IndraLab

Statements

Oligonucleotide inhibits TLR7. 7 / 7
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"Although the inhibitory effect of select LNA/DNA AMOs was surprising, it is consistent with a previous report that phosphorothioate DNA oligonucleotides can inhibit TLR7 sensing in a sequence-dependent manner ( xref )."
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"By contrast, substitution of 2′-O-methyl-C, 2′-O-methyl-5-methyl-C or 5-methyl-dC for C or 2′-O-methyl-G for G leads to loss of immune-stimulatory activity; further, such oligos inhibit TLR7- and TLR9-mediated immune responses ( xref )."
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"In further support of this hypothesis, oligonucleotide inhibitors of TLR7 and low-molecular-weight (LMW) inhibitors of TLR7/8 showed efficacy in mouse models of lupus.15 16 However, clinical trial data of TLR7/8 antagonists in patients suffering from autoimmune diseases are not yet available."
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"IMO-8400 is a second-generation oligonucleotide antagonist that inhibits TLR7, TLR8 and TLR9 as well as disease progression of SLE and psoriasis in animal models (146–148)."
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"Oligonucleotide inhibition of TLR7 and TLR9 in lupus prone mice led to TLR7 and 9 signaling obstructions and reduction of autoantibody levels, proteinuria and kidney damage, which were highly correlated with the induction of IFNα in plasmacytoid dendritic cells (PDCs) [92]."
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"Non-selective small molecule (CpG-52364) as well as oligonucleotide (IMO-8400) antagonists of both TLR7 and TLR9 entered clinical trial to determine its safety and efficacy in patients [ 25–27 ], but [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"IMO‐3100 is an oligonucleotide antagonist of TLR-7 and TLR-9, which is injected subcutaneously for treating psoriasis [73] ."
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