EMDB/PDB/SASBDBから引用されている文献のデータベース

キーワード
構造解析手法	All X線回折 NMR 電子顕微鏡小角散乱中性子線回折線維回折粉末回折赤外分光 EPR FRET 理論モデルハイブリッド
著者・登録者
ジャーナル
IF	>30 >20 >10 >5 all

タイトル	A structural basis for amylin receptor phenotype.
ジャーナル・号・ページ	Science, Vol. 375, Issue 6587, Page eabm9609, Year 2022
掲載日	2022年3月25日
著者	Jianjun Cao / Matthew J Belousoff / Yi-Lynn Liang / Rachel M Johnson / Tracy M Josephs / Madeleine M Fletcher / Arthur Christopoulos / Debbie L Hay / Radostin Danev / Denise Wootten / Patrick M Sexton /
PubMed 要旨	Amylin receptors (AMYRs) are heterodimers of the calcitonin (CT) receptor (CTR) and one of three receptor activity-modifying proteins (RAMPs), AMYR, AMYR, and AMYR. Selective AMYR agonists and dual ...Amylin receptors (AMYRs) are heterodimers of the calcitonin (CT) receptor (CTR) and one of three receptor activity-modifying proteins (RAMPs), AMYR, AMYR, and AMYR. Selective AMYR agonists and dual AMYR/CTR agonists are being developed as obesity treatments; however, the molecular basis for peptide binding and selectivity is unknown. We determined the structure and dynamics of active AMYRs with amylin, AMYR with salmon CT (sCT), AMYR with sCT or human CT (hCT), and CTR with amylin, sCT, or hCT. The conformation of amylin-bound complexes was similar for all AMYRs, constrained by the RAMP, and an ordered midpeptide motif that we call the bypass motif. The CT-bound AMYR complexes were distinct, overlapping the CT-bound CTR complexes. Our findings indicate that activation of AMYRs by CT-based peptides is distinct from their activation by amylin-based peptides. This has important implications for the development of AMYR therapeutics.
リンク	Science / PubMed:35324283
手法	EM (単粒子)
解像度	2.2 - 3.3 Å
構造データ	26178 7tyf EMDB-26178, PDB-7tyf: Human Amylin1 Receptor in complex with Gs and rat amylin peptide 手法: EM (単粒子) / 解像度: 2.2 Å 26179 7tyh EMDB-26179, PDB-7tyh: Human Amylin2 Receptor in complex with Gs and human calcitonin peptide 手法: EM (単粒子) / 解像度: 3.3 Å 26180 7tyi EMDB-26180, PDB-7tyi: Calcitonin Receptor in complex with Gs and rat amylin peptide, CT-like state 手法: EM (単粒子) / 解像度: 3.3 Å 26184 7tyl EMDB-26184, PDB-7tyl: Calcitonin Receptor in complex with Gs and rat amylin peptide, bypass motif 手法: EM (単粒子) / 解像度: 3.3 Å 26188 7tyn EMDB-26188, PDB-7tyn: Calcitonin Receptor in complex with Gs and salmon calcitonin peptide 手法: EM (単粒子) / 解像度: 2.6 Å 26190 7tyo EMDB-26190, PDB-7tyo: Calcitonin receptor in complex with Gs and human calcitonin peptide 手法: EM (単粒子) / 解像度: 2.7 Å 26196 7tyw EMDB-26196, PDB-7tyw: Human Amylin1 Receptor in complex with Gs and salmon calcitonin peptide 手法: EM (単粒子) / 解像度: 3.0 Å 26197 7tyx EMDB-26197, PDB-7tyx: Human Amylin2 Receptor in complex with Gs and rat amylin peptide 手法: EM (単粒子) / 解像度: 2.55 Å 26199 7tyy EMDB-26199, PDB-7tyy: Human Amylin2 Receptor in complex with Gs and salmon calcitonin peptide 手法: EM (単粒子) / 解像度: 3.0 Å 26208 7tzf EMDB-26208, PDB-7tzf: Human Amylin3 Receptor in complex with Gs and rat amylin peptide 手法: EM (単粒子) / 解像度: 2.4 Å
化合物	ChemComp-NAG: 2-acetamido-2-deoxy-beta-D-glucopyranose ChemComp-PLM: PALMITIC ACID ChemComp-Y01: CHOLESTEROL HEMISUCCINATE ChemComp-P42: (2S)-2-{[(1R)-1-hydroxyhexadecyl]oxy}-3-{[(1R)-1-hydroxyoctadecyl]oxy}propyl 2-(trimethylammonio)ethyl phosphate / SPPC, リン脂質YM ChemComp-PTY: PHOSPHATIDYLETHANOLAMINE / リン脂質YM ChemComp-HOH: WATER
由来	homo sapiens (ヒト) lama glama (ラマ) rattus norvegicus (ドブネズミ) salmo salar (タイセイヨウサケ)
キーワード	MEMBRANE PROTEIN / Amylin receptor / GPCR / RAMP / RAMP2 / human calcitonin / calcitonin / CT-like / Amylin / bypass motif / calcitonin receptor / salmon calcitonin / RAMP1 / RAMP3 / rat amylin