Arginine methylation of ribose-5-phosphate isomerase A senses glucose to promote human colorectal cancer cell survival

Structure-Based Discovery of Potent CARM1 Inhibitors for Solid Tumor and Cancer Immunology Therapy

“…The combined filtrates were concentrated, and the resulting residue was purified by column chromatography on silica gel to afford the intermediate as a white solid (380 mg, 30%). 1 (29). A suspension of tert-butyl (2-((tert-butoxycarbonyl)(3-(4-chloro-5-methyl-6-((tetrahydro-2H-pyran-4-yl)amino)-pyrimidin-2-yl)benzyl)amino)ethyl)(methyl)carbamate 57a (100 mg, 0.17 mmol) in methanol (2 mL) was added to 2 mL of HCl solution in dioxane (4 M).…”

“…15,16 Considering these biological characteristics, CARM1 contributes to diverse cellular processes including RNA splicing, 17,18 transcriptional coactivation, 19 DNA repair, 20 cell differentiation, 21 and autophagy. 22,23 Accumulated evidence suggests the essential roles of CARM1 in both hematologic neoplasms like acute myeloid leukemia 24 and solid cancers including breast, 25 lung, 26 liver, 27 prostate 28 and colorectal carcinoma, 29 and overexpressed CARM1 is correlated with poor patient prognosis. 30,31 Pharmacological inhibition and genetic depletion of CARM1 can cause antiproliferation effects in specific cancer cell lines, 8,15,24,26 indicating that targeting CARM1 may be an effective therapeutic strategy for cancer treatment.…”

“…Accumulated evidence suggests the essential roles of CARM1 in both hematologic neoplasms like acute myeloid leukemia and solid cancers including breast, lung, liver, prostate and colorectal carcinoma, and overexpressed CARM1 is correlated with poor patient prognosis. , Pharmacological inhibition and genetic depletion of CARM1 can cause antiproliferation effects in specific cancer cell lines, ,,, indicating that targeting CARM1 may be an effective therapeutic strategy for cancer treatment. Encouraged by the tempting potential, the search for potent and selective CARM1 inhibitors has attracted considerable attention in the pharmaceutical industry and academic institutions.…”

PRMT6 promotes tumorigenicity and cisplatin response of lung cancer through triggering 6PGD/ENO1 mediated cell metabolism

“…Studies by Guo et al. 9 revealed that CARM1 methylates ribose-5-phosphate isomerase A (RPIA), an enzyme in oxidative pentose phosphate pathway (PPP), at arginine 42 (R42) and enhances its activity, which connects the glucose availability to nucleotide synthesis and redox homeostasis. Yamamoto et al.…”

Cancer metabolism and dietary interventions

“…aerobic glycolysis, known as the Warburg effect, to the rewired utilization of various nutrients, including glucose, amino acids, lipids, and other carbon and/or nitrogen suppliers, such as acetate 3 , 4 . The abnormal alterations in nutrient metabolism drive uncontrolled cancer cell proliferation and modulate the tumor microenvironment, thereby facilitatingother malignant tumor cell behaviors such as cancer invasion and metastasis 1 , 2 , 5 . Therefore, metabolic interventions, particularly the management of nutrient availability, are becoming more attractive for cancer treatment.…”