ArticleInorganic chemistry2021
Tuning Cyclometalated Gold(III) for Cysteine Arylation and Ligand-Directed Bioconjugation.
Article in Inorganic chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 28 citations in OpenAlex.
- Biomolecule-polymer conjugates synthesized by a combination of organometallic bioconjugation and atom transfer radical polymerization.Polymer chemistry · 2026Article
- Article
- Harnessing Organometallic Au(III) Complexes as Precision Scaffolds for Next-Generation Therapeutic and Imaging Agents.Chembiochem : a European journal of chemical biology · 2025Review
- Discovery of a Pyrazolopyridinone-Based MYC Inhibitor That Selectively Engages Intracellular c-MYC and Disrupts MYC-MAX Heterodimerization.Journal of medicinal chemistry · 2025Article
- Organometallic Oxidative Addition Complexes forBioconjugate chemistry · 2024Article
- Ultrafast Au(III)-Mediated Arylation of Cysteine.Journal of the American Chemical Society · 2024Article
- Metal-Mediated Ligand Affinity Chemistry (MLAC).Methods in molecular biology (Clifton, N.J.) · 2024Article
- A Conformationally Restricted Gold(III) Complex Elicits Antiproliferative Activity in Cancer Cells.Inorganic chemistry · 2023Article
- OrganometallicBioconjugate chemistry · 2022Article
- Gold(I)-Mediated Rapid Cyclization of Propargylated Peptides via Imine Formation.Journal of the American Chemical Society · 2022Article
- Highly Efficient Cyclization Approach of Propargylated Peptides via Gold(I)-Mediated Sequential C-N, C-O, and C-C Bond Formation.ACS central science · 2021Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Transition-metal-based approaches to selectively modify proteins hold promise in addressing challenges in chemical biology. Unique bioorthogonal chemistry can be achieved with preformed metal-based compounds; however, their utility in native protein sites within cells remain underdeveloped. Here, we tune the ancillary ligands of cyclometalated gold(III) as a reactive group, and the gold scaffold allows for rapid modification of a desired cysteine residue proximal to the ligand binding site of a target protein. Moreover, evidence for a ligand association mechanism toward C-S bond formation by X-crystallography is established. The observed reactivity of cyclometalated gold(III) enables the rational design of a cysteine-targeted covalent inhibitor of mutant KRAS. This work illustrates the potential of structure-activity relationship studies to tune kinetics of cysteine arylation and rational design of metal-mediated ligand affinity chemistry (MLAC) of native proteins.
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Registered trials
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