Immunoregulatory Agent Modulating DOCK2-Rac Pathway
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Solution Overview
Problem
Current cancer treatments, such as antibody therapy targeting immune checkpoint molecules, are hindered by the immune evasion mechanism known as immune privilege, which needs to be canceled for effective therapy. Additionally, clarifying the substance of immune privilege could enable the artificial granting of immune privilege to cells or tissues for transplantation and regenerative medicine.
Innovation Solution
The development of a novel immunoregulatory agent that regulates Dedicator of cytokinesis 2 (DOCK2)-mediated Rac activation, specifically using compounds that bind to cholesterol 3-sulfate or its derivatives, to inhibit or modulate immune cell migration and function, thereby forming or canceling immune-privileged sites.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If antibody therapy targeting immune checkpoint molecules is used, then cancer treatment effectiveness is improved, but immune privilege of cancer tissues prevents the therapy from working effectively
Solution Approach 1:
The patent identifies cholesterol 3-sulfate as the substance that creates immune privilege in cancer tissues. By targeting and inhibiting this substance or its production pathway, the patent converts the harmful immune privilege mechanism into a benefit, allowing immune checkpoint therapy to work effectively while maintaining the ability to create immune privilege in healthy transplanted tissues.
Solution Approach 2:
The patent applies different immunoregulatory strategies to different locations: in cancer tissues, it aims to eliminate immune privilege by inhibiting cholesterol 3-sulfate; in transplanted healthy tissues, it aims to establish immune privilege by promoting cholesterol 3-sulfate production. This spatially differentiated approach resolves the contradiction between treating cancer and protecting healthy tissues.
2Adaptability or versatility
If immune privilege is clarified and artificially granted to cells or tissues, then transplantable allogeneic tissues can be prepared for transplantation and regenerative medicine, but currently the substance of immune privilege is unclear
Solution Approach 1:
The patent identifies cholesterol 3-sulfate as the endogenous substance that naturally creates immune privilege. By harnessing this existing biological mechanism rather than introducing external substances, the patent enables artificial immune privilege granting through modulation of the host's own metabolic pathways, specifically by promoting cholesterol sulfation in transplanted tissues.
3Reliability
If immunoregulatory agent is used to inhibit immune cell migration, then immune-privileged sites are formed and transplant rejection is prevented, but cancer immunity may be suppressed
Solution Approach 1:
The patent employs location-specific immunoregulation: cholesterol 3-sulfate production is promoted in transplanted healthy tissues to create immune privilege and prevent rejection, while in cancer tissues, the same substance is inhibited to allow immune cell infiltration and anti-tumor immunity. This spatial differentiation resolves the contradiction between protecting transplants and fighting cancer.
Data Source
AI summary
An immunoregulatory agent containing a regulatory agent that regulates Dedicator of cytokinesis 2 (DOCK2)-mediated Rac activation as an active ingredient is provided.


