Small Molecule SRC Stimulators for Selective Cancer Cell Death
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Solution Overview
Problem
Current cancer treatments are inadequate in targeting steroid receptor coactivator (SRC) proteins, which are overexpressed in various cancers and contribute to tumorigenesis, progression, and drug resistance, highlighting the need for effective SRC-targeting therapies.
Innovation Solution
Development of small molecule compounds, such as MCB-613, that selectively stimulate SRC proteins, leading to hyper-activation and induction of aberrant cellular stress, specifically targeting cancer cells by enhancing their reliance on these proteins for growth and survival.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional cancer treatments are used, then cancer cells can be treated, but SRC proteins remain overexpressed and continue to drive tumorigenesis and progression
Solution Approach 1:
Instead of inhibiting SRC proteins, the patent applies inverse logic by using selective stimulators to hyper-activate them. This paradoxical approach exploits the oncogene addiction of cancer cells to SRC proteins, causing them to become overly dependent on continued SRC stimulation, which ultimately leads to cell death through proteostatic and oxidative stress.
Solution Approach 2:
The patent changes the functional state of SRC proteins from their normal overexpressed state to a hyper-activated state using small molecule stimulators. This parameter change in SRC activation status transforms the cellular outcome from continued proliferation to stress-induced cell death, resolving the contradiction between treatment effectiveness and maintaining harmful SRC overexpression.
2Productivity
If SRC proteins are inhibited, then cancer cell growth may be suppressed, but cancer cells rely on continued SRC activation for survival
Solution Approach 1:
The patent inverts the conventional inhibition strategy by applying selective stimulation. This creates a therapeutic window where hyper-activated SRC proteins induce proteostatic and oxidative stress that cancer cells cannot withstand, achieving both growth suppression and reliable cell death.
Solution Approach 2:
The patent converts the harmful overexpression of SRC proteins into a beneficial therapeutic effect. By using selective stimulators, the patent transforms the oncogenic drive into a mechanism for selective cell death, where the very proteins that promote cancer growth become the target for inducing lethal stress when hyper-activated.
3Adaptability or versatility
If non-specific cancer treatments are used, then various cancer types can be treated, but lack of specificity allows continued reliance on oncogenes
Solution Approach 1:
The patent applies local quality by developing SRC-selective stimulators that specifically target SRC proteins overexpressed in cancer cells. This selectivity is achieved through structural features of the stimulators that recognize and bind to the unique properties of SRC proteins, particularly SRC-3, SRC-1, and SRC-2, thereby treating cancer while sparing normal cells.
Solution Approach 2:
The patent uses parameter changes in the chemical structure of the stimulators to achieve selective binding to SRC proteins. By adjusting molecular properties such as binding affinity and selectivity parameters, the patent achieves precise targeting of cancer cells with overexpressed SRC proteins, resolving the contradiction between broad treatment coverage and specific targeting.
Data Source
AI summary
Small molecule stimulators of steroid receptor coactivator (SRC) family proteins are provided, as well as methods for their use in treating or preventing cancer. Also provided are methods for stimulating SRC family proteins in a cell.