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Structure paper

タイトルStructural basis of mammalian respiratory complex I inhibition by medicinal biguanides.
ジャーナル・号・ページScience, Vol. 379, Issue 6630, Page 351-357, Year 2023
掲載日2023年1月27日
著者Hannah R Bridges / James N Blaza / Zhan Yin / Injae Chung / Michael N Pollak / Judy Hirst /
PubMed 要旨The molecular mode of action of biguanides, including the drug metformin, which is widely used in the treatment of diabetes, is incompletely characterized. Here, we define the inhibitory drug-target ...The molecular mode of action of biguanides, including the drug metformin, which is widely used in the treatment of diabetes, is incompletely characterized. Here, we define the inhibitory drug-target interaction(s) of a model biguanide with mammalian respiratory complex I by combining cryo-electron microscopy and enzyme kinetics. We interpret these data to explain the selectivity of biguanide binding to different enzyme states. The primary inhibitory site is in an amphipathic region of the quinone-binding channel, and an additional binding site is in a pocket on the intermembrane-space side of the enzyme. An independent local chaotropic interaction, not previously described for any drug, displaces a portion of a key helix in the membrane domain. Our data provide a structural basis for biguanide action and enable the rational design of medicinal biguanides.
リンクScience / PubMed:36701435 / PubMed Central
手法EM (単粒子)
解像度2.17 - 3.5 Å
構造データ

EMDB-14126: Bovine complex I in the slack state at 3.5 A
手法: EM (単粒子) / 解像度: 3.5 Å

14127

7qsd

EMDB-14127, PDB-7qsd:
Bovine complex I in the active state at 3.1 A
手法: EM (単粒子) / 解像度: 3.1 Å

EMDB-14128: Bovine complex I in the active state at 3.1 A (Composite map)
手法: EM (単粒子) / 解像度: 2.8 Å

EMDB-14129: Bovine complex I in the active state at 3.1 A (Hydrophlic domain)
手法: EM (単粒子) / 解像度: 3.1 Å

EMDB-14130: Bovine complex I in the active state at 3.1 A (Proximal hydrophobic domain)
手法: EM (単粒子) / 解像度: 3.3 Å

EMDB-14131: Bovine complex I in the active state at 3.1 A (Distal hydrophobic domain)
手法: EM (単粒子) / 解像度: 3.4 Å

14251

7r41

EMDB-14251, PDB-7r41:
Bovine complex I in the presence of IM1761092, active class i (Composite map)
手法: EM (単粒子) / 解像度: 2.3 Å

EMDB-14252: Bovine complex I in the presence of IM1761092, active class i (Consensus)
手法: EM (単粒子) / 解像度: 2.44 Å

EMDB-14253: Bovine complex I in the presence of IM1761092, active class i (Hydophilic domain)
手法: EM (単粒子) / 解像度: 2.32 Å

EMDB-14254: Bovine complex I in the presence of IM1761092, active class i (Proximal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.41 Å

EMDB-14255: Bovine complex I in the presence of IM1761092, active class i (Distal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.51 Å

14256

7r42

EMDB-14256, PDB-7r42:
Bovine complex I in the presence of IM1761092, active class ii (Composite map)
手法: EM (単粒子) / 解像度: 2.3 Å

EMDB-14257: Bovine complex I in the presence of IM1761092, active class ii (Consensus map)
手法: EM (単粒子) / 解像度: 2.42 Å

EMDB-14258: Bovine complex I in the presence of IM1761092, active class ii (Hydrophilic domain)
手法: EM (単粒子) / 解像度: 2.31 Å

EMDB-14259: Bovine complex I in the presence of IM1761092, active class ii (Proximal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.41 Å

EMDB-14260: Bovine complex I in the presence of IM1761092, active class ii (Distal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.47 Å

14261

7r43

EMDB-14261, PDB-7r43:
Bovine complex I in the presence of IM1761092, active class iii (Composite map)
手法: EM (単粒子) / 解像度: 2.4 Å

EMDB-14262: Bovine complex I in the presence of IM1761092, active class iii (Consensus)
手法: EM (単粒子) / 解像度: 2.61 Å

EMDB-14263: Bovine complex I in the presence of IM1761092, active class iii (Hydrophilic domain)
手法: EM (単粒子) / 解像度: 2.46 Å

EMDB-14264: Bovine complex I in the presence of IM1761092, active class iii (Proximal membrane domain)
手法: EM (単粒子) / 解像度: 2.58 Å

