DHFR
信号通路图
研究领域
抑制剂选择性比较
DHFR产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1135 |
Pemetrexed (LY-231514) disodiumPemetrexed (LY-231514) disodium 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Ki分别为1.3 nM，7.2 nM 和65 nM。Pemetrexed 可诱导自噬和细胞凋亡。 |
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 (CL-14377)Methotrexate (CL14377, MTX, NCI-C04671, Amethopterin, WR19039),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。 |
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 (NSC 754230)Pralatrexate (NSC 754230)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。 |
PK parameters for pralatrexate in the study population. Concentration over time for each dose cohort of pralatrexate (A).
|
|
| S2006 |
PyrimethaminePyrimethamine是二氢叶酸还原酶(DHFR)抑制剂，用作抗疟药。 |
||
| S5971New |
PemetrexedPemetrexed (LY231514, Alimta) 是一种新型的抗叶酸和抗代谢药物，针对 thymidylate synthase (TS)、dihydrofolate reductase (DHFR) 和 glycinamide ribonucleotide formyltransferase (GARFT) 在无细胞试验中，对应的Ki值分别为1.3 nM、7.2 nM和65 nM。Pemetrexed 可诱导自噬和细胞凋亡。 |
||
| S2588New |
Calcium LevofolinateCalcium Levofolinate (Calcium Folinate, Levoleucovorin calcium, CL307782) 是Folinic acid的钙盐，是用于癌症化疗的佐剂。 |
||
| S3129 |
TrimethoprimTrimethoprim (BW 56-72, NIH 204, NSC-106568) 是一种抑制细菌的抗生素，主要用于预防和治疗尿路感染。 |
||
| S5097 |
Methotrexate disodiumMethotrexate 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 HydratePemetrexed 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，Ki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。 |
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.
|
|
| S5927 |
ProguanilProguanil (chlorguanide, chloroguanide) 是预防性抗疟药。它能抑制疟原虫的二氢叶酸还原酶，阻止嘌呤和嘧啶的合成。 |
||
| S5200 |
DiaveridineDiaveridine (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。 |
||
| S5136 |
Calcium folinateCalcium folinate (Leucovorin calcium, Folinic acid calcium salt, Wellcovorin) is a metabolically active, reduced form of folic acid that is rapidly absorbed and extensively metabolized in the liver to other folic acid derivatives. |
||
| S0320 |
Cycloguanil hydrochlorideCycloguanil hydrochloride is an active metabolite of Proguanil. Cycloguanil hydrochloride acts on malaria schizonts in erythrocytes and hepatocytes. |
||
| S1236 |
Leucovorin (NSC -3590) Calcium PentahydrateLeucovorin Calcium Pentahydrate (NSC -3590, Folinic acid)是一种亚叶酸, 用于改善叶酸下降的状况。 |
||
| S0854 |
MetoprineMetoprine (BW 197U), a diaminopyrimidine derivative, is a potent inhibitor of histamine N-methyltransferase (HMT) that crosses the blood-brain barrier and increases brain histamine levels. Metoprine is an antifolate and antitumor agent. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1135 |
Pemetrexed (LY-231514) disodiumPemetrexed (LY-231514) disodium 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Ki分别为1.3 nM，7.2 nM 和65 nM。Pemetrexed 可诱导自噬和细胞凋亡。 |
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 (CL-14377)Methotrexate (CL14377, MTX, NCI-C04671, Amethopterin, WR19039),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。 |
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 (NSC 754230)Pralatrexate (NSC 754230)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。 |
PK parameters for pralatrexate in the study population. Concentration over time for each dose cohort of pralatrexate (A).
|
|
| S2006 |
PyrimethaminePyrimethamine是二氢叶酸还原酶(DHFR)抑制剂，用作抗疟药。 |
||
| S5971New |
PemetrexedPemetrexed (LY231514, Alimta) 是一种新型的抗叶酸和抗代谢药物，针对 thymidylate synthase (TS)、dihydrofolate reductase (DHFR) 和 glycinamide ribonucleotide formyltransferase (GARFT) 在无细胞试验中，对应的Ki值分别为1.3 nM、7.2 nM和65 nM。Pemetrexed 可诱导自噬和细胞凋亡。 |
||
| S2588New |
Calcium LevofolinateCalcium Levofolinate (Calcium Folinate, Levoleucovorin calcium, CL307782) 是Folinic acid的钙盐，是用于癌症化疗的佐剂。 |
||
| S3129 |
TrimethoprimTrimethoprim (BW 56-72, NIH 204, NSC-106568) 是一种抑制细菌的抗生素，主要用于预防和治疗尿路感染。 |
||
| S5097 |
Methotrexate disodiumMethotrexate 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 HydratePemetrexed 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，Ki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。 |
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.
|
|
| S5927 |
ProguanilProguanil (chlorguanide, chloroguanide) 是预防性抗疟药。它能抑制疟原虫的二氢叶酸还原酶，阻止嘌呤和嘧啶的合成。 |
||
| S5200 |
DiaveridineDiaveridine (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。 |
||
| S5136 |
Calcium folinateCalcium folinate (Leucovorin calcium, Folinic acid calcium salt, Wellcovorin) is a metabolically active, reduced form of folic acid that is rapidly absorbed and extensively metabolized in the liver to other folic acid derivatives. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S0320 |
Cycloguanil hydrochlorideCycloguanil hydrochloride is an active metabolite of Proguanil. Cycloguanil hydrochloride acts on malaria schizonts in erythrocytes and hepatocytes. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1236 |
Leucovorin (NSC -3590) Calcium PentahydrateLeucovorin Calcium Pentahydrate (NSC -3590, Folinic acid)是一种亚叶酸, 用于改善叶酸下降的状况。 |
||
| S0854 |
MetoprineMetoprine (BW 197U), a diaminopyrimidine derivative, is a potent inhibitor of histamine N-methyltransferase (HMT) that crosses the blood-brain barrier and increases brain histamine levels. Metoprine is an antifolate and antitumor agent. |
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