Modeling an active conformation for linear peptides and design of a competitive inhibitor for HMG‐CoA reductase

2008 ◽  
Vol 21 (4) ◽  
pp. 224-232 ◽  
Author(s):  
Valeriy V. Pak ◽  
Minseon Koo ◽  
Min Jung Kim ◽  
Hye Jeong Yang ◽  
Lyubov Yun ◽  
...  
Keyword(s):  
Competitive Inhibitor ◽  
Active Conformation ◽  
Hmg Coa Reductase ◽  
Coa Reductase

Recognized sequence and conformation in design of linear peptides as a competitive inhibitor for HMG-CoA reductase

2007 ◽  
Vol 20 (3) ◽  
pp. 197-203 ◽  
Author(s):  
Valeriy V. Pak ◽  
Minseon Koo ◽  
Lyubov Yun ◽  
Dae Young Kwon
Keyword(s):  
Competitive Inhibitor ◽  
Hmg Coa Reductase ◽  
Coa Reductase

scholarly journals Interaction Between Mevalonate Pathway and Retinoic Acid-Induced Differentiation

2001 ◽  
Vol 1 (3) ◽  
pp. 108-113 ◽  
Author(s):  
Naima Gueddari-Pouzols ◽  
Patrick Duriez ◽  
Christine Chomienne ◽  
Aurélie Trussardi ◽  
Jean Claude Jardillier
Keyword(s):  
Retinoic Acid ◽  
Cell Differentiation ◽  
Mevalonate Pathway ◽  
Competitive Inhibitor ◽  
Farnesyltransferase Inhibitors ◽  
Differentiation Process ◽  
Induced Differentiation ◽  
Hmg Coa Reductase ◽  
Potent Inducer ◽  
Coa Reductase

Alltransretinoic acid (ATRA) is a potent inducer of differentiation of HL-60 cell line. The pretreatment of the cells by compactin, a competitive inhibitor of 3-hydroxy-3-methylglutaryl (HMG) CoA reductase, during 24 hours, enhances the ATRA-induced cell differentiation. At 50 nM, the percentage of cell differentiation is 34.9% ± 2 and 73% ± 2.96 in the control and compactin-treated cells, respectively. The removal of compactin boosts the level of HMG-CoA reductase and therefore the biosynthesis of sterol and nonsterol isoprenoid compounds. The participation of sterol and nonsterol pathway was then investigated. The supply of an excess of cholesterol (up to 80 μg/ml of LDL) leads to a significant decrease of cell differentiation by ATRA from 78% ±0.1 to 54% ±2.8. A concomitant decrease of cell growth (51% ± 6.4) was observed. The pretreatment of cells by the geranylgeranyltransferase inhibitor (GGTI-298) has no effect on the cell differentiation process. By contrast, the farnesyltransferase inhibitors (FTI-II and FTI-277) completely abolish theATRA-induced differentiation, thus confirming the involvement of farnesylated proteins in the differentiation mechanism.

Design of Tripeptides as a Competitive Inhibitor for HMG-CoA Reductase

2021 ◽  
Author(s):  
Valeriy V. Pak ◽  
Dae Yong Kwon ◽  
Olim K. Khojimatov ◽  
Aleksandr V. Pak ◽  
Shomansur Sh. Sagdullaev
Keyword(s):  
Competitive Inhibitor ◽  
Hmg Coa Reductase ◽  
Coa Reductase

Peptide design of a competitive inhibitor for HMG-CoA reductase based on statin structure

Biopolymers ◽  
2006 ◽  
Vol 84 (6) ◽  
pp. 586-594 ◽  
Author(s):  
Valeriy V. Pak ◽  
Sung Hee Kim ◽  
Minseon Koo ◽  
Nari Lee ◽  
K. M. Shakhidoyatov ◽  
...  
Keyword(s):  
Competitive Inhibitor ◽  
Peptide Design ◽  
Hmg Coa Reductase ◽  
Coa Reductase

Simvastatin, a competitive inhibitor of HMG-CoA reductase, lowers cholesterol saturation index of gallbladder bile

