PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 34785428-0 2021 PRMT4 inhibitor TP-064 impacts both inflammatory and metabolic processes without changing the susceptibility for early atherosclerotic lesions in male apolipoprotein E knockout mice. TP-064 16-22 coactivator-associated arginine methyltransferase 1 Mus musculus 0-5 34785428-3 2021 Here we investigated the potential anti-atherogenic effect of PRMT4 inhibitor TP-064 in vivo. TP-064 78-84 coactivator-associated arginine methyltransferase 1 Mus musculus 62-67 34785428-5 2021 RESULTS: TP-064 induced a dose-dependent decrease in lipopolysaccharide-induced ex vivo blood monocyte Tnfalpha secretion (p < 0.05 for trend) in the context of unchanged blood monocyte concentrations and neutrophilia induction (p < 0.01 for trend). TP-064 9-15 tumor necrosis factor Mus musculus 103-111 34785428-6 2021 A dose-dependent decrease in gonadal white adipose tissue expression levels of PPARgamma target genes was detected, which translated into a reduced body weight gain after high dose TP-064 treatment (p < 0.05). TP-064 181-187 peroxisome proliferator activated receptor gamma Mus musculus 79-88 34785428-7 2021 TP-064 treatment also dose-dependently downregulated gene expression of the glycogen metabolism related protein G6pc in the liver (p < 0.001 for trend). TP-064 0-6 glucose-6-phosphatase, catalytic Mus musculus 112-116 34785428-11 2021 CONCLUSIONS: The PRMT4 inhibitor TP-064 impacts both inflammatory and metabolic processes without changing atherosclerosis susceptibility of male apolipoprotein E knockout mice. TP-064 33-39 coactivator-associated arginine methyltransferase 1 Mus musculus 17-22 34311083-0 2021 PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo. TP-064 16-22 coactivator-associated arginine methyltransferase 1 Mus musculus 0-5 34311083-2 2021 Here we investigated the effect of PRMT4 inhibitor TP-064 treatment on macrophage inflammation in vitro and in vivo. TP-064 51-57 coactivator-associated arginine methyltransferase 1 Mus musculus 35-40 34311083-4 2021 Similarly, thioglycollate-elicited peritoneal cells isolated from wildtype mice treated with TP-064 showed lowered mRNA expression levels and cytokine production of pro-inflammatory mediators interleukin (IL)-1beta, IL-6, IL-12p40, and tumor necrosis factor-alpha in response to lipopolysaccharide exposure. TP-064 93-99 interleukin 1 alpha Mus musculus 192-214 34311083-4 2021 Similarly, thioglycollate-elicited peritoneal cells isolated from wildtype mice treated with TP-064 showed lowered mRNA expression levels and cytokine production of pro-inflammatory mediators interleukin (IL)-1beta, IL-6, IL-12p40, and tumor necrosis factor-alpha in response to lipopolysaccharide exposure. TP-064 93-99 interleukin 6 Mus musculus 216-220 34311083-4 2021 Similarly, thioglycollate-elicited peritoneal cells isolated from wildtype mice treated with TP-064 showed lowered mRNA expression levels and cytokine production of pro-inflammatory mediators interleukin (IL)-1beta, IL-6, IL-12p40, and tumor necrosis factor-alpha in response to lipopolysaccharide exposure. TP-064 93-99 interleukin 12b Mus musculus 222-230 34311083-4 2021 Similarly, thioglycollate-elicited peritoneal cells isolated from wildtype mice treated with TP-064 showed lowered mRNA expression levels and cytokine production of pro-inflammatory mediators interleukin (IL)-1beta, IL-6, IL-12p40, and tumor necrosis factor-alpha in response to lipopolysaccharide exposure. TP-064 93-99 tumor necrosis factor Mus musculus 236-263 34311083-5 2021 However, TP-064-treated mice exhibited an ongoing pro-inflammatory peritonitis after 5 days of thioglycollate exposure, as evident from a shift in the peritoneal macrophage polarization state from an anti-inflammatory LY6ClowCD206hi to a pro-inflammatory LY6ChiCD206low phenotype. TP-064 9-15 lymphocyte antigen 6 complex, locus C1 Mus musculus 218-232 34311083-7 2021 TP-064 treatment downregulated hepatic mRNA expression levels of the PRMT4 target genes glucose-6-phosphatase catalytic subunit (-50%, P<0.05) and the cyclin-dependent kinases 2 (-50%, P<0.05) and 4 (-30%, P<0.05), suggesting a direct transcriptional effect of PRMT4 also in hepatocytes. TP-064 0-6 coactivator-associated arginine methyltransferase 1 Mus musculus 69-74 34311083-7 2021 TP-064 treatment downregulated hepatic mRNA expression levels of the PRMT4 target genes glucose-6-phosphatase catalytic subunit (-50%, P<0.05) and the cyclin-dependent kinases 2 (-50%, P<0.05) and 4 (-30%, P<0.05), suggesting a