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Identification of the first small-molecule ligand of the neuronal receptor sortilin and structure determination of the receptor-ligand complex.

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Andersen JL, Schrøder TJ, Christensen S, Strandbygård D, Pallesen LT, García-Alai MM, Lindberg S, Langgård M, Eskildsen JC, David L, Tagmose L, Simonsen KB, Maltas PJ, Rønn LC, de Jong IE, Malik IJ, Egebjerg J, Karlsson JJ, Uppalanchi S, Sakumudi DR, Eradi P, Watson SP, Thirup S
OpenAccess logo Acta Crystallogr D Biol Crystallogr 70 451-60 (2014)
Cited: 17 times
EuropePMC logo PMID: 24531479

Abstract

Sortilin is a type I membrane glycoprotein belonging to the vacuolar protein sorting 10 protein (Vps10p) family of sorting receptors and is most abundantly expressed in the central nervous system. Sortilin has emerged as a key player in the regulation of neuronal viability and has been implicated as a possible therapeutic target in a range of disorders. Here, the identification of AF40431, the first reported small-molecule ligand of sortilin, is reported. Crystals of the sortilin-AF40431 complex were obtained by co-crystallization and the structure of the complex was solved to 2.7 Å resolution. AF40431 is bound in the neurotensin-binding site of sortilin, with the leucine moiety of AF40431 mimicking the binding mode of the C-terminal leucine of neurotensin and the 4-methylumbelliferone moiety of AF40431 forming π-stacking with a phenylalanine.

Articles - 4msl mentioned but not cited (3)

  1. Identification of the first small-molecule ligand of the neuronal receptor sortilin and structure determination of the receptor-ligand complex. Andersen JL, