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An agonist switches a receptor on, imitating the natural signal; an antagonist sits in the receptor and blocks it without switching it on. Cancer medicine uses both.
Antagonists are the more familiar: tamoxifen and fulvestrant occupy the oestrogen receptor so oestrogen cannot, and enzalutamide does the same to the androgen receptor. Agonists are used when switching something on helps, such as STING agonists that alarm the innate immune system, CD40 or 4-1BB agonists that stimulate immune cells, and GnRH agonists that paradoxically shut down testosterone production by overstimulating the pituitary. Partial agonists and selective modulators (SERMs) fall in between, activating a receptor in some tissues while blocking it in others.
In plain words · The hormone switch that drives most breast cancers. Blocking or destroying it is the oldest and most effective targeted therapy.
Showing the target this term concerns: Estrogen receptor (ERα).
Shares Hormone therapy, Estrogen receptor (ERα).
Shares Androgen receptor, Endocrine therapy (SERMs, AIs, SERDs).
Shares Estrogen receptor (ERα), Endocrine therapy (SERMs, AIs, SERDs).
Shares Estrogen receptor (ERα), Endocrine therapy (SERMs, AIs, SERDs).
Shares Androgen deprivation & AR pathway inhibitors, Androgen receptor.
Shares Androgen deprivation & AR pathway inhibitors, Androgen receptor.