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In advanced prostate cancer the AR-V7 splice variant of the androgen receptor lacks the ligand-binding domain that enzalutamide and abiraterone act on, and its presence predicts resistance. A degrader or N-terminal binder that removes the whole protein, variants included, would still work; AR-V7 is already measurable in circulating tumour cells.
AR-V7 lacks the ligand-binding domain, so enzalutamide and abiraterone cannot act on it, and its presence predicts resistance. Degraders and N-terminal-domain binders that engage full-length AR and its splice variants could restore control. Full-length AR degraders have reached the clinic; variant-competent agents are the unmet need, and AR-V7 status is already measurable in circulating tumour cells.
One bottleneck page and 24 idea pages on OnCo cite this paper by its DOI; this record gives the citation a page of its own so a reader can follow it without leaving OnCo. Read the abstract above alongside the citing pages listed under Related; the record was created automatically from the Europe PMC entry and its figures have not been checked by hand.
One of the most cited reviews Europe PMC returns for Androgen receptor in Prostate cancer, so it is a natural first reading for anyone weighing the idea it is linked from. The record was linked automatically by title and abstract; read the abstract above and the paper itself before relying on any figure.
One of the most cited reviews Europe PMC returns for Androgen receptor in Prostate cancer, so it is a natural first reading for anyone weighing the idea it is linked from. The record was linked automatically by title and abstract; read the abstract above and the paper itself before relying on any figure.
The first predictive resistance biomarker in prostate cancer, and a mechanism rather than a correlation: a receptor with no ligand-binding domain cannot be blocked by a drug that binds the ligand-binding domain. It is also the origin of the case for androgen receptor degraders, which destroy the protein rather than blocking a site the protein no longer has.
One of the most cited reviews Europe PMC returns for Androgen receptor in Prostate cancer, so it is a natural first reading for anyone weighing the idea it is linked from. The record was linked automatically by title and abstract; read the abstract above and the paper itself before relying on any figure.
Shares AR-V7 and resistance to enzalutamide and abiraterone in prostate cancer, Watch for the cancer changing cell type before the biopsy says neuroendocrine, and act on it, Androgen receptor signalling, The undruggable drivers.
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers, PROTACs & molecular glues (targeted protein degradation).
Shares The undruggable drivers, Prostate cancer roadmap: from Huggins and the discovery that a cancer can depend on a hormone, through the PSA epidemic and what it cost, the androgen receptor drugs, the DNA repair subset and PSMA, to a 2032 registry watch, Androgen receptor, Acquired resistance to every therapy.
Shares AR-V7 and resistance to enzalutamide and abiraterone in prostate cancer, Androgen receptor signalling, Prostate cancer roadmap: from Huggins and the discovery that a cancer can depend on a hormone, through the PSA epidemic and what it cost, the androgen receptor drugs, the DNA repair subset and PSMA, to a 2032 registry watch, Androgen receptor.
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers, PROTACs & molecular glues (targeted protein degradation).
Shares Watch for the cancer changing cell type before the biopsy says neuroendocrine, and act on it, Androgen receptor signalling, Prostate cancer roadmap: from Huggins and the discovery that a cancer can depend on a hormone, through the PSA epidemic and what it cost, the androgen receptor drugs, the DNA repair subset and PSMA, to a 2032 registry watch, Androgen receptor.
Shares Drugging the 'undruggable' cancer targets, The undruggable drivers, PROTACs & molecular glues (targeted protein degradation).
Shares Arvinas, The undruggable drivers, PROTACs & molecular glues (targeted protein degradation).