatment of EPHB4- and RASA1-Related Vascular Anomalies in Humans
Pharmaceuticals 2023, 16(2), 165; https://doi.org/10.3390/ph16020165 - 23 Jan 2023
Viewed by 401
Abstract
Ephrin receptors constitute a large family of receptor tyrosine kinases in mammals that through interaction with cell surface-anchored ephrin ligands regulate multiple different cellular responses in numerous cell types and tissues. In the cardiovascular system, studies performed in vitro and in vivo have [...] Read more.
Ephrin receptors constitute a large family of receptor tyrosine kinases in mammals that through interaction with cell surface-anchored ephrin ligands regulate multiple different cellular responses in numerous cell types and tissues. In the cardiovascular system, studies performed in vitro and in vivo have pointed to a critical role for Ephrin receptor B4 (EPHB4) as a regulator of blood and lymphatic vascular development and function. However, in this role, EPHB4 appears to act not as a classical growth factor receptor but instead functions to dampen the activation of the Ras-mitogen activated protein signaling (MAPK) pathway induced by other growth factor receptors in endothelial cells (EC). To inhibit the Ras-MAPK pathway, EPHB4 interacts functionally with Ras p21 protein activator 1 (RASA1) also known as p120 Ras GTPase-activating protein. Here, we review the evidence for an inhibitory role for an EPHB4–RASA1 interface in EC. We further discuss the mechanisms by which loss of EPHB4–RASA1 signaling in EC leads to blood and lymphatic vascular abnormalities in mice and the implications of these findings for an understanding of the pathogenesis of vascular anomalies in humans caused by mutations in EPHB4 and RASA1 genes. Last, we provide insights into possible means of drug therapy for EPHB4- and RASA1-related vascular anomalies. Full article
(This article belongs to the Special Issue EPH and Ephrins in Pathogenesis and as Drug Target)
Show Figures

Figure 1

Other

Jump to: Review

Case Report
Cooccurring Type 1 Diabetes Mellitus and Autoimmune Thyroiditis in a Girl with Craniofrontonasal Syndrome: Are EFNB1 Variants Associated with Autoimmunity?
Pharmaceuticals 2022, 15(12), 1535; https://doi.org/10.3390/ph15121535 - 10 Dec 2022
Viewed by 434
Abstract
Craniofrontonasal syndrome (CFNS), also known as craniofrontonasal dysplasia, is an X-linked inherited developmental malformation caused by mutations in the ephrin B1 (EFNB1) gene. The main phenotypic features of the syndrome are coronal synostosis, hypertelorism, bifid nasal tip, dry and curly hair, [...] Read more.
Craniofrontonasal syndrome (CFNS), also known as craniofrontonasal dysplasia, is an X-linked inherited developmental malformation caused by mutations in the ephrin B1 (EFNB1) gene. The main phenotypic features of the syndrome are coronal synostosis, hypertelorism, bifid nasal tip, dry and curly hair, and longitudinal splitting of nails. A 9-year-and-11-month-old girl with CFNS was admitted due to polyuria, polydipsia, fatigue, and abdominal pain. On physical examination, she had the classical phenotypical features of CFNS. Genetic tests revealed a c.429_430insT (p.Gly144TrpfsTer31) heterozygote variant in the EFNB1 coding region. The patient was diagnosed with type 1 diabetes mellitus (T1DM) and autoimmune thyroiditis based on laboratory findings and symptoms. The mother of the patient, who had the same CFNS phenotype and EFNB1 variant, was screened for autoimmune diseases and was also with autoimmune thyroiditis. This is the first report describing the association of CFNS with T1DM and autoimmune thyroiditis in patients with EFNB1 mutation. Full article
(This article belongs to the Special Issue EPH and Ephrins in Pathogenesis and as Drug Target)
Show Figures

Figure 1

Back to TopTop