Structure and function of the SIT1 proline transporter in complex with the COVID-19 receptor ACE2.


Journal

Nature communications
ISSN: 2041-1723
Titre abrégé: Nat Commun
Pays: England
ID NLM: 101528555

Informations de publication

Date de publication:
29 Jun 2024
Historique:
received: 24 05 2023
accepted: 16 05 2024
medline: 2 7 2024
pubmed: 2 7 2024
entrez: 1 7 2024
Statut: epublish

Résumé

Proline is widely known as the only proteogenic amino acid with a secondary amine. In addition to its crucial role in protein structure, the secondary amino acid modulates neurotransmission and regulates the kinetics of signaling proteins. To understand the structural basis of proline import, we solved the structure of the proline transporter SIT1 in complex with the COVID-19 viral receptor ACE2 by cryo-electron microscopy. The structure of pipecolate-bound SIT1 reveals the specific sequence requirements for proline transport in the SLC6 family and how this protein excludes amino acids with extended side chains. By comparing apo and substrate-bound SIT1 states, we also identify the structural changes that link substrate release and opening of the cytoplasmic gate and provide an explanation for how a missense mutation in the transporter causes iminoglycinuria.

Identifiants

pubmed: 38951531
doi: 10.1038/s41467-024-48921-x
pii: 10.1038/s41467-024-48921-x
doi:

Substances chimiques

Angiotensin-Converting Enzyme 2 EC 3.4.17.23
Proline 9DLQ4CIU6V
ACE2 protein, human EC 3.4.17.23
SLC6A19 protein, human 0
Amino Acid Transport Systems, Neutral 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

5503

Subventions

Organisme : Innovative Medicines Initiative (IMI)
ID : 875510
Organisme : Innovative Medicines Initiative (IMI)
ID : 875510
Organisme : Innovative Medicines Initiative (IMI)
ID : 875510
Organisme : RCUK | Biotechnology and Biological Sciences Research Council (BBSRC)
ID : BB/V018051/1
Organisme : RCUK | Biotechnology and Biological Sciences Research Council (BBSRC)
ID : BB/V018051/1
Organisme : RCUK | Biotechnology and Biological Sciences Research Council (BBSRC)
ID : BB/V018051/1
Organisme : RCUK | Biotechnology and Biological Sciences Research Council (BBSRC)
ID : BB/V018051/1

Informations de copyright

© 2024. The Author(s).

