ArticleBioconjugate chemistry2012
Specific inhibition of sensitized protein tyrosine phosphatase 1B (PTP1B) with a biarsenical probe.
Article in Bioconjugate chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 15 citations in OpenAlex.
- Destabilization of the SHP2 and SHP1 protein tyrosine phosphatase domains by a non-conserved "backdoor" cysteine.Biochemistry and biophysics reports · 2022Article
- Targeting a Pathogenic Cysteine Mutation: Discovery of a Specific Inhibitor of Y279C SHP2.Biochemistry · 2020Article
- Osteoarthritis Is a Low-Grade Inflammatory Disease: Obesity's Involvement and Herbal Treatment.Evidence-based complementary and alternative medicine : eCAM · 2019Review
- Optimized allosteric inhibition of engineered protein tyrosine phosphatases with an expanded palette of biarsenical small molecules.Bioorganic & medicinal chemistry · 2018Article
- Activation of Engineered Protein Tyrosine Phosphatases with the Biarsenical Compound AsCy3-EDTChembiochem : a European journal of chemical biology · 2017Article
- Rotamer-Restricted Fluorogenicity of the Bis-Arsenical ReAsH.Journal of the American Chemical Society · 2016Article
- Rational design of allosteric-inhibition sites in classical protein tyrosine phosphatases.Bioorganic & medicinal chemistry · 2015Article
- Arsenic binding to proteins.Chemical reviews · 2013Review
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Protein tyrosine phosphatase 1B (PTP1B) is a key regulator of the insulin-receptor and leptin-receptor signaling pathways, and it has therefore emerged as a critical antitype-II-diabetes and antiobesity drug target. Toward the goal of generating a covalent modulator of PTP1B activity that can be used for investigating its roles in cell signaling and disease progression, we report that the biarsenical probe FlAsH-EDT(2) can be used to inhibit PTP1B variants that contain cysteine point mutations in a key catalytic loop of the enzyme. The site-specific cysteine mutations have little effect on the catalytic activity of the enzyme in the absence of FlAsH-EDT(2). Upon addition of FlAsH-EDT(2), however, the activity of the engineered PTP1B is strongly inhibited, as assayed with either small-molecule or phosphorylated-peptide PTP substrates. We show that the cysteine-rich PTP1B variants can be targeted with the biarsenical probe in either whole-cell lysates or intact cells. Together, our data provide an example of a biarsenical probe controlling the activity of a protein that does not contain the canonical tetra-cysteine biarsenical-labeling sequence CCXXCC. The targeting of "incomplete" cysteine-rich motifs could provide a general means for controlling protein activity by targeting biarsenical compounds to catalytically important loops in conserved protein domains.
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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.