We describe the discovery of a thioester-containing glucocorticoid receptor modulator
(GRM) payload and the corresponding antibody–drug conjugate (ADC). Payload 6 was …

Glucocorticoids (GCs) are efficacious drugs used for treating many inflammatory diseases,
but the dose and duration of administration are limited because of severe side effects. We …

Glucocorticoid receptor modulators (GRM) are the first-line treatment for many immune
diseases, but unwanted side effects restrict chronic dosing. However, targeted delivery of a …

Glucocorticoids (GCs) are widely used to treat a variety of autoimmune and inflammatory
diseases; however, systemic delivery of GCs is associated with side effects that affect …

Using a convergent synthetic route to enable multiple points of diversity, a series of
glucocorticoid receptor modulators (GRM) were profiled for potency, selectivity, and drug …

Background: Glucocorticoids (GC) are potent drugs used for treating many inflammatory
diseases. While GCs are effective in many immune diseases, dose and duration of …

Glucocorticoids (GCs) are effective in treating autoimmune and inflammatory disorders but
come with significant side effects, many of which are mediated by non-immunological cells …

Glucocorticoids (GCs) are excellent anti-inflammatory drugs but are dose-limited by on-
target toxicity. We sought to solve this problem by delivering GCs to immune cells with …

On-target, off-tissue toxicity limits the systemic use of drugs that would otherwise reduce
symptoms or reverse the damage of arthritic diseases, leaving millions of patients in pain …

Stable attachment of drug-linkers to the antibody is a critical requirement, and for maleimide
conjugation to cysteine, it is achieved by ring hydrolysis of the succinimide ring. During ADC …