Références

Richardson, J. S. The Anatomy and Taxonomy of Protein Structure. Adv. Protein Chem. 34, 167–339 (1981).
Chou, P. Y. & Fasman, G. D. Conformational parameters for amino acids in helical, β-sheet, and random coil regions calculated from proteins. Biochemistry 13, 211–222 (1974).
pubmed: 4358939 doi: 10.1021/bi00699a001
Adzhubei, A. A. & Sternberg, M. J. E. Left-handed Polyproline II Helices Commonly Occur in Globular Proteins. J. Mol. Biol. 229, 472–493 (1993).
pubmed: 8429558 doi: 10.1006/jmbi.1993.1047
Brodsky, B. & Ramshaw, J. A. M. The collagen triple-helix structure. Matrix Biol. 15, 545–554 (1997).
pubmed: 9138287 doi: 10.1016/S0945-053X(97)90030-5
Gustafson, C. L. et al. A Slow Conformational Switch in the BMAL1 Transactivation Domain Modulates Circadian Rhythms. Mol. Cell 66, 447–457.e7 (2017).
pubmed: 28506462 pmcid: 5484534 doi: 10.1016/j.molcel.2017.04.011
Sarkar, P., Reichman, C., Saleh, T., Birge, R. B. & Kalodimos, C. G. Proline cis-trans Isomerization Controls Autoinhibition of a Signaling Protein. Mol. Cell 25, 413–426 (2007).
pubmed: 17289588 pmcid: 2566824 doi: 10.1016/j.molcel.2007.01.004
Fischer, G. & Schmid, F. X. The mechanism of protein folding. Implications of in vitro refolding models for de novo protein folding and translocation in the cell. Biochemistry 29, 2205–2212 (1990).
pubmed: 2186809 doi: 10.1021/bi00461a001
Henzi, V., Reichling, D. B., Helm, S. W. & MacDermott, A. B. L-proline activates glutamate and glycine receptors in cultured rat dorsal horn neurons. Mol. Pharm. 41, 793–801 (1992).
Bae, M. et al. SLC6A20 transporter: a novel regulator of brain glycine homeostasis and NMDAR function. EMBO Mol. Med. 13, e12632 (2021).
pubmed: 33428810 pmcid: 7863395 doi: 10.15252/emmm.202012632
Namavar, Y. et al. Psychiatric phenotypes associated with hyperprolinemia: A systematic review. Am. J. Med. Genet. 186, 289–317 (2021).
pubmed: 34302426 doi: 10.1002/ajmg.b.32869
Stevens, B. R. & Wright, E. M. Substrate specificity of the intestinal brush-border proline/sodium (IMINO) transporter. J. Membrain Biol. 87, 27–34 (1985).
doi: 10.1007/BF01870696
Kowalczuk, S. et al. Molecular cloning of the mouse IMINO system: an Na+- and Cl−dependent proline transporter. Biochem. J. 386, 417–422 (2005).
pubmed: 15689184 pmcid: 1134859 doi: 10.1042/BJ20050100
Takanaga, H., Mackenzie, B., Suzuki, Y. & Hediger, M. A. Identification of Mammalian Proline Transporter SIT1 (SLC6A20) with Characteristics of Classical System Imino. J. Biol. Chem. 280, 8974–8984 (2005).
pubmed: 15632147 doi: 10.1074/jbc.M413027200
Bröer, S. et al. Iminoglycinuria and hyperglycinuria are discrete human phenotypes resulting from complex mutations in proline and glycine transporters. J. Clin. Invest. 118, 3881–3892 (2008).
pubmed: 19033659 pmcid: 2579706 doi: 10.1172/JCI36625
Hysi, P. G. et al. Metabolome Genome-Wide Association Study Identifies 74 Novel Genomic Regions Influencing Plasma. Metabolites Lev. Metabolites 12, 61 (2022).
Yin, X. et al. Genome-wide association studies of metabolites in Finnish men identify disease-relevant loci. Nat. Commun. 13, 1644 (2022).
pubmed: 35347128 pmcid: 8960770 doi: 10.1038/s41467-022-29143-5
Kim, J.-H. et al. A Genome-Wide Association Study Identifies Potential Susceptibility Loci for Hirschsprung Disease. PLoS One 9, e110292 (2014).
pubmed: 25310821 pmcid: 4195606 doi: 10.1371/journal.pone.0110292
Lee, J. S. et al. Association Analysis of SLC6A20 Polymorphisms With Hirschsprung Disease. J. Pediatr. Gastroenterol. Nutr. 62, 64–70 (2016).
pubmed: 26049783 doi: 10.1097/MPG.0000000000000880
Xie, X. et al. Associations of SLC6A20 genetic polymorphisms with Hirschsprung’s disease in a Southern Chinese population. Biosci. Rep. 39, BSR20182290 (2019).
pubmed: 31358688 pmcid: 6692567 doi: 10.1042/BSR20182290
