Inhibition of Chondrocyte Hypertrophy of Osteoarthritis by Disruptor Peptide

Abstract

The goal of this research project is to characterize how disruptor peptide blocks beta-catenin interaction with PTH receptor, and inhibits chondrocyte hypertrophy in vitro and in vivo. We designed a disruptor peptide corresponding to the carboxyl-terminal region of PTH receptor, and found this disruptor peptide inhibited beta-catenin binding to PTH receptor by GST-pull down assay. We also confirmed that disruptor peptide conjugated to penetratin can enter cells. Importantly, disruptor peptide reversed the beta-catenin-mediated PTH receptor signaling switch by increasing Gs/cAMP signaling and inhibiting Gq/PLC activation in wild-type and beta-catenin knockout cells by using CRISPR/Cas9 genome-editing technology. In addition, the disruptor peptide enhanced PTHrP stimulated chondrogenesis and promoted PTHrP-inhibited chondrocyte hypertrophy. Furthermore, in mouse osteoarthritis model surgically induced by destabilization of the medial meniscus, articular-injection of PTHrP inhibited both type X collagen (hypertrophic marker) and matrix metalloproteinase 13 (catabolic enzyme). These data suggest that the disruptor peptide favors the therapeutic signaling arm and improves the ability of PTHrP to inhibit cartilage degeneration and treat/prevent osteoarthritis.

Open PDF

Document Details

Document Type
Technical Report
Publication Date
Apr 01, 2019
Accession Number
AD1093786

Entities

People

  • Bin Wang

Organizations

  • Thomas Jefferson University

Tags

DTIC Thesaurus Topics

  • Amino Acids
  • Arthritis
  • Biomedical And Dental Materials
  • Bone And Bones
  • Bone Diseases
  • Cartilage
  • Cell Membrane
  • Cell Physiological Processes
  • Cells
  • Chemistry
  • Enzyme Inhibitors
  • Medical Personnel
  • Orthopedics
  • Osteogenesis
  • Osteoporosis
  • Peptides
  • Proteins

Fields of Study

  • Biology
  • Computer science

Readers

  • Immunology and Pathology
  • Molecular and Cellular Biochemistry
  • Neurotoxicology

Technology Areas

  • Biotechnology