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Related Concept Videos

Pharmacokinetics: Drug–Drug Interactions01:25

Pharmacokinetics: Drug–Drug Interactions

65
Drug interactions occur when the pharmacological effect of one drug is altered by another substance, either enhancing or diminishing its activity. The drug whose activity is altered is known as the object drug, and the substance causing the alteration is called the agent drug or the precipitant. The net effects of these interactions are mostly undesirable, leading to decreased effectiveness or increased adverse effects. In rare cases, interactions can be beneficial, such as the enhanced...
65
Hepatic Drug Clearance: Role of Transporters01:14

Hepatic Drug Clearance: Role of Transporters

152
In the liver and bile canaliculi, influx and efflux transporters modification can influence intrinsic clearance. Transporters play a significant role in moving drugs within liver cells. Elaborate models, such as the Biopharmaceutical Classification System (BCS), are essential to relate transporters to drug disposition. This system categorizes drugs into four classes based on solubility and permeability, providing insights into elimination routes and the effects of transporters following oral...
152
Drug Elimination by Renal Route: Tubular Secretion01:15

Drug Elimination by Renal Route: Tubular Secretion

3.0K
Once the process of glomerular filtration is completed, blood carrying unfiltered drug molecules traverses through efferent arterioles and makes its way into the peritubular capillaries in the proximal tubule. A variety of carriers play a pivotal role in actively secreting drugs from these peritubular capillaries into the tubular fluid. The organic anion transporter transfers acidic drugs, against an electrochemical gradient, from the peritubular capillaries into the renal tubule cells and...
3.0K
Factors Affecting Protein-Drug Binding: Drug Interactions01:23

Factors Affecting Protein-Drug Binding: Drug Interactions

373
Drug interactions are a critical aspect of pharmacology and can occur when two or more drugs compete for the same binding site. This competition can result in one drug displacing another, altering the effect of the displaced drug. Drug interactions are complex processes that rely heavily on how much of the displacer drug is present and how strongly it can bind to the same sites as the displaced drug.
Displacement interactions can have varying outcomes, ranging from toxicity to virtually...
373
Nonlinear Pharmacokinetics: Role of Transporters01:27

Nonlinear Pharmacokinetics: Role of Transporters

132
A drug's nonlinear kinetics can be influenced by a diverse range of transporter proteins that serve as crucial players in drug distribution. These transporters, found within cells, can enhance or reduce local drug concentrations by facilitating the influx or efflux of drugs. For instance, the expression of xenobiotic transporters can be influenced by factors such as age and gender, potentially impacting the linearity of drug response.
Polymorphisms occurring in drug transporters can alter...
132
Effect of Hepatic Disease on Pharmacokinetics: Drug Dosing and Hepatic Blood Flow01:26

Effect of Hepatic Disease on Pharmacokinetics: Drug Dosing and Hepatic Blood Flow

50
Chronic liver disease significantly impacts drug metabolism due to alterations in hepatic blood flow and enzyme accessibility. This disruption affects the body's pharmacokinetics—the movement and processing of drugs within the system. Key enzymes crucial for metabolizing medications become less accessible, changing how drugs are processed and utilized. Furthermore, liver disease influences the synthesis of plasma proteins, such as albumin and globulins, which play critical roles in drug...
50

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Interference between copper transport systems and platinum drugs.

Fabio Arnesano1, Giovanni Natile1

  • 1Department of Chemistry, University of Bari, via Orabona, 4, 70125 Bari, Italy.

Seminars in Cancer Biology
|May 31, 2021
PubMed
Summary

Cisplatin, a platinum-based chemotherapy, kills cancer cells by damaging DNA. Its uptake into cells involves copper transport proteins like CTR1 and ATPases, offering potential therapeutic targets.

Keywords:
ATOX1ATP7AATP7BCTR1CancerCisplatinCisplatin resistanceCopper homeostasisCopper transportersPlatinum traffickingPt-interference with copper metabolismSensitization therapy

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Ion Mobility-Mass Spectrometry Techniques for Determining the Structure and Mechanisms of Metal Ion Recognition and Redox Activity of Metal Binding Oligopeptides
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Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Cisplatin (cis-diamminedichloridoplatinum(II)) is a crucial platinum-based chemotherapy agent used against various cancers.
  • Its primary mechanism involves binding to nuclear DNA, inducing malignant cell death.
  • Cellular uptake of cisplatin is complex, involving passive diffusion and potentially endocytosis and active transport.

Purpose of the Study:

  • To provide an updated review of intracellular transport and processing mechanisms of cisplatin.
  • To highlight the roles of specific copper transport proteins in cisplatin's efficacy.
  • To explore the potential of these proteins as pharmacological targets for cancer therapy.

Main Methods:

  • Literature review of current research on cisplatin intracellular transport.
  • Focus on the involvement of copper permease CTR1.
  • Analysis of Cu-transporting ATPases (ATP7A, ATP7B) and the copper chaperone ATOX1.

Main Results:

  • The plasma membrane copper permease CTR1 is a key transporter for cisplatin uptake.
  • ATP7A and ATP7B ATPases in the trans-Golgi network influence cisplatin processing and localization.
  • ATOX1, a soluble copper chaperone, may also play a role in cisplatin's intracellular journey.

Conclusions:

  • Copper transport proteins, including CTR1, ATP7A, ATP7B, and ATOX1, are critical for cisplatin's anticancer efficacy.
  • Understanding these transport systems is vital for optimizing cisplatin-based therapies.
  • Targeting these copper-related proteins presents a promising strategy for enhancing chemotherapy effectiveness.