EMDB-14265: Bovine complex I in the presence of IM1761092, active class iii (Distal membrane domain)
手法: EM (単粒子) / 解像度: 2.62 Å

14266

7r44

EMDB-14266, PDB-7r44:
Bovine complex I in the presence of IM1761092, active class iv (Composite map)
手法: EM (単粒子) / 解像度: 2.4 Å

EMDB-14267: Bovine complex I in the presence of IM1761092, active class iv (Consensus)
手法: EM (単粒子) / 解像度: 2.55 Å

EMDB-14268: Bovine complex I in the presence of IM1761092, active class iv (Hydrophilic domain)
手法: EM (単粒子) / 解像度: 2.41 Å

EMDB-14269: Bovine complex I in the presence of IM1761092, active class iv (Proximal membrane domain)
手法: EM (単粒子) / 解像度: 2.54 Å

EMDB-14270: Bovine complex I in the presence of IM1761092, active class iv (Distal membrane domain)
手法: EM (単粒子) / 解像度: 2.64 Å

14272

7r45

EMDB-14272, PDB-7r45:
Bovine complex I in the presence of IM1761092, deactive class i (Composite map)
手法: EM (単粒子) / 解像度: 2.4 Å

EMDB-14273: Bovine complex I in the presence of IM1761092, deactive class i (Consensus)
手法: EM (単粒子) / 解像度: 2.44 Å

EMDB-14274: Bovine complex I in the presence of IM1761092, deactive class i (Hydrophilic domain)
手法: EM (単粒子) / 解像度: 2.3 Å

EMDB-14275: Bovine complex I in the presence of IM1761092, deactive class i (Proximal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.46 Å

EMDB-14276: Bovine complex I in the presence of IM1761092, deactive class i (Distal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.47 Å

14277

7r46

EMDB-14277, PDB-7r46:
Bovine complex I in the presence of IM1761092, deactive class ii (Composite map)
手法: EM (単粒子) / 解像度: 2.4 Å

EMDB-14278: Bovine complex I in the presence of IM1761092, deactive class ii (Consensus)
手法: EM (単粒子) / 解像度: 2.57 Å

EMDB-14279: Bovine complex I in the presence of IM1761092, deactive class ii (Hydrophilic domain)
手法: EM (単粒子) / 解像度: 2.44 Å

EMDB-14280: Bovine complex I in the presence of IM1761092, deactive class ii (Proximal membrane domain)
手法: EM (単粒子) / 解像度: 2.55 Å

EMDB-14281: Bovine complex I in the presence of IM1761092, deactive class ii (Distal membrane domain)
手法: EM (単粒子) / 解像度: 2.61 Å

14282

7r47

EMDB-14282, PDB-7r47:
Bovine complex I in the presence of IM1761092, deactive class iii (Composite map)
手法: EM (単粒子) / 解像度: 2.3 Å

EMDB-14283: Bovine complex I in the presence of IM1761092, deactive class iii (Consensus)
手法: EM (単粒子) / 解像度: 2.31 Å

EMDB-14284: Bovine complex I in the presence of IM1761092, deactive class iii (Hydrophilic domain)
手法: EM (単粒子) / 解像度: 2.17 Å

EMDB-14285: Bovine complex I in the presence of IM1761092, deactive class iii (Proximal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.29 Å

EMDB-14286: Bovine complex I in the presence of IM1761092, deactive class iii (Distal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.34 Å

14287

7r48

EMDB-14287, PDB-7r48:
Bovine complex I in the presence of IM1761092, deactive class iv (Composite map)
手法: EM (単粒子) / 解像度: 2.3 Å

EMDB-14288: Bovine complex I in the presence of IM1761092, deactive class iv (Consensus)
手法: EM (単粒子) / 解像度: 2.34 Å

EMDB-14289: Bovine complex I in the presence of IM1761092, deactive class iv (Hydrophilic domain)
手法: EM (単粒子) / 解像度: 2.19 Å

EMDB-14290: Bovine complex I in the presence of IM1761092, deactive class iv (Proximal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.34 Å

EMDB-14291: Bovine complex I in the presence of IM1761092, deactive class iv (Distal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.38 Å

14292

7r4c

EMDB-14292, PDB-7r4c:
Bovine complex I in the presence of IM1761092, deactive class v (Composite map)
手法: EM (単粒子) / 解像度: 2.3 Å

EMDB-14293: Bovine complex I in the presence of IM1761092, deactive class v (Consensus)
手法: EM (単粒子) / 解像度: 2.38 Å

