Targeted protein oxidation using a chromophore-modified rapamycin analog

Courtney, Taylor; Hankinson, Chasity P.; Horst, Trevor J.; Deiters, Alexander

doi:10.1039/d1sc04464h

Chem. Sci.

2021

DOI: 10.1039/d1sc04464h

|View full text |Cite

Targeted protein oxidation using a chromophore-modified rapamycin analog

Taylor Courtney

Chasity P. Hankinson

Trevor J. Horst

et al.

Abstract: Utilization of a ROS-generating chromophore for the development of reversible control of rapamycin-induced protein dimerization via targeted oxidation.

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

2021

2024

Publication Types

Select...

Article4

Relationship

Self Cite0

Independent4

Authors

Journals

Cited by 4 publications

References 58 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Ligand‐Enabled Pd‐Catalyzed sp³ C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Bi,

Cui,

Liu

et al. 2024

Angewandte Chemie

View full text Add to dashboard Cite

The development of simplified synthetic strategy to create structurally and functionally diverse pseudo‐natural macrocyclic molecules is highly appealing but poses a marked challenge. Inspired by natural scaffolds, herein, we describe a practical and concise ligand‐enabled Pd(II)‐catalysed sp3 C‒H alkylation, olefination and arylation macrocyclization, which could offer a novel set of pseudo‐natural macrocyclic sulfonamides. Interestingly, the potential of ligand acceleration in C‒H activation is also demonstrated by an unprecedented enantioselective sp3 C‒H alkylation macrocyclization. Moreover, a combination of in silico screening and biological evaluation led to the identification of a novel spiro‐grafted macrocyclic sulfonamide 2a, which showed a promising efficacy for the treatment of Parkinson’s disease (PD) in a mouse model through the activation of silent information regulator sirtuin 3 (SIRT3).

show abstract

Ligand‐Enabled Pd‐Catalyzed sp³ C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Bi,

Cui,

Liu

et al. 2024

Angewandte Chemie

View full text Add to dashboard Cite

show abstract

Ligand‐Enabled Pd‐Catalyzed sp³ C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Bi,

Cui,

Liu

et al. 2024

Angew Chem Int Ed

View full text Add to dashboard Cite

show abstract

Rapamycin functionalized carbon Dots: Target-oriented synthesis and suppression of vascular cell senescence

Dong,

Wang,

et al. 2024

Journal of Colloid and Interface Science

View full text Add to dashboard Cite

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Targeted protein oxidation using a chromophore-modified rapamycin analog

Abstract: Utilization of a ROS-generating chromophore for the development of reversible control of rapamycin-induced protein dimerization via targeted oxidation.

Cited by 4 publications

References 58 publications

Ligand‐Enabled Pd‐Catalyzed sp³ C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Ligand‐Enabled Pd‐Catalyzed sp³ C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Ligand‐Enabled Pd‐Catalyzed sp³ C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Rapamycin functionalized carbon Dots: Target-oriented synthesis and suppression of vascular cell senescence

Contact Info

Product

Resources

About

Targeted protein oxidation using a chromophore-modified rapamycin analog

Abstract: Utilization of a ROS-generating chromophore for the development of reversible control of rapamycin-induced protein dimerization via targeted oxidation.

Cited by 4 publications

References 58 publications

Ligand‐Enabled Pd‐Catalyzed sp3 C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Ligand‐Enabled Pd‐Catalyzed sp3 C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Ligand‐Enabled Pd‐Catalyzed sp3 C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Rapamycin functionalized carbon Dots: Target-oriented synthesis and suppression of vascular cell senescence

Contact Info

Product

Resources

About

Ligand‐Enabled Pd‐Catalyzed sp³ C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Ligand‐Enabled Pd‐Catalyzed sp³ C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease

Ligand‐Enabled Pd‐Catalyzed sp³ C−H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease