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Related Concept Videos

Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Biopharmaceutical Factors Influencing Drug Product Design: Overview01:22

Biopharmaceutical Factors Influencing Drug Product Design: Overview

Rational drug product design integrates knowledge of the drug’s physicochemical properties, formulation components, manufacturing techniques, and intended route of administration. Each factor influences the drug’s performance, including how it is released, absorbed, and eliminated in the body.The physicochemical properties of a drug—such as solubility, stability, and particle size—affect its compatibility with excipients and the choice of dosage form. Excipients, though pharmacologically...
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...

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Related Experiment Video

Updated: Jul 13, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
07:20

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Published on: May 28, 2014

Addressing Clinical Challenges of Platinum Anticancer Drugs through Rational Chemical Design.

Shuren Zhang1, Zijian Guo1,2

  • 1State Key Laboratory of Coordination Chemistry, School of Chemistry, Chemistry and Biomedicine Innovation Center (ChemBIC), 163 Xianlin Avenue, Nanjing University, Nanjing 210023, China.

Accounts of Chemical Research
|July 11, 2026
PubMed
Summary

Platinum(IV) prodrugs are functionalized and targeted for enhanced chemotherapy, overcoming drug resistance and toxicity. These advanced platinum agents co-target cancer pathways and immune responses, offering safer, more effective precision treatments.

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Last Updated: Jul 13, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
07:20

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Published on: May 28, 2014

Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay
11:14

Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay

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Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
08:46

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

Area of Science:

  • Medicinal Chemistry
  • Nanotechnology
  • Cancer Biology

Background:

  • Platinum (Pt)-based chemotherapy is vital but limited by toxicity and resistance.
  • Pt(IV) complexes offer a versatile platform for functionalization and targeted delivery.

Purpose of the Study:

  • To develop novel Pt(IV) prodrugs addressing chemotherapy limitations through functionalization and targeted delivery.
  • To create multifunctional Pt(IV) agents that co-target cancer pathways and modulate the tumor immune microenvironment.
  • To engineer radiotherapy-responsive and targeted delivery systems for precise platinum drug activation and reduced systemic toxicity.

Main Methods:

  • Functionalization of Pt(IV) complexes with bioactive ligands targeting DNA repair, apoptosis, metabolism, and immune pathways.
  • Development of targeted delivery platforms including mitochondria-targeting, biotin-mediated, and antibody-drug conjugates (Pt-ADCs).
  • Design of stimuli-responsive systems (radiotherapy-responsive, in situ self-assembly) for controlled drug release and activation.
  • Utilizing immunocompetent patient-derived organoids for preclinical screening.

Main Results:

  • Multifunctional Pt(IV) prodrugs demonstrated co-targeting of cancer pathways and immune engagement, inducing various cell death mechanisms.
  • Radiotherapy-responsive Pt(IV) prodrugs showed X-ray-triggered activation with reduced toxicity.
  • Targeted delivery platforms improved tumor selectivity and cytotoxicity, with Pt-ADCs enhancing immune responses.
  • Stimuli-responsive systems enabled enhanced tumor accumulation and controlled drug release.

Conclusions:

  • Integrated strategies of multifunctional modulation, targeted delivery, and controlled activation within Pt-based systems address chemoresistance and toxicity synergistically.
  • Programmable Pt therapeutics show promise for safer and more effective precision chemotherapy.
  • Further research focuses on optimizing pharmaceutical properties, clinical translation of advanced Pt(IV) prodrugs and Pt-ADCs, and refining predictive screening platforms.