Molecular basis of promiscuous chemokine binding and structural mimicry at the C-X-C chemokine receptor, CXCR2.

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Tác giả: Hiroaki Akasaka, Nilanjana Banerjee, Ramanuj Banerjee, Andy Chevigné, Annu Dalal, Manisankar Ganguly, Yuzuru Itoh, Takaaki A Kobayashi, Sudha Mishra, Samanwita Mohapatra, Osamu Nureki, Nabarun Roy, Sayantan Saha, Shirsha Saha, Fumiya K Sano, Saloni Sharma, Wataru Shihoya, Arun K Shukla, Divyanshu Tiwari, Manish K Yadav, Nashrah Zaidi

Ngôn ngữ: eng

Ký hiệu phân loại: 155.282 Diagnostic graphology

Thông tin xuất bản: United States : Molecular cell , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 226427

 Selectivity of natural agonists for their cognate receptors is a hallmark of G-protein-coupled receptors (GPCRs)
  however, this selectivity often breaks down at the chemokine receptors. Chemokines often display promiscuous binding to chemokine receptors, but the underlying molecular determinants remain mostly elusive. Here, we perform a comprehensive transducer-coupling analysis, testing all known C-X-C chemokines on every C-X-C type chemokine receptor to generate a global fingerprint of the selectivity and promiscuity encoded within this system. Taking lead from this, we determine cryoelectron microscopy (cryo-EM) structures of the most promiscuous receptor, C-X-C chemokine receptor 2 (CXCR2), in complex with several chemokines. These structural snapshots elucidate the details of ligand-receptor interactions, including structural motifs, which are validated using mutagenesis and functional experiments. We also observe that most chemokines position themselves on CXCR2 as a dimer while CXCL6 exhibits a monomeric binding pose. Taken together, our findings provide the molecular basis of chemokine promiscuity at CXCR2 with potential implications for developing therapeutic molecules.
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