Hepatology ◽  
1988 ◽  
Vol 8 (5) ◽  
pp. 1147-1150 ◽  
Author(s):  
William C. Duane ◽  
Donald B. Hunninghake ◽  
Martin L. Freeman ◽  
Pete A. Pooler ◽  
Linda A. Schlasner ◽  
...  
Keyword(s):  
Saturation Index ◽  
Competitive Inhibitor ◽  
Gallbladder Bile ◽  
Hmg Coa Reductase ◽  
Cholesterol Saturation ◽  
Cholesterol Saturation Index ◽  
Coa Reductase

Ultrastructural analysis of crystalloid endoplasmic reticulum in UT-1 cells and its disappearance in response to cholesterol

1983 ◽  
Vol 63 (1) ◽  
pp. 1-20 ◽  
Author(s):  
R.G. Anderson ◽  
L. Orci ◽  
M.S. Brown ◽  
L.M. Garcia-Segura ◽  
J.L. Goldstein
Keyword(s):  
Endoplasmic Reticulum ◽  
Chinese Hamster Ovary Cells ◽  
Membrane Surface ◽  
Freeze Fracture ◽  
Chinese Hamster ◽  
Competitive Inhibitor ◽  
Morphological Evidence ◽  
Hmg Coa Reductase ◽  
Membrane Area ◽  
Coa Reductase

The crystalloid endoplasmic reticulum (ER) consists of hexagonally packed membrane tubules that contain 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG CoA reductase), an intrinsic membrane protein that catalyses the rate-limiting step in cholesterol synthesis. The crystalloid ER appears in a clone of Chinese hamster ovary cells, designated UT-1, that contain high levels of HMG CoA reductase as a result of growth in the presence of compactin, a competitive inhibitor of the reductase. In the present studies, we have used ultrastructural morphometry to estimate that the crystalloid ER: (1) occupies about 15% of the volume of UT-1 cells; (2) contains 3.4-fold more membrane area than the plasma membrane; and (3) contains less than 700 subunits of HMG CoA reductase per micrometer2 of membrane surface. The crystalloid ER tubules contain 2000 intramembrane particles per micrometer2 with a mean diameter of 10.4 nm, as determined by freeze-fracture. The crystalloid ER membranes are low in cholesterol, as indicated by the small number of filipin-cholesterol complexes in freeze-fracture images after treatment with filipin. The addition of cholesterol or related sterols to UT-1 cells promoted a rapid and stepwise disappearance of the crystalloid ER. Initially, the crystalloid ER fragmented into randomly arranged vesicles and tubules. Subsequently, membrane-bound structures disappeared from the cell so that after incubation with cholesterol for 24–72 h, the cells appeared completely normal. We found no morphological evidence that autophagic vacuoles participate in the degradation. We conclude: (1) that the crystalloid ER is more extensive than necessary merely to support HMG CoA reductase; and (2) that upon exposure to cholesterol the crystalloid ER is degraded by a process that does not involve autophagy.

Design of a highly potent inhibitory peptide acting as a competitive inhibitor of HMG-CoA reductase

Amino Acids ◽  
2012 ◽  
Vol 43 (5) ◽  
pp. 2015-2025 ◽  
Author(s):  
Valeriy V. Pak ◽  
Minseon Koo ◽  
Dae Young Kwon ◽  
Lyubov Yun
Keyword(s):  
Competitive Inhibitor ◽  
Inhibitory Peptide ◽  
Hmg Coa Reductase ◽  
Coa Reductase

Reduction of HMG-CoA-reductase leads to improved cardiac function in doxorubicin-induced cardiomyopathy in mice

2008 ◽  
Vol 7 ◽  
pp. 202-203
Author(s):  
A RIAD ◽  
S BIEN ◽  
F ESCHER ◽  
D WESTERMANN ◽  
U LANDMESSER ◽  
...  
Keyword(s):  
Cardiac Function ◽  
Hmg Coa Reductase ◽  
Coa Reductase
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