S100 to receptor for advanced glycation end-products binding assay: Looking for inhibitors

Padilla, Laura; Dakhel, Sheila; Hernández, José Luís

doi:10.1016/j.bbrc.2014.02.143

Cited by 11 publications

(7 citation statements)

References 22 publications

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“…Recombinant human S100A4 (rhS100A4) protein was obtained as described by [48]. Hybridoma obtaining and cell subcloning was performed using standard technologies.…”

Section: Biosensing Protocolmentioning

confidence: 99%

Al₂O₃microring resonators for the detection of a cancer biomarker in undiluted urine

Goede¹,

Dijkstra²,

Obregón³

et al. 2019

Opt. Express

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Concentrations down to 3 nM of the rhS100A4 protein, associated with human tumor development, have been detected in undiluted urine using an integrated sensor based on microring resonators in the emerging Al 2 O 3 photonic platform. The fabricated microrings were designed for operation in the C-band (λ = 1565 nm) and exhibited a high-quality factor in air of 3.2 × 10 5. The bulk refractive index sensitivity of the devices was ~100 nm/RIU (for TM polarization) with a limit of detection of ~10 −6 RIU. A surface functionalization protocol was developed to allow for the selective binding of the monoclonal antibodies designed to capture the target biomarker to the surface of the Al 2 O 3 microrings. The detection of rhS100A4 proteins at clinically relevant concentrations in urine is a big milestone towards the use of biosensors for the screening and early diagnosis of different cancers. Biosensors based on this microring technology can lead to portable, multiplexed and easy-to-use point of care devices.

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“…Recombinant human S100A4 (rhS100A4) protein was obtained as described by [48]. Hybridoma obtaining and cell subcloning was performed using standard technologies.…”

Section: Biosensing Protocolmentioning

confidence: 99%

Al₂O₃microring resonators for the detection of a cancer biomarker in undiluted urine

Goede¹,

Dijkstra²,

Obregón³

et al. 2019

Opt. Express

View full text Add to dashboard Cite

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“…Of importance, transfection with siRNA significantly decreased migration by 20%. Additionally, in A375‐hRAGE cells, incubation with S100A4 resulted in a significantly increased migration by 23%, whereas blockade of ligand binding to RAGE by using an anti‐RAGE antibody 30 decreased migration by 10% but showed no statistical significance. On the other hand, investigations concerning invasive capability confirmed the stimulating effect of S100A4 (Fig.…”

Section: Resultsmentioning

confidence: 92%

Interaction of extracellular S100A4 with RAGE prompts prometastatic activation of A375 melanoma cells

Herwig

Belter

Wolf

et al. 2016

J Cellular Molecular Medi

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S100A4, a member of the S100 protein family of EF‐hand calcium‐binding proteins, is overexpressed in various tumour entities, including melanoma, and plays an important role in tumour progression. Several studies in epithelial and mesenchymal tumours revealed a correlation between extracellular S100A4 and metastasis. However, exact mechanisms how S100A4 stimulates metastasis in melanoma are still unknown. From a pilot experiment on baseline synthesis and secretion of S100A4 in human melanoma cell lines, which are in broad laboratory use, A375 wild‐type cells and, additionally, newly generated A375 cell lines stably transfected with human S100A4 (A375‐hS100A4) or human receptor for advanced glycation endproducts (A375‐hRAGE), were selected to investigate the influence of extracellular S100A4 on cell motility, adhesion, migration and invasion in more detail. We demonstrated that A375 cells actively secrete S100A4 in the extracellular space via an endoplasmic reticulum‐Golgi‐dependent pathway. S100A4 overexpression and secretion resulted in prometastatic activation of A375 cells. Moreover, we determined the influence of S100A4‐RAGE interaction and its blockade on A375, A375‐hS100A4, A375‐hRAGE cells, and showed that interaction of RAGE with extracellular S100A4 contributes to the observed activation of A375 cells. This investigation reveals additional molecular targets for therapeutic approaches aiming at blockade of ligand binding to RAGE or RAGE signalling to inhibit melanoma metastasis.

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“…The purchased computational screening hits were subjected to initial biological testing for inhibition of S100P-RAGE binding (ELISA), with cromolyn as positive control, using an adaptation of the reported ELISA for S100 family members [ 31 ].…”

Section: Resultsmentioning

confidence: 99%

Discovery of novel small molecule inhibitors of S100P with in vitro anti-metastatic effects on pancreatic cancer cells

Camara

Ogbeni

Gerstmann

et al. 2020

European Journal of Medicinal Chemistry

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S100P, a calcium-binding protein, is known to advance tumor progression and metastasis in pancreatic and several other cancers. Herein is described the in silico identification of a putative binding pocket of S100P to identify, synthesize and evaluate novel small molecules with the potential to selectively bind S100P and inhibit its activation of cell survival and metastatic pathways. The virtual screening of a drug-like database against the S100P model led to the identification of over 100 clusters of diverse scaffolds. A representative test set identified a number of structurally unrelated hits that inhibit S100P-RAGE interaction, measured by ELISA, and reduce in vitro cell invasion selectively in S100P-expressing pancreatic cancer cells at 10 μM. This study establishes a proof of concept in the potential for rational design of small molecule S100P inhibitors for drug candidate development.

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S100 to receptor for advanced glycation end-products binding assay: Looking for inhibitors

Cited by 11 publications

References 22 publications

Al₂O₃microring resonators for the detection of a cancer biomarker in undiluted urine

Al₂O₃microring resonators for the detection of a cancer biomarker in undiluted urine

Interaction of extracellular S100A4 with RAGE prompts prometastatic activation of A375 melanoma cells

Discovery of novel small molecule inhibitors of S100P with in vitro anti-metastatic effects on pancreatic cancer cells

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S100 to receptor for advanced glycation end-products binding assay: Looking for inhibitors

Cited by 11 publications

References 22 publications

Al2O3microring resonators for the detection of a cancer biomarker in undiluted urine

Al2O3microring resonators for the detection of a cancer biomarker in undiluted urine

Interaction of extracellular S100A4 with RAGE prompts prometastatic activation of A375 melanoma cells

Discovery of novel small molecule inhibitors of S100P with in vitro anti-metastatic effects on pancreatic cancer cells

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Al₂O₃microring resonators for the detection of a cancer biomarker in undiluted urine

Al₂O₃microring resonators for the detection of a cancer biomarker in undiluted urine