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Molecules
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Peptides and Small Molecules as Anti-Cancer Agents
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Peptides and Small Molecules as Anti-Cancer Agents

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 June 2020) | Viewed by 31365

Special Issue Editors

Dr. Franco M. Buonaguro

E-Mail Website
Guest Editor
Molecular Biology and Viral Oncology Unit, Istituto Nazionale Tumori IRCCS Fondazione Pascale, 80131 Naples, Italy
Interests: oncology; molecular biology; virology; biochemistry
Special Issues, Collections and Topics in MDPI journals
Dr. Anna Lucia Tornesello

E-Mail Website
Assistant Guest Editor
Innovative Immunological Models Unit, Istituto Nazionale Tumori IRCCS Fondazione Pascale, 80131 Naples, Italy
Interests: bioactive peptides; peptide drug development; peptide drug conjugate; anticancer peptides; peptides in diagnosis and therapy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cancer is the second leading cause of death worldwide, with an estimated 9.6 million deaths in 2018. Novel cancer drugs that selectively suppress cancer cells and limit their chemoresistance as well as the relapse after treatment and the establishment of secondary malignancies are urgently needed. Cancer cells are characterized by the increased expression of normal and/or defective signaling molecules and receptors targeted by specific antagonistic proteins or peptides. Thus, synthetic peptides and peptide-based small molecules represent an attractive class of molecules for the design of new drugs, lead compounds, drug carriers, and excipients.

Recent developments in peptide chemistry and high-throughput screening platforms have generated enthusiasm and interest in the design and discovery of novel moieties for a broad range of biological and pharmacological applications. Advances in peptides and small-molecule engineering have helped to overcome several limitations, such as poor systemic stability, rapid clearance, and low binding affinities to biological targets.

Nanotechnologies providing enzymatic protection and controlled release of peptides or small molecules, made of minimum active peptides, represent optimal strategies for the targeted delivery of bioactive drugs to specific tissues. Moreover, the conjugation of peptides to nanovector surfaces carrying conventional chemotherapeutic agents can be useful for the selective delivery and killing of tumor cells. Peptide-based drugs will therefore have a significant impact in the near future for the treatment of many types of tumor.

We welcome the submission of research and review articles on the advances and opportunities of peptide-based drugs and peptide delivery systems in oncology to bring together expert opinions and new advances from across the field in this Special Issue of Molecules.

Dr. Franco M. Buonaguro
Dr. Anna Lucia Tornesello
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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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
  • theranostics
  • small molecules
  • peptide drugs
  • lead compounds
  • peptidomimetics
  • synthetic anticancer peptides
  • cell-penetrating peptides
  • radiolabeled peptides
  • oncology

Related Special Issue

Published Papers (5 papers)

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Research

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22 pages, 4588 KiB  
Article
Development and Characterization of the Shortest Anti-Adhesion Peptide Analogue of B49Mod1
by Yuan Lyu, Wadie D. Mahauad-Fernandez and Chioma M. Okeoma
Molecules 2020, 25(5), 1188; https://doi.org/10.3390/molecules25051188 - 06 Mar 2020
Cited by 4 | Viewed by 2762
Abstract
Inhibition of cancer cell adhesion is an effective approach to killing adherent cancer cells. B49 and its analog B49Mod1 peptides, derived from the extracellular domain (ECD) of bone marrow stromal antigen 2 (BST-2), display anti-adhesion activity on breast cancer cells. However, the minimal [...] Read more.
Inhibition of cancer cell adhesion is an effective approach to killing adherent cancer cells. B49 and its analog B49Mod1 peptides, derived from the extracellular domain (ECD) of bone marrow stromal antigen 2 (BST-2), display anti-adhesion activity on breast cancer cells. However, the minimal sequence required for this anti-adhesion activity is unknown. Here, we further characterized the anti-adhesion activity of B49Mod1. We show that the anti-adhesion activity of B49Mod1 may require cysteine-linked disulfide bond and that the peptide is susceptible to proteolytic deactivation. Using structure-activity relationship studies, we identified an 18-Mer sequence (B18) as the minimal peptide sequence mediating the anti-adhesion activity of B49Mod1. Atomistic molecular dynamic (MD) simulations reveal that B18 forms a stable complex with the ECD of BST-2 in aqueous solution. MD simulations further reveal that B18 may cause membrane defects that facilitates peptide translocation across the bilayer. Placement of four B18 chains as a transmembrane bundle results in water channel formation, indicating that B18 may impair membrane integrity and form pores. We hereby identify B18 as the minimal peptide sequence required for the anti-adhesion activity of B49Mod1 and provide atomistic insight into the interaction of B18 with BST-2 and the cell membrane. Full article
(This article belongs to the Special Issue Peptides and Small Molecules as Anti-Cancer Agents)
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Review

