Fibroblast activation protein alpha: Comprehensive detection methods for drug target and tumor marker

Song, Pei-Fang; Pan, Quisha; Sun, Zhao-Hui; Zou, Liwei; Yang, Ling

doi:10.1016/j.cbi.2022.109830

Cited by 11 publications

(7 citation statements)

References 98 publications

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“…54 Upon enzymatic cleavage of the DEVD peptide by caspase-3, the solubility of the obtained probe significantly decreased, which 4a). 55 The Cbz-GP peptide sequence within the probe can be enzymatically cleaved by fibroblast activation protein α (FAP-α), 56 which results in the generation of C(StBu)K(Cou)-CBT. Subsequently, the reduction of disulfide bonds facilitated by GSH triggers a CBT-Cys click reaction, thereby leading to the formation of cyclic Cou-CBT-dimers.…”

Section: Fluorescence Imaging (Fli)mentioning

confidence: 99%

“…Taking advantage of this characteristic, Gao et al developed a “smart” fluorescent probe Cbz-Gly-Pro-Cys(StBu)-Lys(coumarin)-CBT [ Cbz-GPC(StBu)K(Cou)-CBT ] for tumor imaging (Figure a) . The Cbz-GP peptide sequence within the probe can be enzymatically cleaved by fibroblast activation protein α (FAP-α), which results in the generation of C(StBu)K(Cou)-CBT . Subsequently, the reduction of disulfide bonds facilitated by GSH triggers a CBT-Cys click reaction, thereby leading to the formation of cyclic Cou-CBT-dimers .…”

Section: Bioimaging Applications Of Enzyme-instructed Cbt-cys-like Cl...mentioning

confidence: 99%

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Enzyme-Instructed CBT-Cys-like Click Cyclization Reactions for Bioimaging

Yang,

Liu,

et al. 2023

Chemical & Biomedical Imaging

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With high efficiency, mild conditions, and rapid reaction rate, click reactions have garnered much attention in the field of bioimaging since proposed by Sharpless et al. in 2001 (Angew. Chem., Int. Ed. 2001, 40, 2004. Inspired by the regenerative pathway of D-luciferin in fireflies, Liang et al. (Nat. Chem. 2010, 2, 54−60) raised a 2-cyanobenzothiazole (CBT)-cysteine (Cys) click condensation reaction in 2010, which exhibits a higher secondorder reaction rate (9.19 M −1 s −1 ) and superior biocompatibility. As it has been developed in the past decade, remarkable progress has been made in the construction of enzyme-instructed CBT-Cys-based bioimaging probes. This review introduces the concept of the CBT-Cys click reaction, elucidates the mechanism of the CBT-Cys click reaction, and concerns the development progress of CBT-Cys reaction and its derived reactions [i.e., 2-cyano-6hydroxyquinoline (CHQ)-Cys reaction and 2-pyrimidinecarbonitrile (PMN)-Cys reaction]. Furthermore, we give a comprehensive and up-to-date review of enzyme-instructed CBT-Cyslike click reaction-based probes with significantly enhanced imaging signal and contrast for various bioimaging modes, including fluorescence imaging, photoacoustic imaging, magnetic resonance imaging, and positron emission tomography. In the end, we discuss the possible challenges and opportunities that may arise in the future.

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Section: Fluorescence Imaging (Fli)mentioning

confidence: 99%

Section: Bioimaging Applications Of Enzyme-instructed Cbt-cys-like Cl...mentioning

confidence: 99%

Enzyme-Instructed CBT-Cys-like Click Cyclization Reactions for Bioimaging

Yang,

Liu,

et al. 2023

Chemical & Biomedical Imaging

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“…By targeting FAP, Talabostat is able to suppress cancer cell proliferation, migration and invasion. In the context of anti-cancer, mechanisms of Talabostat in suppressing cancer progression are complex (Song et al 2022). Currently, Talabostat is found to induce oxidative stress to threaten cancer cells (Yang et al 2023).…”

Section: Introductionmentioning

confidence: 99%

Fibroblast activation protein as a biomarker for containment of triple-negative breast cancer