Chao, J. R. et al. Human retinal pigment epithelial cells prefer proline as a nutrient and transport metabolic intermediates to the retinal side. J. Biol. Chem. 292, 12895–12905 (2017).
pubmed: 28615447 pmcid: 5546030 doi: 10.1074/jbc.M117.788422
Strunnikova, N. V. et al. Transcriptome analysis and molecular signature of human retinal pigment epithelium. Hum. Mol. Genet. 19, 2468–2486 (2010).
pubmed: 20360305 pmcid: 2876890 doi: 10.1093/hmg/ddq129
Bennis, A. et al. Comparison of Mouse and Human Retinal Pigment Epithelium Gene Expression Profiles: Potential Implications for Age-Related Macular Degeneration. PLoS One 10, e0141597 (2015).
pubmed: 26517551 pmcid: 4627757 doi: 10.1371/journal.pone.0141597
Bonelli, R. et al. Identification of genetic factors influencing metabolic dysregulation and retinal support for MacTel, a retinal disorder. Commun. Biol. 4, 274 (2021).
pubmed: 33654266 pmcid: 7925591 doi: 10.1038/s42003-021-01788-w
Gao, X. R., Huang, H. & Kim, H. Genome-wide association analyses identify 139 loci associated with macular thickness in the UK Biobank cohort. Hum. Mol. Genet. 28, 1162–1172 (2019).
pubmed: 30535121 doi: 10.1093/hmg/ddy422
Vuille-dit-Bille, R. N. et al. Human intestine luminal ACE2 and amino acid transporter expression increased by ACE-inhibitors. Amino Acids 47, 693–705 (2015).
pubmed: 25534429 doi: 10.1007/s00726-014-1889-6
Shen, Y. et al. Structures of ACE2–SIT1 recognized by Omicron variants of SARS-CoV-2. Cell Discov. 8, 123 (2022).
pubmed: 36384914 pmcid: 9667838 doi: 10.1038/s41421-022-00488-x
The Severe Covid-19 GWAS Group. Genomewide Association Study of Severe Covid-19 with Respiratory Failure. N. Engl. J. Med. 383, 1522–1534 (2020).
doi: 10.1056/NEJMoa2020283
COVID-19 Host Genetics Initiative. et al. Mapping the human genetic architecture of COVID-19. Nature 600, 472–477 (2021).
doi: 10.1038/s41586-021-03767-x
The GenOMICC Investigators. et al. Genetic mechanisms of critical illness in COVID-19. Nature 591, 92–98 (2021).
doi: 10.1038/s41586-020-03065-y
Bröer, S. & Gether, U. The solute carrier 6 family of transporters: The Solute Carrier Family 6. Br. J. Pharmacol. 167, 256–278 (2012).
pubmed: 22519513 pmcid: 3481037 doi: 10.1111/j.1476-5381.2012.01975.x
Yamashita, A., Singh, S. K., Kawate, T., Jin, Y. & Gouaux, E. Crystal structure of a bacterial homologue of Na+/Cl–dependent neurotransmitter transporters. Nature 437, 215–223 (2005).
pubmed: 16041361 doi: 10.1038/nature03978
Malinauskaite, L. et al. A mechanism for intracellular release of Na+ by neurotransmitter/sodium symporters. Nat. Struct. Mol. Biol. 21, 1006–1012 (2014).
pubmed: 25282149 pmcid: 4346222 doi: 10.1038/nsmb.2894
Gotfryd, K. et al. X-ray structure of LeuT in an inward-facing occluded conformation reveals mechanism of substrate release. Nat. Commun. 11, 1005 (2020).
pubmed: 32081981 pmcid: 7035281 doi: 10.1038/s41467-020-14735-w
Krishnamurthy, H. & Gouaux, E. X-ray structures of LeuT in substrate-free outward-open and apo inward-open states. Nature 481, 469–474 (2012).
pubmed: 22230955 pmcid: 3306218 doi: 10.1038/nature10737
Piscitelli, C. L. & Gouaux, E. Insights into transport mechanism from LeuT engineered to transport tryptophan: Insights into transport mechanism. EMBO J. 31, 228–235 (2012).
pubmed: 21952050 doi: 10.1038/emboj.2011.353
Focht, D. et al. A non‐helical region in transmembrane helix 6 of hydrophobic amino acid transporter MhsT mediates substrate recognition. EMBO J. 40, e105164 (2021).
pubmed: 33155685 doi: 10.15252/embj.2020105164
Weyand, S. et al. Structure and Molecular Mechanism of a Nucleobase–Cation–Symport-1 Family Transporter. Science 322, 709–713 (2008).
pubmed: 18927357 pmcid: 2885439 doi: 10.1126/science.1164440