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29 pages, 1357 KiB  
Review
Antimicrobial Peptides as Anticancer Agents: Functional Properties and Biological Activities
by Anna Lucia Tornesello, Antonella Borrelli, Luigi Buonaguro, Franco Maria Buonaguro and Maria Lina Tornesello
Molecules 2020, 25(12), 2850; https://doi.org/10.3390/molecules25122850 - 19 Jun 2020
Cited by 196 | Viewed by 9839
Abstract
Antimicrobial peptides (AMPs), or host defense peptides, are small cationic or amphipathic molecules produced by prokaryotic and eukaryotic organisms that play a key role in the innate immune defense against viruses, bacteria and fungi. AMPs have either antimicrobial or anticancer activities. Indeed, cationic [...] Read more.
Antimicrobial peptides (AMPs), or host defense peptides, are small cationic or amphipathic molecules produced by prokaryotic and eukaryotic organisms that play a key role in the innate immune defense against viruses, bacteria and fungi. AMPs have either antimicrobial or anticancer activities. Indeed, cationic AMPs are able to disrupt microbial cell membranes by interacting with negatively charged phospholipids. Moreover, several peptides are capable to trigger cytotoxicity of human cancer cells by binding to negatively charged phosphatidylserine moieties which are selectively exposed on the outer surface of cancer cell plasma membranes. In addition, some AMPs, such as LTX-315, have shown to induce release of tumor antigens and potent damage associated molecular patterns by causing alterations in the intracellular organelles of cancer cells. Given the recognized medical need of novel anticancer drugs, AMPs could represent a potential source of effective therapeutic agents, either alone or in combination with other small molecules, in oncology. In this review we summarize and describe the properties and the mode of action of AMPs as well as the strategies to increase their selectivity toward specific cancer cells. Full article
(This article belongs to the Special Issue Peptides and Small Molecules as Anti-Cancer Agents)
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22 pages, 1371 KiB  
Review
How Computational Chemistry and Drug Delivery Techniques Can Support the Development of New Anticancer Drugs
by Mariangela Garofalo, Giovanni Grazioso, Andrea Cavalli and Jacopo Sgrignani
Molecules 2020, 25(7), 1756; https://doi.org/10.3390/molecules25071756 - 10 Apr 2020
Cited by 24 | Viewed by 5049
Abstract
The early and late development of new anticancer drugs, small molecules or peptides can be slowed down by some issues such as poor selectivity for the target or poor ADME properties. Computer-aided drug design (CADD) and target drug delivery (TDD) techniques, although apparently [...] Read more.
The early and late development of new anticancer drugs, small molecules or peptides can be slowed down by some issues such as poor selectivity for the target or poor ADME properties. Computer-aided drug design (CADD) and target drug delivery (TDD) techniques, although apparently far from each other, are two research fields that can give a significant contribution to overcome these problems. Their combination may provide mechanistic understanding resulting in a synergy that makes possible the rational design of novel anticancer based therapies. Herein, we aim to discuss selected applications, some also from our research experience, in the fields of anticancer small organic drugs and peptides. Full article
(This article belongs to the Special Issue Peptides and Small Molecules as Anti-Cancer Agents)
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24 pages, 577 KiB  
Review
Targeting Tumors Using Peptides
by Pablo Scodeller and Eliana K. Asciutto
Molecules 2020, 25(4), 808; https://doi.org/10.3390/molecules25040808 - 13 Feb 2020
Cited by 37 | Viewed by 6803
Abstract
To penetrate solid tumors, low molecular weight (Mw < 10 KDa) compounds have an edge over antibodies: their higher penetration because of their small size. Because of the dense stroma and high interstitial fluid pressure of solid tumors, the penetration of higher Mw [...] Read more.
To penetrate solid tumors, low molecular weight (Mw < 10 KDa) compounds have an edge over antibodies: their higher penetration because of their small size. Because of the dense stroma and high interstitial fluid pressure of solid tumors, the penetration of higher Mw compounds is unfavored and being small thus becomes an advantage. This review covers a wide range of peptidic ligands—linear, cyclic, macrocyclic and cyclotidic peptides—to target tumors: We describe the main tools to identify peptides experimentally, such as phage display, and the possible chemical modifications to enhance the properties of the identified peptides. We also review in silico identification of peptides and the most salient non-peptidic ligands in clinical stages. We later focus the attention on the current validated ligands available to target different tumor compartments: blood vessels, extracelullar matrix, and tumor associated macrophages. The clinical advances and failures of these ligands and their therapeutic conjugates will be discussed. We aim to present the reader with the state-of-the-art in targeting tumors, by using low Mw molecules, and the tools to identify new ligands. Full article
(This article belongs to the Special Issue Peptides and Small Molecules as Anti-Cancer Agents)
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25 pages, 610 KiB  
Review
Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy
by Huihui Zhu, Tao Wei, Yong Cai and Jingji Jin
Molecules 2020, 25(3), 578; https://doi.org/10.3390/molecules25030578 - 29 Jan 2020
Cited by 16 | Viewed by 6206
Abstract
Epigenetic modifications (or epigenetic tags) on DNA and histones not only alter the chromatin structure, but also provide a recognition platform for subsequent protein recruitment and enable them to acquire executive instructions to carry out specific intracellular biological processes. In cells, different epigenetic-tags [...] Read more.
Epigenetic modifications (or epigenetic tags) on DNA and histones not only alter the chromatin structure, but also provide a recognition platform for subsequent protein recruitment and enable them to acquire executive instructions to carry out specific intracellular biological processes. In cells, different epigenetic-tags on DNA and histones are often recognized by the specific domains in proteins (readers), such as bromodomain (BRD), chromodomain (CHD), plant homeodomain (PHD), Tudor domain, Pro-Trp-Trp-Pro (PWWP) domain and malignant brain tumor (MBT) domain. Recent accumulating data reveal that abnormal intracellular histone modifications (histone marks) caused by tumors can be modulated by small molecule-mediated changes in the activity of the above domains, suggesting that small molecules targeting histone-mark reader domains may be the trend of new anticancer drug development. Here, we summarize the protein domains involved in histone-mark recognition, and introduce recent research findings about small molecules targeting histone-mark readers in cancer therapy. Full article
(This article belongs to the Special Issue Peptides and Small Molecules as Anti-Cancer Agents)
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