direct transcriptional effect of PRMT4 also in hepatocytes. TP-064 0-6 coactivator-associated arginine methyltransferase 1 Mus musculus 261-266 34311083-8 2021 In conclusion, we have shown that the PRMT4 inhibitor TP-064 induces peritonitis-associated neutrophilia in vivo and inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo. TP-064 54-60 coactivator-associated arginine methyltransferase 1 Mus musculus 38-43 34311083-9 2021 Our findings suggest that TP-064 can possibly be applied as therapy in NF-kappaB -based inflammatory diseases. TP-064 26-32 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 71-80 35245741-0 2022 Histone arginine methyltransferase CARM1 selective inhibitor TP-064 induces apoptosis in endometrial cancer. TP-064 61-67 coactivator associated arginine methyltransferase 1 Homo sapiens 35-40 35245741-3 2022 Lately, it has been suggested that CARM1 is associated with human carcinogenesis, and the CARM1-selective inhibitor, TP-064, has been shown to be a potential therapeutic agent for multiple myeloma. TP-064 117-123 coactivator associated arginine methyltransferase 1 Homo sapiens 90-95 29719619-0 2018 TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma. TP-064 0-6 coactivator associated arginine methyltransferase 1 Homo sapiens 59-64 29719619-3 2018 Here, we report the discovery of TP-064, a potent, selective, and cell-active chemical probe of human PRMT4 and its co-crystal structure with PRMT4. TP-064 33-39 coactivator associated arginine methyltransferase 1 Homo sapiens 102-107 29719619-3 2018 Here, we report the discovery of TP-064, a potent, selective, and cell-active chemical probe of human PRMT4 and its co-crystal structure with PRMT4. TP-064 33-39 coactivator associated arginine methyltransferase 1 Homo sapiens 142-147 29719619-4 2018 TP-064 inhibited the methyltransferase activity of PRMT4 with high potency (half-maximal inhibitory concentration, IC50 < 10 nM) and selectivity over other PRMT family proteins, and reduced arginine dimethylation of the PRMT4 substrates BRG1-associated factor 155 (BAF155; IC50= 340 +- 30 nM) and Mediator complex subunit 12 (MED12; IC50 = 43 +- 10 nM). TP-064 0-6 coactivator associated arginine methyltransferase 1 Homo sapiens 51-56 29719619-4 2018 TP-064 inhibited the methyltransferase activity of PRMT4 with high potency (half-maximal inhibitory concentration, IC50 < 10 nM) and selectivity over other PRMT family proteins, and reduced arginine dimethylation of the PRMT4 substrates BRG1-associated factor 155 (BAF155; IC50= 340 +- 30 nM) and Mediator complex subunit 12 (MED12; IC50 = 43 +- 10 nM). TP-064 0-6 coactivator associated arginine methyltransferase 1 Homo sapiens 223-228 29719619-4 2018 TP-064 inhibited the methyltransferase activity of PRMT4 with high potency (half-maximal inhibitory concentration, IC50 < 10 nM) and selectivity over other PRMT family proteins, and reduced arginine dimethylation of the PRMT4 substrates BRG1-associated factor 155 (BAF155; IC50= 340 +- 30 nM) and Mediator complex subunit 12 (MED12; IC50 = 43 +- 10 nM). TP-064 0-6 SWI/SNF related, matrix associated, actin dependent regulator of chromatin subfamily c member 1 Homo sapiens 240-266 29719619-4 2018 TP-064 inhibited the methyltransferase activity of PRMT4 with high potency (half-maximal inhibitory concentration, IC50 < 10 nM) and selectivity over other PRMT family proteins, and reduced arginine dimethylation of the PRMT4 substrates BRG1-associated factor 155 (BAF155; IC50= 340 +- 30 nM) and Mediator complex subunit 12 (MED12; IC50 = 43 +- 10 nM). TP-064 0-6 SWI/SNF related, matrix associated, actin dependent regulator of chromatin subfamily c member 1 Homo sapiens 268-274 29719619-4 2018 TP-064 inhibited the methyltransferase activity of PRMT4 with high potency (half-maximal inhibitory concentration, IC50 < 10 nM) and selectivity over other PRMT family proteins, and reduced arginine dimethylation of the PRMT4 substrates BRG1-associated factor 155 (BAF155; IC50= 340 +- 30 nM) and Mediator complex subunit 12 (MED12; IC50 = 43 +- 10 nM). TP-064 0-6 mediator complex subunit 12 Homo sapiens 300-327 29719619-4 2018 TP-064 inhibited the methyltransferase activity of PRMT4 with high potency (half-maximal inhibitory concentration, IC50 < 10 nM) and selectivity over other PRMT family proteins, and reduced arginine dimethylation of the PRMT4 substrates BRG1-associated factor 155 (BAF155; IC50= 340 +- 30 nM) and Mediator complex subunit 12 (MED12; IC50 = 43 +- 10 nM). TP-064 0-6 mediator complex subunit 12 Homo sapiens 329-334