Chen,

Li,

Zhang

2024

Preprint

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Objectives The aim of this study was to investigate effect of Talabostat (a fibroblast activation protein inhibitor) on the cell viability of MDA-MB-231 cells and organoids. And the mechanism of containment of cells and organoids was also studied. Methods Cell viability of cells was demonstrated through some assays, including CCK-8, Transwell, etc. Potential mechanisms were investigated through TEM, TUNEL staining, western blot and flow cytometry. Results It was found that the cell viability and migration of MDA-MB-231 cells were inhibited by Talabostat (one kind of FAP inhibitor). And the mitochondria-mediated apoptosis induced by Talabostat was considered as the proliferation suppression mechanism, which was certified by RNA sequencing results. More importantly, the proliferation inhibitions of organoids induced by Talabostat were realized, which suggests the repression of FAP for TNBC treatment has strong clinical values. Conclusions Herein, the therapy effect of Talabostat on triple-negative breast cancer was investigated systematically, and it was found that the cell viability and migration of MDA-MB-231 cells were inhibited by Talabostat. And the mitochondria-mediated apoptosis induced by Talabostat was considered as the proliferation suppression mechanism, which was certified by RNA sequencing results. Importantly, the proliferation inhibitions of organoids induced by Talabostat were realized, which suggests the repression of FAP for TNBC treatment has strong clinical values. Our findings shed new lights on the promising treatment strategies for TNBC.

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“…As a type-II transmembrane serine protease, FAP-α is overexpressed in more than 90% of epithelial tumors but negligible in almost all normal tissues in humans. 28 It promotes tumor growth and invasiveness through extracellular matrix remodeling. 29 Therefore, FAP-α is considered as a promising target for tumor diagnosis.…”

mentioning

confidence: 99%

“…Hence, as a proof-of-concept, we designed a “smart” fluorescence probe Cbz-Gly-Pro-Cys(StBu)-Lys(coumarin)-CBT ( Cbz-GPC(StBu)K(Cou)-CBT ), which, upon fibroblast activation protein alpha (FAP-α)-activation, subjected to the CBT-Cys click reaction self-assembles into nanoparticle Cou-CBT-NP , turning coumarin excimer fluorescence “on” for high contrast tumor imaging. As a type-II transmembrane serine protease, FAP-α is overexpressed in more than 90% of epithelial tumors but negligible in almost all normal tissues in humans . It promotes tumor growth and invasiveness through extracellular matrix remodeling .…”

mentioning

confidence: 99%

FAP-α-Instructed Coumarin Excimer Formation for High Contrast Fluorescence Imaging of Tumor

et al. 2022

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Emissive excimers, which are formed by planar polycyclic aromatic fluorophores (e.g., coumarin), enable high contrast tumor imaging. However, it is still challenging to "turn on" excimer fluorescence in physiological dilute solutions. The biocompatible CBT-Cys click condensation reaction enables both intra-and intermolecular aggregations of the as-loaded fluorophores on the probe molecules, which may promote the generation of emissive excimers in a synergistic manner. As a proof-of-concept, we herein design a fluorescence probe Cbz-Gly-Pro-Cys(StBu)-Lys(coumarin)-CBT (Cbz-GPC(StBu)K(Cou)-CBT), which can be activated by FAP-α under tumor-inherent reduction conditions, undergo a CBT-Cys click reaction, and selfassemble into coumarin nanoparticle Cou-CBT-NP to "turn on" the excimer fluorescence. In vitro and in vivo studies validate that this "smart" probe realizes efficient excimer fluorescence imaging of FAP-α-overexpressed tumor cells with high contrast and enhanced accumulation, respectively. We anticipate that this probe can be applied for diagnosis of FAP-α-related diseases in the clinic in near future.

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Fibroblast activation protein alpha: Comprehensive detection methods for drug target and tumor marker

Cited by 11 publications

References 98 publications

Enzyme-Instructed CBT-Cys-like Click Cyclization Reactions for Bioimaging

Enzyme-Instructed CBT-Cys-like Click Cyclization Reactions for Bioimaging

Fibroblast activation protein as a biomarker for containment of triple-negative breast cancer

FAP-α-Instructed Coumarin Excimer Formation for High Contrast Fluorescence Imaging of Tumor

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