Xie, Haibo Yang, Ka Winston-McPherson, Gabrielle N Stapleton, Donnie S Keller, Mark P Attie, Alan D Smith, Kerry A Tang, Weiping
Published in
European journal of medicinal chemistry
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a recently validated therapeutic target for lowering low-density lipoprotein cholesterol (LDL-C). Through phenotypic screening, we previously discovered a class of small-molecules with a 2,3'-diindolymethane (DIM) skeleton that can decrease the expression of PCSK9. But these compounds have lo...
Doggrell, Sheila A.
Introduction: If statins are unsuccessful at achieving the LDL cholesterol level goal in subjects with hypercholesterolemia, non-statin therapy should be added to reduce cardiovascular morbidity and mortality. The first inhibitors of proprotein convertase substilisin-kexin type 9 (PCSK9) were human monoclonal antibodies and these reduced LDL choles...
Abdelwahed, Khaldoun S Siddique, Abu Bakar Mohyeldin, Mohamed M Qusa, Mohammed H Goda, Amira A Singh, Sitanshu S Ayoub, Nehad M King, Judy Ann Jois, Seetharama D El Sayed, Khalid A
...
Published in
Pharmacological research
Hypercholesterolemia has been documented to drive hormone-dependent breast cancer (BC) progression and resistance to hormonal therapy. Proprotein convertase subtilisin/kexin type-9 (PCSK9) regulates cholesterol metabolism through binding to LDL receptor (LDLR) and targeting the receptor for lysosomal degradation. Inhibition of PCSK9 is an establish...
Liu, Shijie Deng, Xiaoyan Zhang, Peng Wang, Xianwei Fan, Yubo Zhou, Sichang Mu, Shengyu Mehta, Jawahar L Ding, Zufeng
Published in
Cardiovascular research
Blood flow patterns play an important role in the localization of atherosclerosis in the sense that low-flow state is pro-atherogenic, and helical flow is protective against atherosclerosis. Proprotein convertase subtilisin/kexin type 9 (PCSK9) regulates cholesterol metabolism via low-density lipoprotein receptor (LDLr) degradation and is highly ex...
Toth, Stefan Pella, Dominik Fedacko, Jan
Published in
Cardiology and Therapy
Despite progress in both primary and secondary prevention, cardiovascular diseases (CVD) are still the largest group of ailments contributing to morbidity and mortality worldwide. Atherosclerotic changes, the primary pathological substrate for CVD, are closely related to hypercholesterolemia. Therefore, the treatment of hypercholesterolemia is a ke...
Leopold, Jane A
Published in
JACC. Basic to translational science
Roth, Eli M Kastelein, John J P Cannon, Christopher P Farnier, Michel McKenney, James M DiCioccio, A Thomas Brunet, Aurélie Manvelian, Garen Sasiela, William J Baccara-Dinet, Marie T
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Published in
Journal of clinical lipidology
The ODYSSEY CHOICE I study (NCT01926782) evaluated alirocumab 300 mg every 4 weeks (Q4W) in patients with hypercholesterolemia receiving maximally tolerated statin or no statin. The objective of the study was to assess the relationship between alirocumab, proprotein convertase subtilisin/kexin type 9 (PCSK9), and low-density lipoprotein cholesterol...
Nergiz-Unal, Reyhan Ulug, Elif Kisioglu, Betul Tamer, Funda Bodur, Mahmut Yalcimin, Hacer Yuruk, Armagan Aytug
Published in
Nutrition (Burbank, Los Angeles County, Calif.)
The aim of this study was to investigate the uncertain effects of high saturated fatty acids (SFAs) or fructose intake on cholesterol and lipoproteins with an insight of proprotein convertase subtilisin/kexin type 9 (PCSK9)- and cluster of differentiation 36 (CD36)-induced mechanisms. Forty male C57 BL/6 mice (8 wks of age) were divided into four g...
Thompson, Gilbert R
Published in
Journal of lipid research
AbstractAfter training as a gastroenterologist in the UK the author became interested in lipidology while he was a research fellow in the USA and switched careers after returning home. Together with Nick Myant he introduced the use of plasma exchange to treat FH homozygotes and undertook non-steady state studies of LDL kinetics, which showed that t...
Kuo, Wan-chin Stevens, Jennifer M. Ersig, Anne L. Johnson, Heather M. Tung, Tsan-Hua Bratzke, Lisa C.
Published in
Current Atherosclerosis Reports
Purpose of ReviewHigher plasma proprotein convertase subtilisin/kexin type 9 (PCSK9) concentration has been associated with a higher risk of atherosclerotic cardiovascular disease (ASCVD). Animal and human studies have examined the relationship between 24-h activity cycles (24-HAC) and PCSK9, but conflicting results exist. Therefore, this review ai...
