Tumor {associated|related|connected|linked} macrophages (TAMs) {support|assistance|help} tumor {development|improvement} and have emerged as {important|essential|crucial|critical|significant|vital} regulators of therapeutic response to cytostatic agents. To target TAMs, {we have|we’ve|we’ve got} {developed|created} a novel drug delivery {approach|method|strategy} which induces drug release in response to inhibition of pro-tumor cysteine cathepsin activity. Such inhibitory prodrug (IPD) establishes a self-regulated delivery {system|method|program|technique} {where|exactly where} drug release stops {after|following|right after|soon after|immediately after|just after} all cysteine cathepsins are inhibited. This could {improve|enhance|boost|increase|strengthen} the therapeutic window for drugs with {severe|serious|extreme} {side effects|unwanted side effects|negative effects|unwanted effects}. We demonstrate this self-regulation {concept|idea|notion} {with a|having a|using a} fluorogenic IPD model. {We have|We’ve|We’ve got} applied our IPD {strategy|technique|method|approach|tactic} to two cytotoxic agents, doxorubicin and monomethyl auristatin E, which {could be|might be|could possibly be|may be|may very well be} {efficiently|effectively} released {from the|in the} IPD scaffold to induce concentration dependent toxicity in RAW macrophages. Lastly, by taking {advantage|benefit} {of the|from the|in the|on the|with the|of your} {increased|elevated|improved|enhanced} cathepsin activity in TAM-like M2 polarized bone marrow derived macrophages, we show that IPD Dox selectively eliminates M2 {over|more than} M1 macrophages. This demonstrates the {potential|possible|prospective} of our IPD {strategy|technique|method|approach|tactic} for selective drug delivery and modulation {of the|from the|in the|on the|with the|of your} tumor microenvironment. 6-Bromo-2-fluoro-3-nitropyridine web Fmoc-D-beta-indanylglycine Purity PMID:23935843
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