Related Experiment Video

Updated: Jan 31, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
09:11

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

7.0K

Is Anacetrapib Better Than Its CETP Inhibitor Counterparts?

Mordechai Grabie1, Cheng-Hung Tai2, William H Frishman3

  • 1From the Departments of Medicine, Hofstra-Northwell School of Medicine, Manhasset, NY.

Cardiology in Review
|January 3, 2019
PubMed

Insights

Cholesterol metabolism research is vital for cardiovascular disease prevention. New cholesteryl ester transfer protein (CETP) inhibitors, like anacetrapib, show promise in reducing heart disease risk where statins have limitations.

Area of Science:

  • Cardiovascular Science
  • Metabolic Research
  • Pharmacology

Background:

  • Cardiovascular disease (CVD) remains a leading cause of mortality in the US.
  • Hydroxymethylglutaryl-CoA reductase inhibitors (statins) are primary agents for CVD risk reduction.
  • Despite statin efficacy, further interventions are needed to decrease CVD incidence and mortality.

Purpose of the Study:

  • To review high-density lipoprotein (HDL) metabolism and transport.
  • To examine the role and potential of cholesteryl ester transfer protein (CETP) inhibitors in CVD risk modification.

Main Methods:

  • Literature review focusing on HDL metabolism.
  • Analysis of clinical trial data for CETP inhibitors.
  • Evaluation of anacetrapib's efficacy and safety profile.

Main Results:

  • Previous CETP inhibitors have not demonstrated significant CVD risk reduction.
  • Anacetrapib, a novel CETP inhibitor, presents potentially improved outcomes.
  • Further investigation into anacetrapib's cardiovascular benefits is warranted.

Conclusions:

  • Targeting HDL metabolism via CETP inhibition is a potential strategy for CVD risk reduction.
  • Anacetrapib may offer a promising therapeutic avenue beyond current statin therapies.
  • Continued research is essential to validate anacetrapib's role in preventing cardiovascular events.

More Related Videos

Author Spotlight: Advancing Therapeutics to Treat Vibriosis in Humans and Aquatic Organisms03:29

Author Spotlight: Advancing Therapeutics to Treat Vibriosis in Humans and Aquatic Organisms

Published on: May 31, 2024

950
Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

11.8K

Related Concept Videos

Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
11.0K
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
667
Antihypertensive Drugs: Direct Renin Inhibitors01:25

Antihypertensive Drugs: Direct Renin Inhibitors

The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...
1.5K
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors01:30

Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors

Angiotensin-converting enzyme (ACE), a vital component of the renin-angiotensin-aldosterone system, is abundant in lung endothelial cells. ACE converts the inactive decapeptide, angiotensin I, into the active octapeptide, angiotensin II. This potent vasoconstrictor narrows blood vessels, increasing resistance to blood flow and elevating blood pressure. Angiotensin II also stimulates aldosterone production, encouraging kidney cells to reabsorb more sodium and water from urine, thereby increasing...
2.5K
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
600
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
575