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Approach from Chemical Biology for Cancer Research

Submission Deadline: 30 March 2023 (closed) View: 147

Guest Editors

Hiroyuki Osada, University of Shizuoka, Japan. Email: osadahiro@u-shizuoka-ken.ac.jp;

Herbert Waldmann, Max-Planck-Institute of Molecular Physiology, Department of Chemical Biology, Germany. Email: herbert.waldmann@mpi-dortmund.mpg.de;

Haian Fu, Department of Pharmacology and Chemical Biology, Emory University School of Medicine, USA. Email: hfu@emory.edu

Summary

Chemical biology is a research field which integrates multi-discipline and has yielded various small molecules such as probes and inhibitors. Cancer research is one of the most successful areas for chemical biology. Screening of anticancer drugs targeting oncogenes enabled new drug discovery. Imatinib, an inhibitor against Bcr-abl kinase, is the most prominent example and development of series of tyrosine kinase inhibitors was followed. Recent discovery of anti-cancer drugs targeting oncogenes, cancer metabolism and epigenetics will be compiled.

The aim of this special issue is to compile advancing knowledge of chemical biology for cancer research.

Keywords

probe, inhibitor, tyrosine kinase, oncogene, cancer metabolism, epigenetics

Published Papers

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ARTICLE

DPY19L3 promotes vasculogenic mimicry by its C-mannosyltransferase activity
HASSAN BAYDOUN, YUJI KATO, HIROKI KAMO, ANNA HÜSCH, HAYATO MIZUTA, RYOTA KAWAHARA, SIRO SIMIZU
Oncology Research, Vol.32, No.4, pp. 607-614, 2024, DOI:10.32604/or.2023.030304
（This article belongs to the Special Issue: Approach from Chemical Biology for Cancer Research)
Abstract
C-mannosylation is a post-translational modification that occurs intracellularly in the endoplasmic reticulum. In humans, biosynthesis of C-mannosylation in proteins containing thrombospondin type 1 repeat is catalyzed by the DPY19 family; nonetheless, biological functions of protein C-mannosylation are not yet fully understood, especially in tumor progression. Vasculogenic mimicry (VM) is the formation of fluid-conducting channels by highly invasive and genetically deregulated tumor cells, enabling the tumors to form matrix-embedded vasculogenic structures, containing plasma and blood cells to meet the metabolic demands of rapidly growing tumors. In this study, we focused on DPY19L3, a C-mannosyltransferase, and aimed to unravel
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ARTICLE

Cisplatin-induced activation of TGF-β signaling contributes to drug resistance
SAYAKA IMATSUJI, YUKIKO UJIE, HIROYUKI ODAKE, MASAYA IMOTO, SUSUMU ITOH, ETSU TASHIRO
Oncology Research, Vol.32, No.1, pp. 139-150, 2024, DOI:10.32604/or.2023.030190
（This article belongs to the Special Issue: Approach from Chemical Biology for Cancer Research)
Abstract Growing evidence suggests an association between epithelial-mesenchymal transition (EMT), a hallmark of tumor malignancy, and chemoresistance to a number of anti-cancer drugs. However, the mechanism of EMT induction in the process of acquiring anti-cancer drug resistance remains unclear. To address this issue, we obtained a number of cisplatin-resistant clones from LoVo cells and found that almost all of them lost cell-cell contacts. In these clones, the epithelial marker E-cadherin was downregulated, whereas the mesenchymal marker N-cadherin was upregulated. Moreover, the expression of EMT-related transcription factors, including Slug, was elevated. On the other hand, the upregulation More >

