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Molecules
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Small Molecule Immuno-Oncology Drugs in Cancer Therapy
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Small Molecule Immuno-Oncology Drugs in Cancer Therapy

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

Deadline for manuscript submissions: closed (31 October 2022) | Viewed by 7742

Special Issue Editor

Prof. Dr. Liwu Fu

E-Mail Website
Guest Editor
Department of Experimental Research (Cancer Institute), Cancer Center, Sun Yat-sen University, Guangzhou 510060, China
Interests: multidrug resistance; tyrosine kinase inhibitor; ABC transporters; exosomes; cancer; cancer stem cells
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Immuno-oncology is an emerging option to treat cancer malignancies. Immune checkpoint inhibitors represented by immunocytotoxic T lymphocyte-associated antigens 4 (CTLA-4) and programmed death receptor 1 (PD-1) monoAbs have made breakthroughs in the field of tumor immunotherapy. Additionally, small-molecule tumor immunotherapeutic agents generally exert antitumor effects by regulating the tumor immunosuppressive microenvironment or by targeting innate/adaptive immune pathways. Compared with antibody drugs, small-molecule tumor immunotherapeutic drugs can act not only on extracellular or cell-surface targets, but also through the cell membrane and other biological barriers to act on specific intracellular targets to cause antitumor immune response and have higher permeability to the tumor microenvironment. Furthermore, small-molecule tumor immunotherapeutic agents have superior pharmacokinetic properties to macromolecular antibodies, such as short half-life and good oral bioavailability, and can also balance the risk of possible side effects caused by combination therapies. The targets of the action of small-molecule immune drugs entering the clinical research stage mainly include PD-1/PD-L1, A2A adenosine receptor (A2AR), chemokine receptors, stimulator of interferon genes (Sting), indoleamine 2,3-dioxygenase (IDO), V-domain immunoglobulin suppressor of T-cell activation (VISTA), transforming growth factor β (TGF-β), toll-like receptor (TLR), the retinoic acid-receptor-related orphan receptor γt (ROR t), arginases (ARGs), and so on.

To make this Special Issue more interesting, we look forward to your contributions and those of your colleagues in the form of reviews, comments and original research articles.

Thanks for your attention.

Prof. Dr. Liwu Fu
Guest Editor

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

  • cancer
  • immunotherapy
  • small-molecule agents
  • PD-1/PD-L1
  • A2A adenosine receptor
  • chemokine receptors
  • Sting
  • indoleamine 2,3-dioxygenase
  • V-domain immunoglobulin suppressor of T-cell activation
  • transforming growth factor β (TGF-β)
  • toll-like receptor (TLR)
  • retinoic acid-receptor-related orphan receptor γt (ROR t)
  • arginases (ARGs)

Published Papers (3 papers)

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Research

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15 pages, 7979 KiB  
Article
Discovery of Novel PI3Kδ Inhibitors Based on the p110δ Crystal Structure
by Wenqing Jia, Shuyu Luo, Wennan Zhao, Weiren Xu, Yuxu Zhong and Dexin Kong
Molecules 2022, 27(19), 6211; https://doi.org/10.3390/molecules27196211 - 21 Sep 2022
Cited by 4 | Viewed by 1540
Abstract
PI3Kδ is a key mediator of B-cell receptor signaling and plays an important role in the pathogenesis of certain hematological malignancies, such as chronic lymphocytic leukemia. Idelalisib, which targets PI3Kδ specifically, is the first approved PI3K inhibitor for cancer therapy. Recently, we carried [...] Read more.
PI3Kδ is a key mediator of B-cell receptor signaling and plays an important role in the pathogenesis of certain hematological malignancies, such as chronic lymphocytic leukemia. Idelalisib, which targets PI3Kδ specifically, is the first approved PI3K inhibitor for cancer therapy. Recently, we carried out virtual screening, cell-based assays, adapta kinase assays, and molecular dynamic analysis to discover novel PI3Kδ inhibitors and identified NSC348884 as a lead PI3Kδ inhibitor. NSC348884 had an excellent docking score, potent PI3Kδ-inhibitory activity, antitumor effects on various cancer cell lines, and a favorable binding mode with the active site of PI3Kδ. Moreover, through the structural modification of NSC348884, we further discovered comp#1, which forms H-bonds with both Val828 and Lys779 in the ATP binding pocket of PI3Kδ, with a more favorable conformation binding to PI3Kδ. In addition, we found that N1, N1, N2-trimethyl-N2-((6-methyl-1H-benzo[d]imidazol-2-yl) methyl) ethane-1,2-diamine might be a potential scaffold structure. Thus, the result of this study provides a far more efficient approach for discovering novel inhibitors targeting PI3Kδ. Full article
(This article belongs to the Special Issue Small Molecule Immuno-Oncology Drugs in Cancer Therapy)
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Review

