Selenated-Folate Hybrids for Targeted Anticancer Delivery

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Solution Overview

Problem

Current cancer therapies lack effective organoselenium compounds fused with folates to maximize anticancer activity, as existing agents show limited selectivity and specificity towards cancer cells.

Innovation Solution

Development of novel selenate-folate antagonists that enhance the cellular uptake of organoselenium compounds by targeting the SLC19A1 carrier and inhibiting MTHFD1 and MTHFD2 enzymes, leading to increased cellular concentration of organoselenium and induction of cell cycle arrest in cancer cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing organoselenium agents are used, then anticancer activity is achieved, but selectivity and specificity towards cancer cells is limited

Engineering Contradiction:
Improveanticancer activityVSAvoidlack of selectivity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent combines organoselenium agents with folate structures to create hybrid compounds. The folate portion targets cancer cells that overexpress folate receptors and have elevated folate uptake, while the organoselenium portion provides the anticancer activity. This merging allows the compound to selectively accumulate in cancer cells, resolving the contradiction between achieving anticancer activity and improving selectivity.

Inventive Principle:
Principle #5Merging (Combining)

2Quantity of substance

If novel selenate-folate antagonists are developed, then cellular uptake of organoselenium is enhanced, but device complexity increases

Engineering Contradiction:
Improvecellular concentration of organoseleniumVSAvoidchemical structure complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The invention creates composite molecular structures by covalently linking organoselenium moieties with folate structures. This composite approach allows the molecule to exploit the high-affinity folate transport system (SLC19A1) for cellular uptake, thereby increasing intracellular organoselenium concentration. The complexity is justified by the significant improvement in targeted delivery and anticancer efficacy.

Inventive Principle:
Principle #40Composite materials

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 novel compounds effectively trap folates, maximizing anticancer activity and promoting cancer cell death, offering a chemopreventive approach against cancer.

Implementation Method 1

facilitating their movement through SLC19A1 from outside the cell into the cytoplasm

Methodology Applied
Scientific EffectFacilitated diffusion: Diffusion

Implementation Method 2

maximize the anticancer activity of organoselenium compounds by blocking the action of folates by targeting MTHFD1 and MTHFD2 inhibition

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Data Source

PatentUS11845750B1Antiproliferative selenated-folate hybrids
Publication Date: 2023.12.19 KING FAISAL UNIV
  • US11845750B1 patent drawing
  • US11845750B1 patent drawing
  • US11845750B1 patent drawing

AI summary

Novel organoselenium compounds formed with folates that can be used to maximize anticancer activity of the organoselenium. Novel organoselenium compounds that can be used as a chemopreventive against cancer. These compounds may be present in pharmaceutical compositions and may be used in various treatment methods.