Natural products are widely used as source for drugs development. An interesting example is represented by natural drugs developed against human topoisomerase IB, a ubiquitous enzyme involved in many cellular processes where several topological problems occur due the formation of supercoiled DNA. Human topoisomerase IB, involved in the solution of such problems relaxing the DNA cleaving and religating a single DNA strand, represents an important target in anticancer therapy. Several natural compounds inhibiting or poisoning this enzyme are under investigation as possible new drugs. This review summarizes the natural products that target human topoisomerase IB that may be used as the lead compounds to develop new anticancer drugs. Moreover, the natural compounds and their derivatives that are in clinical trial are also commented on.
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http://dx.doi.org/10.3390/ijms22084138 | DOI Listing |
Nat Commun
January 2025
Computational Oncology, Memorial Sloan Kettering Cancer Center, New York, NY, USA.
Large-scale combination drug screens are generally considered intractable due to the immense number of possible combinations. Existing approaches use ad hoc fixed experimental designs then train machine learning models to impute unobserved combinations. Here we propose BATCHIE, an orthogonal approach that conducts experiments dynamically in batches.
View Article and Find Full Text PDFMalays J Pathol
December 2024
Universiti Sains Malaysia, School of Dental Sciences, Health Campus, Kubang Kerian, Kelantan, Malaysia.
Introduction: Oral cancer is considered the sixth most common form of cancer worldwide. It causes significant morbidity and mortality, especially in low socioeconomic status groups. However, Cancer chemoprevention encompasses the use of specific compounds to suppress the growth of tumours or inhibit carcinogenesis.
View Article and Find Full Text PDFCurr Oncol
December 2024
Gynecology and Obstetrics 1U, Department of Surgical Sciences, University of Turin, 10126 Turin, Italy.
The enzyme topoisomerase II alpha (TOP2A) plays a critical role in DNA replication and cell proliferation, making it a promising target for cancer therapy. In epithelial ovarian cancer (EOC), TOP2A overexpression is associated with poor prognosis and resistance to conventional treatments. This review explores the biological functions of TOP2A in EOC and discusses its potential as a therapeutic target.
View Article and Find Full Text PDFGenes Cells
January 2025
School of Science and Technology, Gunma University, Kiryu, Japan.
Sulforaphane (SFN), an isothiocyanate found in plants of the Brassicaceae family, possesses antioxidant, apoptosis-inducing, and radiosensitizing effects. As one of the mechanisms of cytotoxicity by SFN, SFN has been suggested to be involved in the induction of DNA damage and inhibition of DNA repair. Recently, we reported on the potency of SFN in inducing single-ended double-strand breaks (DSBs) that are caused by the collision of replication forks with single-strand breaks (SSBs).
View Article and Find Full Text PDFAdv Rheumatol
December 2024
Department of Immunology & Molecular Medicine, Sher-I-Kashmir Institute of Medical Sciences (SKIMS), Soura, Srinagar, Jammu and Kashmir, 190011, India.
Background: As a master immune system regulator, transforming growth factor β1 (TGF-β1) is closely linked to the complicated pathophysiology and development of systemic sclerosis (SSc), a multisystem fibrotic disease.
Objective: We aim to evaluate the transcriptional levels of TGF-β1 mRNA in PBMCs, assess the TGF-β1 serum levels of SSc patients, and compare them with those of healthy subjects.
Methods: PBMCs were isolated from whole blood of 50 SSc patients and in 30 healthy controls.
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