Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Lipid-Lowering Drugs: Statins and Miscellaneous Agents01:20

Lipid-Lowering Drugs: Statins and Miscellaneous Agents

1.7K
Hyperlipidemia, a medical condition often referred to as high cholesterol, is characterized by abnormally elevated levels of lipids in the bloodstream. When present in excess, these lipids, specifically cholesterol and triglycerides, can lead to serious health complications, often involving cardiovascular diseases. Illnesses like atherosclerosis, heart attacks, and pancreatitis have all been linked to untreated hyperlipidemia. This means controlling and regulating cholesterol and triglyceride...
1.7K
Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

290
After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
290
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

292
Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
292
Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

411
Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
411
Pharmaceutical Alternatives: Stability-Related Therapeutic Nonequivalence01:22

Pharmaceutical Alternatives: Stability-Related Therapeutic Nonequivalence

235
Generic intravenous (IV) drugs are considered bioequivalent to their branded counterparts due to their 100% bioavailability upon administration. However, variations in stability among different drug products can significantly influence their therapeutic performance, even if they are pharmaceutically equivalent.Cefuroxime, a prophylactic antimicrobial, is often used as a single-dose IV injection for patients undergoing coronary artery bypass grafting surgery. A 3 g dose typically provides...
235
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

579
Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
579

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Automated irrigation systems in mitigating laser-induced temperature during simulated ureteroscopy.

BJU international·2026
Same author

3-Hydroxypyrimidine-2,4-dione derivatives as monkeypox virus resolvase (Mpr) inhibitors.

RSC medicinal chemistry·2026
Same author

Driving mechanisms of adaptive strategies and heavy metal remediation potential in Artemisia lavandulaefolia during succession of abandoned Pb-Zn mining areas.

Journal of environmental management·2026
Same author

Psychedelic Use, Microdosing, Motives, and Information and Product Sources Among Young Adults in the United States.

Journal of psychoactive drugs·2026
Same author

Discovery and characterization of a hydroxypyridone-3-carboxamide analog as an antiviral lead against orthopoxviruses.

Antimicrobial agents and chemotherapy·2026
Same author

Emergence of Task-Related Motor Cortical Dysfunction in Mice with Progressive Parkinsonism.

bioRxiv : the preprint server for biology·2026

Related Experiment Video

Updated: Mar 13, 2026

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
09:15

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles

Published on: November 10, 2017

15.2K

Eeyarestatin I derivatives with improved aqueous solubility.

Rui Ding1, Ting Zhang2, Jiashu Xie1

  • 1Center for Drug Design, Academic Health Center, University of Minnesota, Minneapolis, MN 55455, United States.

Bioorganic & Medicinal Chemistry Letters
|October 13, 2016
PubMed
Summary

Researchers developed new Eeyarestatin I (EerI) derivatives to improve cancer therapy. These compounds target p97 (valosin-containing protein) with better solubility for potential in vivo use.

Keywords:
EerIEeyarestatin ISolubilityVCPValosin-containing proteinp97

More Related Videos

Stabilizing Hepatocellular Phenotype Using Optimized Synthetic Surfaces
08:50

Stabilizing Hepatocellular Phenotype Using Optimized Synthetic Surfaces

Published on: September 26, 2014

10.7K
Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
08:18

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Published on: July 27, 2022

1.7K

Related Experiment Videos

Last Updated: Mar 13, 2026

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
09:15

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles

Published on: November 10, 2017

15.2K
Stabilizing Hepatocellular Phenotype Using Optimized Synthetic Surfaces
08:50

Stabilizing Hepatocellular Phenotype Using Optimized Synthetic Surfaces

Published on: September 26, 2014

10.7K
Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
08:18

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Published on: July 27, 2022

1.7K

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Therapeutics

Background:

  • p97 (valosin-containing protein/VCP) inhibition is a validated cancer therapy strategy.
  • Eeyarestatin I (EerI) inhibits p97 via a novel mechanism and shows anti-cancer effects in vitro.
  • Poor aqueous solubility of EerI limits its in vivo application.

Purpose of the Study:

  • To develop EerI derivatives with enhanced aqueous solubility.
  • To assess the in vitro anti-cancer activities and metabolic properties of these derivatives.

Main Methods:

  • Chemical modification of EerI by introducing a single solubilizing group.
  • Evaluation of endoplasmic reticulum (ER) stress induction.
  • Assessment of antiproliferative activity against cancer cells.
  • In vitro metabolic stability testing.

Main Results:

  • Novel EerI derivatives with significantly improved aqueous solubility were identified.
  • These derivatives retained ER stress-inducing and antiproliferative activities.
  • Generally favorable in vitro metabolic profiles were observed for the modified compounds.

Conclusions:

  • The developed EerI derivatives represent promising candidates for further optimization in cancer therapy.
  • Improved solubility addresses a key limitation for potential in vivo efficacy.
  • These compounds warrant further investigation for their therapeutic potential.