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ARTICLE

Identification of a dihydroorotate dehydrogenase inhibitor that inhibits cancer cell growth by proteomic profiling
MAKOTO KAWATANI, HARUMI AONO, SAYOKO HIRANUMA, TAKESHI SHIMIZU, MAKOTO MUROI, TOSHIHIKO NOGAWA, TOMOKAZU OHISHI, SHUN-ICHI OHBA, MANABU KAWADA, KANAMI YAMAZAKI, SHINGO DAN, NAOSHI DOHMAE, HIROYUKI OSADA
Oncology Research, Vol.31, No.6, pp. 833-844, 2023, DOI:10.32604/or.2023.030241
（This article belongs to the Special Issue: Approach from Chemical Biology for Cancer Research)
Abstract Dihydroorotate dehydrogenase (DHODH) is a central enzyme of the de novo pyrimidine biosynthesis pathway and is a promising drug target for the treatment of cancer and autoimmune diseases. This study presents the identification of a potent DHODH inhibitor by proteomic profiling. Cell-based screening revealed that NPD723, which is reduced to H-006 in cells, strongly induces myeloid differentiation and inhibits cell growth in HL-60 cells. H-006 also suppressed the growth of various cancer cells. Proteomic profiling of NPD723-treated cells in ChemProteoBase showed that NPD723 was clustered with DHODH inhibitors. H-006 potently inhibited human DHODH activity in vitro, whereas More >

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ARTICLE

Deoxynortryptoquivaline: A unique antiprostate cancer agent
YOHKO YAMAZAKI, MANABU KAWADA, ISAO MOMOSE
Oncology Research, Vol.31, No.6, pp. 845-853, 2023, DOI:10.32604/or.2023.030266
（This article belongs to the Special Issue: Approach from Chemical Biology for Cancer Research)
Abstract The androgen receptor (AR) is a critical target in all the clinical stages of prostate cancer. To identify a new AR inhibitor, we constructed a new screening system using the androgen-dependent growth of prostate cancer cell lines as a screening indicator. We screened 50,000 culture broths of microorganisms using this screening system and found that the fermentation broth produced by a fungus inhibited androgen-dependent growth of human prostate cancer LNCaP cells without cytotoxicity. Purification of this culture medium was performed, and this resulted in deoxynortryptoquivaline (DNT) being identified as a novel inhibitor of AR function. More >
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Isolation and characterization of β-transducin repeat-containing protein ligands screened using a high-throughput screening system
XINTONG LIU, EMIKO SANADA, JIANG LI, XIAOMENG LI, HIROYUKI OSADA, NOBUMOTO WATANABE
Oncology Research, Vol.31, No.5, pp. 645-654, 2023, DOI:10.32604/or.2023.030240
（This article belongs to the Special Issue: Approach from Chemical Biology for Cancer Research)
Abstract β-transducin repeat-containing protein (β-TrCP) is an F-box protein subunit of the E3 Skp1-Cullin-F box (SCF) type ubiquitin-ligase complex, and provides the substrate specificity for the ligase. To find potent ligands of β-TrCP useful for the proteolysis targeting chimera (PROTAC) system using β-TrCP in the future, we developed a high-throughput screening system for small molecule β-TrCP ligands. We screened the chemical library utilizing the system and obtained several hit compounds. The effects of the hit compounds on in vitro ubiquitination activity of SCF^β-TrCP1 and on downstream signaling pathways were examined. Hit compounds NPD5943, NPL62020-01, and NPL42040-01 inhibited the… More >
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Identification of microbial metabolites that accelerate the ubiquitin-dependent degradation of c-Myc
ZIYU LIU, AKIKO OKANO, EMIKO SANADA, YUSHI FUTAMURA, TOSHIHIKO NOGAWA, KOSUKE ISHIKAWA, KENTARO SEMBA, JIANG LI, XIAOMENG LI, HIROYUKI OSADA, NOBUMOTO WATANABE
Oncology Research, Vol.31, No.5, pp. 655-666, 2023, DOI:10.32604/or.2023.030248
（This article belongs to the Special Issue: Approach from Chemical Biology for Cancer Research)
Abstract
Myc belongs to a family of proto-oncogenes that encode transcription factors. The overexpression of c-Myc causes many types of cancers. Recently, we established a system for screening c-Myc inhibitors and identified antimycin A by screening the RIKEN NPDepo chemical library. The specific mechanism of promoting tumor cell metastasis by high c-Myc expression remains to be explained. In this study, we screened approximately 5,600 microbial extracts using this system and identified a broth prepared from Streptomyces sp. RK19-A0402 strongly inhibits c-Myc transcriptional activity. After purification of the hit broth, we identified compounds closely related to the aglycone
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Approach from Chemical Biology for Cancer Research

Guest Editors

Summary

Keywords

Published Papers

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539

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761

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496

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781

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