Faham, S. et al. The Crystal Structure of a Sodium Galactose Transporter Reveals Mechanistic Insights into Na
pubmed: 18599740 pmcid: 3654663 doi: 10.1126/science.1160406
Yan, R. et al. Structural basis for the recognition of SARS-CoV-2 by full-length human ACE2. Science 367, 1444–1448 (2020).
pubmed: 32132184 pmcid: 7164635 doi: 10.1126/science.abb2762
Yan, R. et al. Structural basis for the different states of the spike protein of SARS-CoV-2 in complex with ACE2. Cell Res. 31, 717–719 (2021).
pubmed: 33737693 pmcid: 7972335 doi: 10.1038/s41422-021-00490-0
Chen, Y. et al. ACE2-targeting monoclonal antibody as potent and broad-spectrum coronavirus blocker. Sig Transduct. Target Ther. 6, 315 (2021).
doi: 10.1038/s41392-021-00740-y
Motiwala, Z. et al. Structural basis of GABA reuptake inhibition. Nature 606, 820–826 (2022).
pubmed: 35676483 pmcid: 9394549 doi: 10.1038/s41586-022-04814-x
Coleman, J. A., Green, E. M. & Gouaux, E. X-ray structures and mechanism of the human serotonin transporter. Nature 532, 334–339 (2016).
pubmed: 27049939 pmcid: 4898786 doi: 10.1038/nature17629
Yang, D. & Gouaux, E. Illumination of serotonin transporter mechanism and role of the allosteric site. Sci. Adv. 7, eabl3857 (2021).
pubmed: 34851672 pmcid: 8635421 doi: 10.1126/sciadv.abl3857
Munck, B. G. Transport of imino acids and non-α-amino acids across the brush-border membrane of the rabbit ileum. J. Membrain Biol. 83, 15–24 (1985).
doi: 10.1007/BF01868734
Olkhova, E., Raba, M., Bracher, S., Hilger, D. & Jung, H. Homology Model of the Na+/Proline Transporter PutP of Escherichia coli and Its Functional Implications. J. Mol. Biol. 406, 59–74 (2011).
pubmed: 21130773 doi: 10.1016/j.jmb.2010.11.045
Bröer, A. et al. Sodium translocation by the iminoglycinuria associated imino transporter (SLC6A20). Mol. Membr. Biol. 26, 333–346 (2009).
pubmed: 19657969 doi: 10.1080/09687680903150027
Shajahan, A. et al. Comprehensive characterization of N- and O- glycosylation of SARS-CoV-2 human receptor angiotensin converting enzyme 2. Glycobiology 31, 410–424 (2021).
pubmed: 33135055 doi: 10.1093/glycob/cwaa101
Singer, D. et al. Orphan Transporter SLC6A18 Is Renal Neutral Amino Acid Transporter B0AT3. J. Biol. Chem. 284, 19953–19960 (2009).
pubmed: 19478081 pmcid: 2740421 doi: 10.1074/jbc.M109.011171
Camargo, S. M. R. et al. Tissue-Specific Amino Acid Transporter Partners ACE2 and Collectrin Differentially Interact With Hartnup Mutations. Gastroenterology 136, 872–882.e3 (2009).
pubmed: 19185582 doi: 10.1053/j.gastro.2008.10.055
Penmatsa, A., Wang, K. H. & Gouaux, E. X-ray structure of dopamine transporter elucidates antidepressant mechanism. Nature 503, 85–90 (2013).
pubmed: 24037379 pmcid: 3904663 doi: 10.1038/nature12533
D’Imprima, E. et al. Protein denaturation at the air-water interface and how to prevent it. eLife 8, e42747 (2019).
pubmed: 30932812 pmcid: 6443348 doi: 10.7554/eLife.42747
Barad, B. A. et al. EMRinger: side chain–directed model and map validation for 3D cryo-electron microscopy. Nat. Methods 12, 943–946 (2015).
pubmed: 26280328 pmcid: 4589481 doi: 10.1038/nmeth.3541
Hattne, J. et al. Analysis of Global and Site-Specific Radiation Damage in Cryo-EM. Structure 26, 759–766.e4 (2018).
pubmed: 29706530 pmcid: 6333475 doi: 10.1016/j.str.2018.03.021
Yonekura, K. & Maki-Yonekura, S. Refinement of cryo-EM structures using scattering factors of charged atoms. J. Appl. Crystallogr. 49, 1517–1523 (2016).
doi: 10.1107/S1600576716011274
Pintilie, G. et al. Measurement of atom resolvability in cryo-EM maps with Q-scores. Nat. Methods 17, 328–334 (2020).
pubmed: 32042190 pmcid: 7446556 doi: 10.1038/s41592-020-0731-1
Kantcheva, A. K. et al. Chloride binding site of neurotransmitter sodium symporters. Proc. Natl Acad. Sci. USA 110, 8489–8494 (2013).