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17 pages, 1806 KiB  
Review
Effect of Gut Microbiota-Derived Metabolites on Immune Checkpoint Inhibitor Therapy: Enemy or Friend?
by Haobin Zhao, Di Wang, Zhifu Zhang, Junfang Xian and Xiaosu Bai
Molecules 2022, 27(15), 4799; https://doi.org/10.3390/molecules27154799 - 27 Jul 2022
Cited by 9 | Viewed by 2639
Abstract
The human gut is inhabited by hundreds of billions of commensal microbiota that collectively produce thousands of small molecules and metabolites with local and systemic effects on the physiology of the host. Much evidence from preclinical to clinical studies has gradually confirmed that [...] Read more.
The human gut is inhabited by hundreds of billions of commensal microbiota that collectively produce thousands of small molecules and metabolites with local and systemic effects on the physiology of the host. Much evidence from preclinical to clinical studies has gradually confirmed that the gut microbiota can regulate anti-tumor immunity and affect the efficacy of cancer immune checkpoint inhibitors (ICIs) therapy. In particular, one of the main modes of gut microbiota regulating anti-tumor immunity is through metabolites, which are small molecules that can be transported in the body and act on local and systemic anti-tumor immune responses to promote ICIs immunotherapy efficacy. We discuss the functions of microbial metabolites in humans, focusing on the effects and mechanisms of microbial metabolites on immunotherapy, and analyze their potential applications as immune adjuvants and therapeutic targets to regulate immunity and enhance ICIs. In summary, this review provides the basis for the rational design of microbiota and microbial metabolite-based strategies of enhancing ICIs. Full article
(This article belongs to the Special Issue Small Molecule Immuno-Oncology Drugs in Cancer Therapy)
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13 pages, 1610 KiB  
Review
Therapeutic Perspectives of CD26 Inhibitors in Imune-Mediated Diseases
by Xiaopeng Hu, Xisheng Wang and Xingkui Xue
Molecules 2022, 27(14), 4498; https://doi.org/10.3390/molecules27144498 - 14 Jul 2022
Cited by 7 | Viewed by 2933
Abstract
The enzymatic activity of CD26/DPP4 (dipeptidyl peptidase 4/DPP4) is highlighted in multiple studies to play a vital role in glucose metabolism by cleaving and inactivating the incretins glucagon-like peptide-1 (GLP) and gastric inhibitory protein (GIP). A large number of studies demonstrate that CD26 [...] Read more.
The enzymatic activity of CD26/DPP4 (dipeptidyl peptidase 4/DPP4) is highlighted in multiple studies to play a vital role in glucose metabolism by cleaving and inactivating the incretins glucagon-like peptide-1 (GLP) and gastric inhibitory protein (GIP). A large number of studies demonstrate that CD26 also plays an integral role in the immune system, particularly in T cell activation. CD26 is extensively expressed in immune cells, such as T cells, B cells, NK cells, dendritic cells, and macrophages. The enzymatic activity of CD26 cleaves and regulates numerous chomokines and cytokines. CD26 inhibitors have been widely used for the treatment of diabetes mellitus, while it is still under investigation as a therapy for immune-mediated diseases. In addition, CD26’s involvement in cancer immunology was also described. The review aims to summarize the therapeutic effects of CD26 inhibitors on immune-mediated diseases, as well as the mechanisms that underpin them. Full article
(This article belongs to the Special Issue Small Molecule Immuno-Oncology Drugs in Cancer Therapy)
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