DHFR

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研究领域

抑制剂选择性比较

DHFR产品

所有产品(7) DHFR抑制剂(7)

目录号	产品描述	文献引用	实验数据
S1135	Pemetrexed Pemetrexed (LY-231514) 是一种新型抗叶酸和抗代谢药物，作用于TS，DHFR和GARFT，无细胞试验中K_i分别为1.3 nM，7.2 nM 和65 nM。Pemetrexed 可诱导自噬和细胞凋亡。	Nat Commun, 2020, 14;11(1):1825 J Hematol Oncol, 2020, 1;13(1):40 Cell Death Dis, 2020, 11(11):945	Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
S1210	Methotrexate Methotrexate (MTX, NCI-C04671),一种叶酸类似物，是细菌、癌细胞和正常细胞中dihydrofolate reductase(DHFR)的非选择性抑制剂，与DHFR、NADPH形成无活性的三元复合物。Methotrexate (MTX)可诱导凋亡。	Gastroenterology, 2020, 159(6):2203-2220.e14 Anal Chem, 2020, 10.1021/acs.analchem.0c02756 Toxicol Sci, 2020, 10.1093/toxsci/kfaa014	Toxicity of MTX (3) and toxic analogues 5 a-e on a) hY1R-expressing MDA-MB-468 and b) non-hYR-expressing HEK293 cells. Cell viability was determined by resazurin assay. Bars represent the mean±SEM of at least three independent experiments performed in triplicate. Measurements were normalized by using only HBSS, pH 7, treated cells (set at 100 %) and ethanol-treated cells (set at 0 %). Statistical significances refer to only HBSS, pH 7, treated cells indicated as a dashed line.
S1497	Pralatrexate Pralatrexate 是一种抗叶酸药，结构与叶酸类似，作用于一些细胞系，IC50低于300 nM。Pralatrexate 可诱导肿瘤细胞的凋亡。	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8	PK parameters for pralatrexate in the study population. Concentration over time for each dose cohort of pralatrexate (A).
S2006	Pyrimethamine Pyrimethamine是二氢叶酸还原酶(DHFR)抑制剂，用作抗疟药。	PLoS Pathog, 2020, 16;16(3):e1008341 Cell, 2019, 178(1):160-175 Cell, 2019, 178(1):160-175
S5097	Methotrexate disodium Methotrexate sodium是tetrahydrofolate dehydrogenase的抑制剂，是一种抗肿瘤抗代谢药，具有免疫抑制活性。	Gastroenterology, 2020, 159(6):2203-2220.e14 Oncol Lett, 2018, 15(5):6107-6114 J Med Chem, 2016, 59(7):3409-17
S7785	Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate (LY-231514) 培美曲塞是一种新型抗叶酸剂和抗代谢物质，作用于TS，DHFR 和 GARFT，K_i分别为1.3 nM，7.2 nM 和 65 nM。Pemetrexed Disodium Hydrate 可刺激细胞自噬和凋亡。	J Cell Mol Med, 2020, 24(10):5811-5816 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z	Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
S5200	Diaveridine Diaveridine (AI3-23935, CCRIS-3784) 是一种球虫抑制药，具有抗寄生虫活性，是dihydrofolate reductase (DHFR)抑制剂，在肺囊虫属中抑制叶酸合成。

目录号	产品描述	文献引用	实验数据
S1135	Pemetrexed Pemetrexed (LY-231514) 是一种新型抗叶酸和抗代谢药物，作用于TS，DHFR和GARFT，无细胞试验中K_i分别为1.3 nM，7.2 nM 和65 nM。Pemetrexed 可诱导自噬和细胞凋亡。	Nat Commun,2020, 14;11(1):1825 J Hematol Oncol,2020, 1;13(1):40 Cell Death Dis,2020, 11(11):945	Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
S1210	Methotrexate Methotrexate (MTX, NCI-C04671),一种叶酸类似物，是细菌、癌细胞和正常细胞中dihydrofolate reductase(DHFR)的非选择性抑制剂，与DHFR、NADPH形成无活性的三元复合物。Methotrexate (MTX)可诱导凋亡。	Gastroenterology,2020, 159(6):2203-2220.e14 Anal Chem,2020, 10.1021/acs.analchem.0c02756 Toxicol Sci,2020, 10.1093/toxsci/kfaa014	Toxicity of MTX (3) and toxic analogues 5 a-e on a) hY1R-expressing MDA-MB-468 and b) non-hYR-expressing HEK293 cells. Cell viability was determined by resazurin assay. Bars represent the mean±SEM of at least three independent experiments performed in triplicate. Measurements were normalized by using only HBSS, pH 7, treated cells (set at 100 %) and ethanol-treated cells (set at 0 %). Statistical significances refer to only HBSS, pH 7, treated cells indicated as a dashed line.
S1497	Pralatrexate Pralatrexate 是一种抗叶酸药，结构与叶酸类似，作用于一些细胞系，IC50低于300 nM。Pralatrexate 可诱导肿瘤细胞的凋亡。	Cancer Cell Int,2020, 19;20:58 Hum Cell,2020, 10.1007/s13577-020-00420-z Hum Cell,2020, 10.1007/s13577-020-00425-8	PK parameters for pralatrexate in the study population. Concentration over time for each dose cohort of pralatrexate (A).
S2006	Pyrimethamine Pyrimethamine是二氢叶酸还原酶(DHFR)抑制剂，用作抗疟药。	PLoS Pathog,2020, 16;16(3):e1008341 Cell,2019, 178(1):160-175 Cell,2019, 178(1):160-175
S5097	Methotrexate disodium Methotrexate sodium是tetrahydrofolate dehydrogenase的抑制剂，是一种抗肿瘤抗代谢药，具有免疫抑制活性。	Gastroenterology,2020, 159(6):2203-2220.e14 Oncol Lett,2018, 15(5):6107-6114 J Med Chem,2016, 59(7):3409-17
S7785	Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate (LY-231514) 培美曲塞是一种新型抗叶酸剂和抗代谢物质，作用于TS，DHFR 和 GARFT，K_i分别为1.3 nM，7.2 nM 和 65 nM。Pemetrexed Disodium Hydrate 可刺激细胞自噬和凋亡。	J Cell Mol Med,2020, 24(10):5811-5816 Cancer Cell Int,2020, 19;20:58 Hum Cell,2020, 10.1007/s13577-020-00420-z	Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
S5200	Diaveridine Diaveridine (AI3-23935, CCRIS-3784) 是一种球虫抑制药，具有抗寄生虫活性，是dihydrofolate reductase (DHFR)抑制剂，在肺囊虫属中抑制叶酸合成。