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Bioactivation, Mutagenicity, DNA Damage, and Oxidative Stress Induced by 3,4-Dimethylaniline.
Biomolecules
December 2024
Department of Pharmacology & Toxicology, University of Louisville School of Medicine, Louisville, KY 40202, USA.
3,4-Dimethylaniline (3,4-DMA) is present in cigarette smoke and widely used as an intermediate in dyes, drugs, and pesticides. Nucleotide excision repair-deficient Chinese hamster ovary (CHO) cells stably transfected with human CYP1A2 and N-acetyltransferase 1 (NAT1) alleles: (reference allele) or (the most common variant allele) were utilized to assess 3,4-DMA -acetylation and hypoxanthine phosphoribosyl transferase (HPRT) mutations, double-strand DNA breaks and reactive oxygen species (ROS). CHO cells expressing exhibited significantly ( < 0.
View Article and Find Full Text PDFStructure-activity relationship studies and design of a PTPN22 inhibitor with enhanced isozyme selectivity and cellular efficacy.
Eur J Med Chem
February 2025
Borch Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA; James Tarpo Jr. and Margaret Tarpo Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA; Institute for Drug Discovery, Purdue University, West Lafayette, IN 47907, USA; Institute for Cancer Research, Purdue University, West Lafayette, IN 47907, USA. Electronic address:
Protein tyrosine phosphatase non-receptor type 22 (PTPN22) lies downstream of the T cell receptor (TCR) and attenuates T cell signaling by dephosphorylating key effector proteins such as LCK, Zap70, and the intracellular region of the TCR. Recent evidence implicates PTPN22 as an exciting target for enabling immunotherapeutic efficacy against cancer. We carried out structural optimization of a benzofuran salicylic acid-based orthosteric PTPN22 inhibitor 8b, using a combination of crystal structure analysis, synthesis, matched molecular pairs analysis, and biochemical and cell-based assays.
View Article and Find Full Text PDFAldehyde dehydrogenases as drug targets for cancer: SAR and structural biology aspects for inhibitor design.
Bioorg Chem
January 2025
Department of Bioinformatics, School of Life Scicnces, Pondicherry University, Pondicherry 605014, India. Electronic address:
Aldehydes are organic compounds containing a carbonyl group found exogenously or produced by normal metabolic processes and their accumulation can lead to toxicity if not cleared. Aldehyde dehydrogenases (ALDHs) are NAD(P)-dependent enzymes that catalyze the oxidation of such aldehydes and prevent their accumulation. Along with this primary detoxification function, the known 19 human isoforms of ALDHs, which act on different substrates, are also involved in various physiological and developmental processes.
View Article and Find Full Text PDFBevacizumab increases cisplatin efficacy by inhibiting epithelial-mesenchymal transition via ALDH1 in cervical carcinoma.
Int Immunopharmacol
January 2025
Department of Gynecology, Cancer Hospital of Dalian University of Technology (Liaoning Cancer Institute and Hospital), No. 44, Xiaoheyan Road, Shenyang 110042, Liaoning Province, China. Electronic address:
Cervical carcinoma has the highest incidence among gynaecological cancers in developing countries where the human papillomavirus (HPV) vaccine is not yet widely used. Cancer stem cells (CSCs) are the key factors affecting treatment efficacy and cancer prognosis. Aldehyde dehydrogenase 1 (ALDH1) is a marker of CSCs, and its expression is closely related to chemotherapy resistance in cervical carcinoma.
View Article and Find Full Text PDFTOE1 deadenylase inhibits gastric cancer cell proliferation by regulating cell cycle progression.
Biochim Biophys Acta Gen Subj
January 2025
Beijing International Science and Technology Cooperation Base of Antivirus Drug, College of Chemistry and Life Science, Beijing University of Technology, Beijing 100124, China. Electronic address:
TOE1, also known as hCaf1z, belongs to the DEDD superfamily of deadenylases and a newly identified isoenzyme of hCaf1 deadenylases. Previous research has demonstrated that TOE1 has deadenylase activity, which can catalyze the degradation of poly(A) substrates and interact with hCcr4d to form the unconventional human Ccr4-Caf1 deadenylase complex. Our recent research indicates that hCaf1a and hCaf1b isoenzymes, highly expressed in gastric cancer, promote gastric cancer cell proliferation and tumorigenicity via modulating cell cycle progression.
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