Platinum-Folate Complex Targeting Tumor Cells

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Solution Overview

Problem

Platinum-containing chemotherapeutic agents lack specificity, causing toxicity to both cancer cells and healthy cells due to non-selective DNA binding, necessitating the development of compounds that target tumor cells while sparing healthy tissues.

Innovation Solution

Designing platinum compounds that interact with folate transporters in cancer cells, utilizing a platinum complex combined with a folic acid antagonist to inhibit DNA replication and target cancer cells expressing these transporters.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If platinum compounds bind to DNA to inhibit replication, then cancer cells are killed effectively, but healthy cells are also damaged causing profound toxicities

Engineering Contradiction:

Improvecancer cell killing effectivenessVSAvoidtoxicity to healthy cells

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The platinum compound is segmented into two functional parts: a platinum moiety responsible for DNA binding and cell killing, and a folic acid antagonist moiety responsible for selective recognition of cancer cells. This segmentation allows each part to perform its specific function independently, achieving both effectiveness and selectivity

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The folic acid antagonist acts as an intermediary that mediates the selective entry of the platinum compound into cancer cells through folate transporters. This intermediary enables the platinum compound to reach its target selectively in cancer cells while avoiding healthy cells, thereby resolving the contradiction between effectiveness and toxicity

Inventive Principle:

Principle #24Intermediary (Mediator)

2Quantity of substance

If platinum compounds are used at therapeutic doses to treat cancer, then tumor cells are targeted, but healthy tissues are still affected due to non-specific transport

Engineering Contradiction:

Improveplatinum delivery to tumorVSAvoiddamage to healthy tissues

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The compound exhibits local quality by being selectively taken up by cancer cells through folate transporters that are overexpressed in these cells. This localized uptake ensures that the platinum compound concentrates in tumor tissues while minimizing exposure of healthy tissues, resolving the contradiction between sufficient drug delivery and avoidance of healthy tissue damage

Inventive Principle:

Principle #3Local quality

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The platinum-folate transporter complex effectively inhibits DNA replication in cancer cells, reducing toxicity to healthy cells by selectively targeting tumor cells, as demonstrated by higher potency in cancer cell lines and improved tumor treatment outcomes.

Implementation Method 1

Platinum compounds may bind to DNA and inhibit DNA replication

Methodology Applied

Scientific EffectDNA binding: Chemical Bonding

Implementation Method 2

transporters that bring folic acid into tumor cells could be important in the cancer cell growth

Methodology Applied

Scientific EffectTransporter-mediated transport: Permeation

Data Source

PatentUS10392412B2Platinum anticancer agents

Publication Date: 2019.08.27 CORNELL UNIVERSITY

AI summary

Disclosed herein, inter alia, are platinum-based compounds useful for treating cancer.