Pharmacological modulation of cholesterol 7α-hydroxylase (CYP7A1) as a therapeutic strategy for hypercholesterolemia

MYC Lim, HK Ho - Biochemical Pharmacology, 2023 - Elsevier
Despite the availability of many therapeutic options, the prevalence of hypercholesterolemia
remains high. There exists a significant unmet medical need for novel drugs and/or …

Regulation of cholesterol-7α-hydroxylase: BAREly missing a SHP

RA Davis, JH Miyake, TY Hui, NJ Spann - Journal of lipid research, 2002 - ASBMB
Abstract Cholesterol-7α-hydroxylase (CYP7A1) regulates the pathway through which
cholesterol is converted into bile acids. The unique detergent properties of bile acids are …

[PDF][PDF] Overexpression of cholesterol 7α‐hydroxylase promotes hepatic bile acid synthesis and secretion and maintains cholesterol homeostasis

T Li, M Matozel, S Boehme, B Kong, LM Nilsson… - …, 2011 - Wiley Online Library
We reported previously that mice overexpressing cytochrome P450 7a1 (Cyp7a1; Cyp7a1‐
tg mice) are protected against high fat diet–induced hypercholesterolemia, obesity, and …

Down-regulation of cholesterol 7α-hydroxylase (CYP7A1) gene expression by bile acids in primary rat hepatocytes is mediated by the c-Jun N-terminal kinase …

S Gupta, RT Stravitz, P Dent, PB Hylemon - Journal of Biological Chemistry, 2001 - ASBMB
Cholesterol 7α-hydroxylase (CYP7A1), the rate-limiting enzyme in the neutral pathway of
bile acid biosynthesis, is feedback-inhibited at the transcriptional level by hydrophobic bile …

Advances in understanding the regulatory mechanism of cholesterol 7α-hydroxylase

M Ge, R Shao, H He - Biochemical pharmacology, 2019 - Elsevier
The conversion of cholesterol to bile acids (BAs) contributes to the elimination of total
cholesterol from the body. In addition, manipulating BA homeostasis by modulating …

Retinoic acid represses CYP7A1 expression in human hepatocytes and HepG2 cells by FXR/RXR-dependent and independent mechanisms

SY Cai, H He, T Nguyen, A Mennone, JL Boyer - Journal of lipid research, 2010 - ASBMB
Cholesterol 7α-hydroxylase (CYP7A1) plays a key role in maintaining lipid and bile salt
homeostasis as it is the rate-limiting enzyme converting cholesterol to bile acids. Deficiency …

Cholesterol 7α-hydroxylase protects the liver from inflammation and fibrosis by maintaining cholesterol homeostasis [S]

H Liu, P Pathak, S Boehme, JYL Chiang - Journal of lipid research, 2016 - ASBMB
Cholesterol 7α-hydroxylase (CYP7A1) plays a critical role in control of bile acid and
cholesterol homeostasis. Bile acids activate farnesoid X receptor (FXR) and Takeda G …

The pharmacological exploitation of cholesterol 7α-hydroxylase, the key enzyme in bile acid synthesis: from binding resins to chromatin remodelling to reduce plasma …

F Gilardi, N Mitro, C Godio, E Scotti, D Caruso… - Pharmacology & …, 2007 - Elsevier
Mammals dispose of cholesterol mainly through 7α-hydroxylated bile acids, and the enzyme
catalyzing the 7α-hydroxylation, cholesterol 7α-hydroxylase (CYP7A1), has a deep impact …

[HTML][HTML] An FXR agonist reduces bile acid synthesis independently of increases in FGF19 in healthy volunteers

A Al-Khaifi, M Rudling, B Angelin - Gastroenterology, 2018 - Elsevier
Bile acid (BA) synthesis is regulated through suppression of hepatic cholesterol 7α-
hydroxylase via farnesoid X receptor (FXR) activation in hepatocytes and/or enterocytes; in …

[HTML][HTML] Up to date on cholesterol 7 alpha-hydroxylase (CYP7A1) in bile acid synthesis

JYL Chiang, JM Ferrell - Liver research, 2020 - Elsevier
Abstract Cholesterol 7 alpha-hydroxylase (CYP7A1, EC1. 14) is the first and rate-limiting
enzyme in the classic bile acid synthesis pathway. Much progress has been made in …