pubmed: 23641004 pmcid: 3666746 doi: 10.1073/pnas.1221279110
Sauer, D. B. et al. Structural basis of ion – substrate coupling in the Na+-dependent dicarboxylate transporter VcINDY. Nat. Commun. 13, 2644 (2022).
pubmed: 35551191 pmcid: 9098524 doi: 10.1038/s41467-022-30406-4
Wang, X. & Boudker, O. Large domain movements through the lipid bilayer mediate substrate release and inhibition of glutamate transporters. eLife 9, e58417 (2020).
pubmed: 33155546 pmcid: 7682989 doi: 10.7554/eLife.58417
Sauer, D. B. et al. Structure and inhibition mechanism of the human citrate transporter NaCT. Nature 591, 157–161 (2021).
pubmed: 33597751 pmcid: 7933130 doi: 10.1038/s41586-021-03230-x
Nayal, M. & Cera, E. D. Valence Screening of Water in Protein Crystals Reveals Potential Na+Binding Sites. J. Mol. Biol. 256, 228–234 (1996).
pubmed: 8594192 doi: 10.1006/jmbi.1996.0081
Zhao, Y. et al. Single-molecule dynamics of gating in a neurotransmitter transporter homologue. Nature 465, 188–193 (2010).
pubmed: 20463731 pmcid: 2940119 doi: 10.1038/nature09057
Ma, J. et al. Structural basis for substrate binding and specificity of a sodium–alanine symporter AgcS. Proc. Natl Acad. Sci. USA 116, 2086–2090 (2019).
pubmed: 30659158 pmcid: 6369739 doi: 10.1073/pnas.1806206116
Shafqat, S. et al. Human brain-specific L-proline transporter: molecular cloning, functional expression, and chromosomal localization of the gene in human and mouse genomes. Mol. Pharm. 48, 219–229 (1995).
Pei, J., Kim, B.-H. & Grishin, N. V. PROMALS3D: a tool for multiple protein sequence and structure alignments. Nucleic Acids Res. 36, 2295–2300 (2008).
pubmed: 18287115 pmcid: 2367709 doi: 10.1093/nar/gkn072
Price, M. N., Dehal, P. S. & Arkin, A. P. FastTree 2 – Approximately Maximum-Likelihood Trees for Large Alignments. PLoS ONE 5, e9490 (2010).
pubmed: 20224823 pmcid: 2835736 doi: 10.1371/journal.pone.0009490
Chi, G. et al. Phospho‐regulation, nucleotide binding and ion access control in potassium‐chloride cotransporters. EMBO J. 40, e107294 (2021).
pubmed: 34031912 pmcid: 8280820 doi: 10.15252/embj.2020107294
Mahajan, P. et al. Expression Screening of Human Integral Membrane Proteins Using BacMam. In Structural Genomics (eds. Chen, Y. W. & Yiu, C.-P. B.) 2199, 95–115 (Springer US, 2021).
Schorb, M., Haberbosch, I., Hagen, W. J. H., Schwab, Y. & Mastronarde, D. N. Software tools for automated transmission electron microscopy. Nat. Methods 16, 471–477 (2019).
pubmed: 31086343 pmcid: 7000238 doi: 10.1038/s41592-019-0396-9
Punjani, A., Rubinstein, J. L., Fleet, D. J. & Brubaker, M. A. cryoSPARC: algorithms for rapid unsupervised cryo-EM structure determination. Nat. Methods 14, 290–296 (2017).
pubmed: 28165473 doi: 10.1038/nmeth.4169
Zivanov, J., Nakane, T. & Scheres, S. H. W. Estimation of high-order aberrations and anisotropic magnification from cryo-EM data sets in RELION -3.1. IUCrJ 7, 253–267 (2020).
pubmed: 32148853 pmcid: 7055373 doi: 10.1107/S2052252520000081
Bepler, T. et al. Positive-unlabeled convolutional neural networks for particle picking in cryo-electron micrographs. Nat. Methods 16, 1153–1160 (2019).
pubmed: 31591578 pmcid: 6858545 doi: 10.1038/s41592-019-0575-8
Stein, N. CHAINSAW: a program for mutating pdb files used as templates in molecular replacement. J. Appl. Crystallogr. 41, 641–643 (2008).
doi: 10.1107/S0021889808006985
Emsley, P. & Cowtan, K. Coot: model-building tools for molecular graphics. Acta Crystallogr. D. Biol. Crystallogr. 60, 2126–2132 (2004).
pubmed: 15572765 doi: 10.1107/S0907444904019158
Afonine, P. V. et al. Real-space refinement in PHENIX for cryo-EM and crystallography. Acta Crystallogr. D. Struct. Biol. 74, 531–544 (2018).
pubmed: 29872004 pmcid: 6096492 doi: 10.1107/S2059798318006551
Smart, O. et al. Grade. https://www.globalphasing.com (2011).

