Our finding that C10M reduces pCRP*/mCRP‐induced NETosis further highlights the relevance of CRP regulation as an important immune checkpoint and the therapeutic potential of C10M. pCRP*/mCRP induces suicidal NETosis after 3 h of stimulation (Fig EV2B), a mode of NETosis where the membrane integrity is lost during the process (Yipp & Kubes ...

2022年12月5日 · The monovalent CRP inhibitor C10M prevents binding of pCRP to PC/PE and conformational change in pCRP toward pCRP*/mCRP and consequently reduces pro‐inflammatory actions.

2023年1月11日 · C-reactive protein (CRP) is an early-stage acute phase protein and highly upregulated in response to inflammatory reactions. We recently identified a novel mechanism that leads to a conformational change from the native, functionally relatively inert, pentameric CRP (pCRP) structure to a pentameric …

We designed a low molecular weight pCRP – PC inhibitor, C10M. Binding assays and X-ray crystallography revealed direct, competitive binding of C10M to pCRP, blocking interaction with PC and thereby inhibiting formation of pCRP*/mCRP and their pro-inflammatory effects.

2021年12月1日 · In this study, the pharmacokinetics and metabolism of the new drug candidate C10m was investigated. A sensitive and selective method for detection of C10m and its metabolites from plasma and urine was developed with LC-MS and LC-MS/MS coupling. The LLOQ is at 0.1 µg mL −1 and recovery at 87.4% ± 2.8%.

2024年3月7日 · Inclusion of a specific CRP dissociation/mCRP inhibitor (C10M) effectively inhibited PBMs clustering, as well as abrogating p-FAK expression, and partially reduced the expression of markers associated with M1 macrophage differentiation. mCRP also increased the secretion of pro-inflammatory cytokines Interleukin-8 (IL-8) and Interleukin-1β (IL ...

2022年12月5日 · The monovalent CRP inhibitor C10M prevents binding of pCRP to PC/PE and conformational change in pCRP toward pCRP*/mCRP and consequently reduces pro-inflammatory actions.

2021年9月28日 · We designed a low molecular weight pCRP – PC inhibitor, C10M. Binding assays and X-ray crystallography revealed direct, competitive binding of C10M to pCRP, blocking interaction with PC and...

2022年12月5日 · We recently identified a novel mechanism that leads to a conformational change from the native, functionally relatively inert, pentameric CRP (pCRP) structure to a pentameric CRP intermediate...

2022年12月5日 · Our finding that C10M reduces pCRP*/mCRP‐induced NETosis further highlights the relevance of CRP regulation as an important immune checkpoint and the therapeutic potential of C10M. pCRP*/mCRP induces suicidal NETosis after 3 h of stimulation (Fig EV2B), a mode of NETosis where the membrane integrity …