EMDB-14294: Bovine complex I in the presence of IM1761092, deactive class v (Hydrophilic domain)
手法: EM (単粒子) / 解像度: 2.22 Å

EMDB-14295: Bovine complex I in the presence of IM1761092, deactive class v (Proximal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.38 Å

EMDB-14296: Bovine complex I in the presence of IM1761092, deactive class v (Distal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.4 Å

14297

7r4d

EMDB-14297, PDB-7r4d:
Bovine complex I in the presence of IM1761092, deactive class vi (Composite map)
手法: EM (単粒子) / 解像度: 2.3 Å

EMDB-14298: Bovine complex I in the presence of IM1761092, deactive class vi (Consensus)
手法: EM (単粒子) / 解像度: 2.33 Å

EMDB-14299: Bovine complex I in the presence of IM1761092, deactive class vi (Hydrophilic domain)
手法: EM (単粒子) / 解像度: 2.19 Å

EMDB-14300: Bovine complex I in the presence of IM1761092, deactive class vi (Proximal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.35 Å

EMDB-14301: Bovine complex I in the presence of IM1761092, deactive class vi (Distal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.4 Å

14302

7r4f

EMDB-14302, PDB-7r4f:
Bovine complex I in the presence of IM1761092, slack class i (Composite map)
手法: EM (単粒子) / 解像度: 2.4 Å

EMDB-14303: Bovine complex I in the presence of IM1761092, slack class i (Consensus)
手法: EM (単粒子) / 解像度: 2.4 Å

EMDB-14304: Bovine complex I in the presence of IM1761092, slack class i (Hydrophilic domain)
手法: EM (単粒子) / 解像度: 2.2 Å

EMDB-14305: Bovine complex I in the presence of IM1761092, slack class i (Proximal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.41 Å

EMDB-14306: Bovine complex I in the presence of IM1761092, slack class i (Distal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.47 Å

14307

7r4g

EMDB-14307, PDB-7r4g:
Bovine complex I in the presence of IM1761092, slack class ii (Composite map)
手法: EM (単粒子) / 解像度: 2.5 Å

EMDB-14308: Bovine complex I in the presence of IM1761092, slack class ii (Consensus)
手法: EM (単粒子) / 解像度: 2.61 Å

EMDB-14309: Bovine complex I in the presence of IM1761092, slack class ii (Hydrophillic domain)
手法: EM (単粒子) / 解像度: 2.37 Å

EMDB-14310: Bovine complex I in the presence of IM1761092, slack class ii (Proximal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.62 Å

EMDB-14311: Bovine complex I in the presence of IM1761092, slack class ii (Distal hydrophobic domain)
手法: EM (単粒子) / 解像度: 2.68 Å

化合物

ChemComp-PC1:
1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE / リン脂質*YM

ChemComp-3PE:
1,2-Distearoyl-sn-glycerophosphoethanolamine / DSPE / リン脂質*YM

ChemComp-SF4:
IRON/SULFUR CLUSTER

ChemComp-FES:
FE2/S2 (INORGANIC) CLUSTER

ChemComp-FMN:
FLAVIN MONONUCLEOTIDE / FMN

ChemComp-CDL:
CARDIOLIPIN / リン脂質*YM

ChemComp-LMT:
DODECYL-BETA-D-MALTOSIDE / ドデシルβ-D-マルトシド / 可溶化剤*YM

ChemComp-GTP:
GUANOSINE-5'-TRIPHOSPHATE / GTP / GTP, エネルギー貯蔵分子*YM

ChemComp-MG:
Unknown entry / マグネシウムジカチオン

ChemComp-NDP:
NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE / NADPH

ChemComp-ZN:
Unknown entry

ChemComp-EHZ:
~{S}-[2-[3-[[(2~{R})-3,3-dimethyl-2-oxidanyl-4-phosphonooxy-butanoyl]amino]propanoylamino]ethyl] (3~{S})-3-oxidanyltetradecanethioate

ChemComp-K:
Unknown entry / カリウムカチオン

ChemComp-I49:
1-carbamimidoyl-3-[2-(3-chloranyl-4-iodanyl-phenyl)ethyl]guanidine

ChemComp-MYR:
MYRISTIC ACID / ミリスチン酸

ChemComp-HOH:
WATER

由来
  • bos taurus (ウシ)
  • cattle (ウシ)
キーワードOXIDOREDUCTASE / Complex I

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