ArticleBioorganic & medicinal chemistry letters2012
Development of clickable active site-directed photoaffinity probes for γ-secretase.
Article in Bioorganic & medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 27 citations in OpenAlex.
- Nootropic benzothiazoles promote dendritic spine formation by targeting fascin-1.The Journal of biological chemistry · 2025Article
- Hypoxia Inducible Factor-1α binds and activates γ-secretase for Aβ production under hypoxia and cerebral hypoperfusion.Molecular psychiatry · 2022Article
- γ-Secretase inhibitors and modulators: Mechanistic insights into the function and regulation of γ-Secretase.Seminars in cell & developmental biology · 2020Review
- Structural and Chemical Biology of Presenilin Complexes.Cold Spring Harbor perspectives in medicine · 2017Review
- Identification of lipid-phosphatidylserine (PS) as the target of unbiasedly selected cancer specific peptide-peptoid hybrid PPS1.Oncotarget · 2016Article
- γ-Secretase Inhibitors and Modulators Induce Distinct Conformational Changes in the Active Sites of γ-Secretase and Signal Peptide Peptidase.ACS chemical biology · 2015Article
- Targeting the γ-/β-secretase interaction reduces β-amyloid generation and ameliorates Alzheimer's disease-related pathogenesis.Cell discovery · 2015Article
- Development of CBAP-BPyne, a probe for γ-secretase and presenilinase.MedChemComm · 2014Article
- Article
- Applications of copper-catalyzed click chemistry in activity-based protein profiling.Molecules (Basel, Switzerland) · 2014Review
- Recent advances in target characterization and identification by photoaffinity probes.Molecules (Basel, Switzerland) · 2013Review
- Development and mechanism of γ-secretase modulators for Alzheimer's disease.Biochemistry · 2013Review
- γ-Secretase modulator (GSM) photoaffinity probes reveal distinct allosteric binding sites on presenilin.The Journal of biological chemistry · 2013Article
- Target deconvolution techniques in modern phenotypic profiling.Current opinion in chemical biology · 2013Review
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
Abstract
We have developed clickable active site-directed photoaffinity probes for γ-secretase which incorporate a photoreactive benzophenone group and an alkyne handle for subsequent click chemistry mediated conjugation with azide-linked reporter tags for visualization (e.g., TAMRA-azide) or enrichment (e.g., biotin-azide) of labeled proteins. Specifically, we synthesized clickable analogs of L646 (2) and L505 (3) and validated specific labeling to presenilin-1N-terminal fragment (PS1-NTF), the active site aspartyl protease component within the γ-secretase complex. Additionally, we were able to identify signal peptide peptidase (SPP) by Western blot analysis. Furthermore, we analyzed the photo-labeled proteins in an unbiased fashion by click chemistry with TAMRA-azide followed by in-gel fluorescence detection. This approach expands the utility of γ-secretase inhibitor (GSI) photoaffinity probes in that labeled proteins can be tagged with any number of azide-linked reporters groups using a single clickable photoaffinity probe for target pull down and/or fluorescent imaging applications.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.