From Wikipedia,
the free encyclopedia.
Cholesterylester transfer
protein (CETP) is a
plasma
protein that converts
high density lipoprotein (HDL)
into
intermediate density lipoprotein
(IDL). Its exact mechanism of
action is still uncertain. Apart
from converting HDL to IDL, it
also appears to mediate uptake of
HDL by the
liver.
Genetics
The CETP gene is located
on the sixteenth
chromosome (16q21).
Role in disease
Rare mutations leading to
increased function of CETP have
been linked to accelerated
atherosclerosis. In contrast,
a polymorphism of the CEPT
gene leading to lower serum levels
has also been linked to
exceptional longetivity (Barzilai
et al 2003).
Pharmacology
As HDL has a protective
function in
atherosclerosis and
cardiovascular disease, and
certain disease states (such as
the
metabolic syndrome) feature
low HDL, pharmacological
inhibition of CETP is being
studied as a method to improve HDL
levels (Barter et al 2003).
Specifically, the small molecular
agent
torcetrapib (JTT-705) has been
shown to increase HDL levels
(alone and with a statin) and
lower LDL (when co-administered
with a statin) in a 2004 study (Brousseau
et al).
References
- Barter PJ, Brewer HB Jr,
Chapman MJ, Hennekens CH, Rader
DJ, Tall AR. Cholesteryl
ester transfer protein: a novel
target for raising HDL and
inhibiting atherosclerosis.
Arterioscler Thromb Vasc Biol
2003;23:160-7.
PMID 12588754.
- Barzilai N, Atzmon G,
Schechter C, Schaefer EJ,
Cupples AL, Lipton R, Cheng S,
Shuldiner AR. Unique
lipoprotein phenotype and
genotype associated with
exceptional longevity. JAMA
2003;290:2030-40.
PMID 14559957.
- Brousseau ME, Schaefer EJ,
Wolfe ML, Bloedon LT, Digenio
AG, Clark RW, Mancuso JP, Rader
DJ. Effects of an inhibitor
of cholesteryl ester transfer
protein on HDL cholesterol.
N Engl J Med 2004;350:1505-15.
PMID 15071125.
