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Chaves, J. C. S.

Publications and source records attributed to Chaves, J. C. S..

3 recordsLinked to original sources

Increased tau expression in the APOE4 blood-brain barrier model is associated with reduced anti-tau therapeutic antibody delivery in vitro.

Tau protein is a critical driver of neurodegeneration and an important drug target in Alzheimers disease (AD). Tau-specific immunotherapy has emerged as a promising treatment strategy for AD, however the therapeutic efficacy of anti-tau antibodies may be limited by their insufficient delivery across the blood-brain barrier (BBB). The apolipoprotein E4 allele (APOE4) is the strongest genetic risk factor for sporadic AD and is known to influence tau-mediated neurodegeneration. Interestingly, both tau and APOE4 have been implicated in the cerebrovascular pathology observed in AD. Yet, the crosstalk between APOE4 and tau at the level of the BBB and its consequences for anti-tau immunotherapeutics delivery, remain poorly understood. Here, we utilised APOE3- and APOE4-carrying human iPSC-derived induced brain endothelial-like cells (iBECs) as a sporadic AD BBB model, determined the levels of endogenous tau in iBECs, and explored the transport of two novel monoclonal anti-tau antibodies, RNF5 and RN2N, across the in vitro barrier. Our results demonstrate that MAPT gene transcription, tau protein levels and tau phosphorylation are increased in iBECs in an APOE4-related manner and are associated with reduced iBEC monolayer integrity and increased permeability to biologically inert fluorescent tracers. Additionally, elevated levels of intracellular tau in APOE4 cells were accompanied by the reduced passive permeability of therapeutic anti-tau antibodies through the APOE4 iBEC monolayer, which could be improved by the application of focused ultrasound and microbubble drug-delivery technology. Together, our study illustrates a new role for APOE4 and tau in human iBECs with potential implications for BBB dysfunction and anti-tau therapeutic antibody delivery.

cell biology↗

A patient-derived blood-brain barrier model for screening copper bis(thiosemicarbazone) complexes as potential therapeutics in Alzheimer's disease

Alzheimers disease (AD) is the most prevalent cause of dementia characterised by progressive cognitive decline. Addressing neuroinflammation represents a promising therapeutic avenue to treat AD, however, the development of effective anti-neuroinflammatory compounds is often hindered by their limited blood-brain barrier (BBB) permeability. Consequently, there is an urgent need for accurate, preclinical AD patient-specific BBB models to facilitate the early identification of immunomodulatory drugs capable of efficiently crossing human AD BBB. This study presents a unique approach to BBB drug permeability screening as it utilises the familial AD patient-derived induced brain endothelial-like cells (iBEC)-based model, which exhibits increased disease relevance and serves as an improved BBB drug permeability assessment tool when compared to traditionally employed in vitro models. To demonstrate its utility as a small molecule drug candidate screening platform, we investigated the effects of CuII(atsm) and a library of novel metal bis(thiosemicarbazone) complexes - a class of compounds exhibiting anti-neuroinflammatory therapeutic potential in neurodegenerative disorders. By evaluating the toxicity, cellular accumulation and permeability of those compounds in the AD patient-derived iBEC, we have identified CuII(dtsm) as an emerging drug candidate with enhanced transport across the AD BBB. Furthermore, we have developed a multiplex approach where AD patient-derived iBEC were combined with immune modulators TNF and IFN{gamma} to establish an in vitro model representing the characteristic neuroinflammatory phenotype at the patients BBB. Here we observed that treatment with CuII(dtsm) not only reduced the expression of proinflammatory cytokine genes but also reversed the detrimental effects of TNF and IFN{psi} on the integrity and function of the AD iBEC monolayer. This suggests a novel pathway through which copper bis(thiosemicarbazone) complexes may exert neurotherapeutic effects in AD by mitigating BBB neuroinflammation and related BBB integrity impairment. Together, the presented model provides an effective and easily scalable in vitro BBB platform for screening AD drug candidates. Its improved translational potential makes it a valuable tool for advancing the development of metal-based compounds aimed at modulating neuroinflammation in AD. Graphical abstract O_FIG O_LINKSMALLFIG WIDTH=199 HEIGHT=200 SRC="FIGDIR/small/554047v1_ufig1.gif" ALT="Figure 1"> View larger version (71K): org.highwire.dtl.DTLVardef@1d949b5org.highwire.dtl.DTLVardef@7629ccorg.highwire.dtl.DTLVardef@1b2125dorg.highwire.dtl.DTLVardef@1d3cde1_HPS_FORMAT_FIGEXP M_FIG C_FIG

neuroscience↗

A sporadic Alzheimer's blood-brain barrier model for developing ultrasound-mediated delivery of Aducanumab and anti-Tau antibodies.

RationaleThe blood-brain barrier (BBB) is a major impediment to therapeutic intracranial drug delivery for the treatment of neurodegenerative diseases, including Alzheimers disease (AD). Focused ultrasound applied together with microbubbles (FUS+MB) is a novel technique to transiently open the BBB and increase drug delivery. Evidence suggests that FUS+MB is safe, however the effects of FUS+MB on human BBB cells, especially in the context of AD, remain sparsely investigated. MethodsHere we generated BBB cells (induced brain endothelial cells (iBECs) and astrocytes (iAstrocytes)) from apolipoprotein E gene allele E4 (APOE4, high AD risk) and allele E3 (APOE3, lower AD risk) carrying patient-derived induced pluripotent stem cells (iPSCs). We then developed a human sporadic AD BBB cell platform to investigate the effects of FUS+MB on BBB cells and screen for the delivery of two potentially therapeutic AD antibodies. ResultsWe utilized this robust and reproducible human BBB model to demonstrate increased delivery of therapeutic AD antibodies across the BBB following FUS+MB treatment, including an analogue of Aducanumab (AduhelmTM; anti-amyloid-{beta}) and a novel anti-Tau antibody RNF5. Our results also demonstrate the safety of FUS+MB indicated by minimal changes in the cell transcriptome as well as little or no changes in cell viability and inflammatory responses within the first 24 h post FUS+MB. Finally, we report a more physiologically relevant hydrogel-based 2.5D BBB model as a key development for FUS+MB-mediated drug delivery screening, with potentially higher translational utility. ConclusionOur results demonstrate an important translatable patient BBB cell model for identifying FUS+MB-deliverable drugs and screening for cell- and patient-specific effects of FUS+MB, accelerating the use of FUS+MB as a therapeutic modality in AD. One Sentence SummaryFocused ultrasound increases the in vitro delivery of therapeutic antibodies Aducanumab and anti-Tau in a sporadic Alzheimers disease patient-derived blood-brain barrier cell model.

neuroscience↗