Aldose Reductase
Aldose Reductase(ALR2) is a small, cytosolic, monomeric enzyme which belongs to the aldo-keto reductase superfamily. It catalyzes the NADPH dependent reduction of a wide variety of aldehydes to their corresponding alcohols, showing a broad substrate specificity and ALR2 is the key enzyme of the so called polyol pathway. Since its identification, in the early sixties, this enzyme has been always linked to the development of long term diabetic complications.It converts glucose to sorbitol, which is then oxidized to fructose by sorbitol dehydrogenase.In addition to the osmotic imbalance, an increase in the activity of the polyol pathway during hyperglycemia causes a substantial imbalance in the free cytosolic coenzyme ratios NADPH/NADP+ and NAD+/NADH, which contributes to the onset of hyperglycemic oxidative stress through the accumulation of reactive
oxygen species (ROS). ROS, in turn, trigger activation of downstream mechanisms, namely protein kinase C (PKC) isoforms, mitogen-activated protein kinases (MAPKs) and poly(ADP-ribose)polymerase (PARP), as well as the inflammatory cascade. ALR2 inhibition may be also considered a useful strategy to control pathological conditions emerging from tissue inflammation like atherosclerosis, sepsis, arthritis and also cancer.
References
1.Quattrini L,et al. Expert Opin Ther Pat. 2019 Mar;29(3):199-213.
oxygen species (ROS). ROS, in turn, trigger activation of downstream mechanisms, namely protein kinase C (PKC) isoforms, mitogen-activated protein kinases (MAPKs) and poly(ADP-ribose)polymerase (PARP), as well as the inflammatory cascade. ALR2 inhibition may be also considered a useful strategy to control pathological conditions emerging from tissue inflammation like atherosclerosis, sepsis, arthritis and also cancer.
References
1.Quattrini L,et al. Expert Opin Ther Pat. 2019 Mar;29(3):199-213.
Metabolic Enzyme/Protease
11β-HSD(15)
15-PGDH(1)
ACC(10)
ACE(15)
AChE(47)
Adenylate Cyclase(12)
ALDH(14)
Aldose Reductase(5)
Aminopeptidase(19)
BACE(19)
Casein Kinase(51)
CAT(5)
Cathepsin(9)
CETP(13)
COMT(2)
CPG2(1)
CYPs(6)
Decarboxylase(3)
Dehydrogenase(131)
DGAT(4)
Dopamine beta-hydroxylase(2)
DPP(32)
Elastase(6)
FAAH(28)
Factor Xa(31)
Fatty Acid Synthase(17)
Ftase(2)
FXR(26)
Glucokinase(1)
GSNOR(2)
Guanylate Cyclase(13)
HMGCR(17)
IDH(7)
IDO(20)
IMPDH(2)
LDH(2)
LDL(8)
Lipase(17)
Lipid(12)
MAGL(6)
MAO(72)
MMP(78)
NAMPT(12)
Neprilysin(7)
Other Targets(10)
P450(112)
PAI-1(9)
Phosphatase(95)
Phospholipase(65)
PPAR(115)
Protein Phosphatase/PTP(6)
Renin(8)
Retinoid Receptor(37)
SCD(6)
Steroid Sulfatase (STS)(2)
Thioredoxin(1)
TPH(5)
Transferase(37)
Vitamin(44)
Xanthine Oxidase (XAO)(11)
Aldose Reductase
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Epalrestat
产品货号 : M16054
cas no: 82159-09-9
一种非竞争性可逆醛糖还原酶抑制剂,对来自大鼠晶状体和人胎盘的纯化醛糖还原酶的 IC50 分别为 10 nM 和 26 nM。 -
IDD388
产品货号 : M14015
cas no: 314297-26-2
IDD388 是一种有效的醛糖还原酶(ALR2 或 AKR1B1)抑制剂,IC50 为 0.4 uM。 -
MK-204
产品货号 : M13074
cas no: 1959605-73-2
MK-204 是一种有效的选择性 AKR1B10 抑制剂,IC50 为 80 nM。 -
Fidarestat
产品货号 : M11487
cas no: 136087-85-9
Fidarestat (SNK860) 是一种有效的醛糖还原酶抑制剂。 -
Aldose reductase-IN-1
产品货号 : M11455
cas no: 1355612-71-3
一种醛糖还原酶抑制剂,IC50 为 28.9 pM。