CD73 Inhibitor Compounds for Blocking AMP-to-Adenosine Signaling
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Solution Overview
Problem
Current treatments for cancer, infections, and neurodegenerative diseases are inadequate, particularly due to the immunosuppressive effects of CD73, which contributes to therapy resistance and immune evasion.
Innovation Solution
Development of compounds that inhibit CD73 activity, including pharmaceutical compositions, to disrupt adenosine signaling and enhance immune response.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If CD73 is active, then adenosine signaling is enhanced, but immune suppression increases and therapy resistance develops
Solution Approach 1:
The patent extracts and removes the harmful function of CD73 by developing small molecule inhibitors that specifically block CD73 enzymatic activity. The compounds are designed to bind to the catalytic site of CD73, preventing adenosine monophosphate (AMP) hydrolysis and subsequent adenosine production, thereby eliminating the immunosuppressive effect while preserving other physiological functions
Solution Approach 2:
The patent changes the biochemical parameter of CD73 activity by introducing compounds that alter the enzyme's catalytic function. The inhibitors modify the kinetic parameters of CD73 by blocking substrate binding or catalysis, transforming the enzyme from an active immunosuppressive state to an inhibited state, thereby reversing therapy resistance
2Reliability
If current treatments are used, then some therapeutic effect is achieved, but therapy resistance develops due to CD73-mediated immune evasion
Solution Approach 1:
The patent applies preliminary action by administering CD73 inhibitors before or alongside conventional cancer therapies. This preemptive inhibition of CD73 prevents the development of therapy resistance by blocking the immunosuppressive adenosine pathway before it can counteract the therapeutic effect, thereby maintaining stable immune response throughout treatment
Solution Approach 2:
The patent introduces CD73 inhibitors as intermediary compounds that mediate between the immune system and the tumor. These small molecules act as mediators by blocking the CD73 enzyme, thereby preventing the conversion of AMP to adenosine and interrupting the immunosuppressive signaling pathway that would otherwise protect the tumor from immune attack
Data Source
AI summary
Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases.