3N94

Crystal structure of human pituitary adenylate cyclase 1 Receptor-short N-terminal extracellular domain

3N94 の概要

• エントリーDOI: 10.2210/pdb3n94/pdb
• 関連するBIRD辞書のPRD_ID: PRD_900001
• 分子名称: Fusion protein of Maltose-binding periplasmic protein and pituitary adenylate cyclase 1 Receptor-short, alpha-D-glucopyranose-(1-4)-alpha-D-glucopyranose, SULFATE ION, ... (4 entities in total)
• 機能のキーワード: g-protein coupled receptor, mbp fusion protein, membrane receptor, peptide hormone receptor
• 由来する生物種: Escherichia coli; 詳細
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 53175.82

構造登録者

Kumar, S.,Pioszak, A.A.,Swaminathan, K.,Xu, H.E. (登録日: 2010-05-28, 公開日: 2011-06-08, 最終更新日: 2024-10-16)

主引用文献

Kumar, S.,Pioszak, A.,Zhang, C.,Swaminathan, K.,Xu, H.E.
Crystal Structure of the PAC1R Extracellular Domain Unifies a Consensus Fold for Hormone Recognition by Class B G-Protein Coupled Receptors.
Plos One, 6:e19682-e19682, 2011

PubMed Abstract: Pituitary adenylate cyclase activating polypeptide (PACAP) is a member of the PACAP/glucagon family of peptide hormones, which controls many physiological functions in the immune, nervous, endocrine, and muscular systems. It activates adenylate cyclase by binding to its receptor, PAC1R, a member of class B G-protein coupled receptors (GPCR). Crystal structures of a number of Class B GPCR extracellular domains (ECD) bound to their respective peptide hormones have revealed a consensus mechanism of hormone binding. However, the mechanism of how PACAP binds to its receptor remains controversial as an NMR structure of the PAC1R ECD/PACAP complex reveals a different topology of the ECD and a distinct mode of ligand recognition. Here we report a 1.9 Å crystal structure of the PAC1R ECD, which adopts the same fold as commonly observed for other members of Class B GPCR. Binding studies and cell-based assays with alanine-scanned peptides and mutated receptor support a model that PAC1R uses the same conserved fold of Class B GPCR ECD for PACAP binding, thus unifying the consensus mechanism of hormone binding for this family of receptors.

PubMed: 21625560
DOI: 10.1371/journal.pone.0019682

実験手法

X-RAY DIFFRACTION (1.8 Å)