Auteurs

Huanyu Z Li (HZ)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Ashley C W Pike (ACW)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Irina Lotsaris (I)

Molecular Biomedicine Theme, School of Medical Sciences, University of Sydney, Sydney, NSW, Australia.

Gamma Chi (G)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Jesper S Hansen (JS)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Sarah C Lee (SC)

School of Biosciences, University of Birmingham, Birmingham, UK.

Karin E J Rödström (KEJ)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Simon R Bushell (SR)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

David Speedman (D)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Adam Evans (A)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Dong Wang (D)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Didi He (D)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Leela Shrestha (L)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Chady Nasrallah (C)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Nicola A Burgess-Brown (NA)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK.

Robert J Vandenberg (RJ)

Molecular Biomedicine Theme, School of Medical Sciences, University of Sydney, Sydney, NSW, Australia. robert.vandenberg@sydney.edu.au.

Timothy R Dafforn (TR)

School of Biosciences, University of Birmingham, Birmingham, UK. t.r.dafforn@bham.ac.uk.

Elisabeth P Carpenter (EP)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK. lizcarpen1@gmail.com.

David B Sauer (DB)

Centre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford, UK. david.sauer@cmd.ox.ac.uk.

Articles similaires

[Redispensing of expensive oral anticancer medicines: a practical application].

Lisanne N van Merendonk, Kübra Akgöl, Bastiaan Nuijen
1.00
Humans Antineoplastic Agents Administration, Oral Drug Costs Counterfeit Drugs

Smoking Cessation and Incident Cardiovascular Disease.

Jun Hwan Cho, Seung Yong Shin, Hoseob Kim et al.
1.00
Humans Male Smoking Cessation Cardiovascular Diseases Female
Humans United States Aged Cross-Sectional Studies Medicare Part C
1.00
Humans Yoga Low Back Pain Female Male

Classifications MeSH