2023
DOI: 10.1021/acs.jmedchem.3c00594
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Discovery and Design of Novel Cyclic Peptides as Specific Inhibitors Targeting CCN2 and Disrupting CCN2/EGFR Interaction for Kidney Fibrosis Treatment

Abstract: Kidney fibrosis is a serious consequence of chronic kidney disease (CKD), and currently, there is no effective pharmacological treatment available. Cellular communication network-2 (CCN2/CTGF) is an extracellular matrix (ECM) protein that regulates the fibrotic process by activating the epidermal growth factor receptor (EGFR) signaling pathway. We herein present the discovery and structure−activity relationship study of novel peptides targeting CCN2 to develop potent and stable specific inhibitors of the CCN2/… Show more

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Cited by 8 publications
(2 citation statements)
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“…However, the application of this natural peptide in fibrotic diseases has been limited due to its high instability and poor half-life ( T 1/2 = 0.098 h). Inspired by our recent research efforts on the design of functional peptide skeletons, structure–activity relationships, and pharmacological mechanisms in the field of fibrotic diseases, ,, we present here the design and discovery of a new library of ultralong-acting peptides as antagonists targeting elastin-binding proteins for the treatment of PF ( T 1/2 = 33.0 h). The observed prolongation of plasma half-life is likely due to the increasing length of fatty acid chains .…”
Section: Discussionmentioning
confidence: 99%
“…However, the application of this natural peptide in fibrotic diseases has been limited due to its high instability and poor half-life ( T 1/2 = 0.098 h). Inspired by our recent research efforts on the design of functional peptide skeletons, structure–activity relationships, and pharmacological mechanisms in the field of fibrotic diseases, ,, we present here the design and discovery of a new library of ultralong-acting peptides as antagonists targeting elastin-binding proteins for the treatment of PF ( T 1/2 = 33.0 h). The observed prolongation of plasma half-life is likely due to the increasing length of fatty acid chains .…”
Section: Discussionmentioning
confidence: 99%
“…Our research group is dedicated to discovering peptide drugs for the treatment of fibrotic diseases. Therefore, we have developed peptide drugs targeting GPR55, a recently identified target that affects liver fibrosis. …”
Section: Discussionmentioning
confidence: 99%