P-Glycoprotein Inhibition; the Past, the Present and the Future.

02:22 EDT 2nd August 2015 | BioPortfolio

Summary of "P-Glycoprotein Inhibition; the Past, the Present and the Future."

The multidrug resistant phenotype of cancer cells can often result from the over-production of a number of ATP binding cassette (ABC) transporters, including P-glycoprotein (P-gp). These multi-drug efflux transporters expel administered anti-cancer drugs from the cancer cell, preventing sufficient intracellular drug accumulation and ultimately, drug efficacy. The co-administration of compounds that can impede the efflux of chemotherapeutic agents by these ABC-transporters can concomitantly modulate various cytochrome P450 (CYP450) enzymes, consequently impacting upon anti-cancer drug metabolism. This can further result in unfavourable drug-drug interactions and altered pharmacokinetic properties of the administered anti-cancer drugs with knock-on adverse cytotoxic side effects. This review will discuss some of the P-gp inhibitors designed and employed to date, as well as expressing our views of the shortcomings of their design strategy. We present a medicinal chemist's wish list for the paradigmatic P-gp inhibitor molecule and examine the possible future strategies that could be implemented to achieve its design.

Affiliation

Nuffield Department of Clinical Laboratory Sciences, University of Oxford, UK. richard.darby@ndcls.ox.ac.uk.

Journal Details

This article was published in the following journal.

Name: Current drug metabolism
ISSN: 1875-5453
Pages:

Links

PubMed Articles [20266 Associated PubMed Articles listed on BioPortfolio]

Differential Retrieval of Past and Future Autobiographical Experiences.

Selective retrieval can both impair and enhance memory. In this study we analysed the effects of retrieval practice in the recall of past and future experiences. The participants generated past autobi...

Episodic elaboration: Investigating the structure of retrieved past events and imagined future events.

Five experiments investigated the cognitive processes involved in the elaboration of past and future events. A production listing procedure was used, in which participants listed details of each event...

Massage Therapy in Cancer Care: An Overview of the Past, Present, and Future.

Despite a plethora of research using various touch-based therapies on people in treatment or recovery from cancer, as well as at the end of life, there are still some misconceptions about massage in t...

Demethoxycurcumin Modulates Human P-Glycoprotein Function via Uncompetitive Inhibition of ATPase Hydrolysis Activity.

Curcuminoids are major components of Curcuma longa L., which is widely used as spice in food. This study aimed at identifying whether curcumin, demethoxycurcumin, and bisdemethoxycurcumin could modula...

Drug Shortages in Perioperative Medicine: Past, Present, or Future?

Clinical Trials [2432 Associated Clinical Trials listed on BioPortfolio]

Duration of P-glycoprotein Inhibition After Oral Administration of HM30181AK Tablet

The purposes of this study are to investigate the duration of P-glycoprotein inhibition after oral administration of HM30181AK tablet in healthy male subject and proper dose of HM30181AK t...

Reactogenicity and Immunogenicity of Vaginal ZM96gp140

To determine the local (cervico-vaginal) and systemic (whole body) safety of vaginal immunisation with ZM96gp140 glycoprotein administered 9 times over a 3 week period.

PET Imaging With Tc-94m Sestamibi to Assess Resistance to Chemotherapy

Background: - Tc-94m sestamibi is a radioactive imaging drug approved by the Food and Drug Administration to help photograph and study bodily functions. - Tc-94m sestami...

Effects of Dual Cyclooxygenase-2 and Carbonic Anhydrase Inhibition

Cyclooxygenase-2 (COX-2) inhibitors have become a common analgesic treatment option for patients with arthritis. However, long-term treatment has been associated with increased cardiovascu...

ID & Testing in Male Partners

This pilot study is a sub-study of ATN 067. ATN 067 utilizes a cross-sectional research design to recruit Latina and African American young women to undergo HIV screening. The primary goal...

Medical and Biotech [MESH] Definitions

A stochastic process such that the conditional probability distribution for a state at any future instant, given the present state, is unaffected by any additional knowledge of the past history of the system.

A course or method of action selected to guide and determine present and future decisions.

Decisions for determining and guiding present and future objectives from among alternatives.

A course or method of action selected, usually by a government, from among alternatives to guide and determine present and future decisions.

Decisions, usually developed by government policymakers, for determining present and future objectives pertaining to the health care system.


Advertisement
 

Relevant Topics

Cancer Disease
Latest News Clinical Trials Research Drugs Reports Corporate
Cancer is not just one disease but many diseases. There are more than 100 different types of cancer. Most cancers are named for the organ or type of cell in which they start - for example, cancer that begins in the colon is called colon cancer; cancer th...

Pharmacy
Latest News Clinical Trials Research Drugs Reports Corporate
Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...

Head and neck cancers
Latest News Clinical Trials Research Drugs Reports Corporate
Cancer can occur in any of the tissues or organs in the head and neck. There are over 30 different places that cancer can develop in the head and neck area. Mouth cancers (oral cancers)  - Mouth cancer can develop on the lip, the tongue, the floor...

Advertisement