DHFR

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研究领域

抑制剂选择性比较

DHFR产品

所有产品 DHFR抑制剂(8)

目录号	产品描述	文献引用	实验数据
S1135	Pemetrexed Pemetrexed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。	Cell Death Dis, 2019, 10(9):660 Cells, 2019, 8(12) Lung Cancer, 2019, 139:170-178	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),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。	Cancer Cell, 2019, 36(2):179-193 Cell, 2019, 36(2):179-193 Cell Rep, 2019, 27(12):3587-3601	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。	Blood, 2018, 131(4):397-407 Cancer Cell, 2017, 31(6):833-843	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。	Cell, 2019, 178(1):160-175 Cell, 2019, 178(1):160-175 Cancer Cell, 2017, 31(6):833-843
S1618	Sulfameter Sulfameter 是一种长效的磺胺类抗菌药。
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。
S7785	Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate 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。	BMC Cancer, 2019, 19(1):108 Oncotarget, 2017, 8(14):23020-23032 Biochem Biophys Res Commun, 2015, 456(1):86-91	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。	Cell Death Dis,2019, 10(9):660 Cells,2019, 8(12) Lung Cancer,2019, 139:170-178	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),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。	Cancer Cell,2019, 36(2):179-193 Cell,2019, 36(2):179-193 Cell Rep,2019, 27(12):3587-3601	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。	Blood,2018, 131(4):397-407 Cancer Cell,2017, 31(6):833-843	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。	Cell,2019, 178(1):160-175 Cell,2019, 178(1):160-175 Cancer Cell,2017, 31(6):833-843
S1618	Sulfameter Sulfameter 是一种长效的磺胺类抗菌药。
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。
S7785	Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate 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。	BMC Cancer,2019, 19(1):108 Oncotarget,2017, 8(14):23020-23032 Biochem Biophys Res Commun,2015, 456(1):86-91	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。