CYPs
Cytochrome P450 (P450) is a superfamily of heme-thiolate enzymes that are ubiquitous in almost all biological systems. There are more than 35,000 P450 enzymes that have been isolated from all biological organisms, with exception of some primitive prokaryotes. In humans, there are 18 P450 families comprised of 60 P450 enzymes, of which the majority is microsomal P450 belong to CYP2, CYP3 and CYP4 families. Microsomal P450 enzymes are collectively described as “nature’s most versatile biological catalyst”, due to the diversity of reactions it can mediate. Most of the reactions mediated by P450 enzymes are of oxidation-reduction nature. P450s are involved in ~ 75% of the enzymatic reactions that occur in the metabolism of drugs, so there is great enthusiasm to similarly develop new drugs based on P450-mediated AA pathway.
References
1.El-Sherbeni AA,et al. Drug Metab Rev. 2017 Feb;49(1):1-17.
References
1.El-Sherbeni AA,et al. Drug Metab Rev. 2017 Feb;49(1):1-17.
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)
CYPs
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Borneol
产品货号 : M19531
cas no: 507-70-0
从肉桂中提取。它是一种 TRPM9 激动剂,可增加眼表湿度。 -
Allotropal
产品货号 : M19486
cas no: 77-75-8
3-Mmethyl-1-pentyn-3-ol 具有潜在的抑制 CYP3A 的特性。 -
Methoxsalen
产品货号 : M13918
cas no: 298-81-7
一种有效的三环呋喃香豆素自杀剂,用于治疗牛皮癣、湿疹、白癜风和一些皮肤淋巴瘤,同时将皮肤暴露在阳光下。 -
Fadrozole
产品货号 : M10129
cas no: 102676-47-1
Fadrozole (CGS 16949A free base) 是一种有效,选择性和非甾体类的?aromatase?抑制剂,IC50?值为6.4 nM。 -
Fadrozole hydrochloride
产品货号 : M10128
cas no: 102676-31-3
一种有效的、选择性的、口服生物可利用的芳香酶抑制剂,IC50 为 1.7 nM。