TLR7-1A

TLR7-1A is a potent, cell-impermeable Toll-like receptor 7 (TLR7) agonist developed by researchers at Purdue University. It is a hydroxymethyl-modified derivative of the TLR7 agonist TLR7-54. TLR7-1A is designed to stimulate the innate immune system by activating TLR7, which is located in intracellular endosomes. Because free TLR7 agonists can cause severe systemic toxicity and cytokine release syndrome when administered systemically, TLR7-1A is typically utilized as a payload or component in targeted conjugates. These include folate-targeted conjugates (such as FA-TLR7-1A) designed to selectively reprogram folate receptor beta (FRβ)-expressing immunosuppressive tumor-associated macrophages (TAMs) and myeloid-derived suppressor cells (MDSCs) in the tumor microenvironment, as well as fluorescein-conjugated forms (fluorescein-TLR7-1A) used to rejuvenate exhausted anti-fluorescein chimeric antigen receptor (CAR) T cells.

Other names

Toll-like receptor 7 agonist 1ahydroxymethyl-modified TLR7-54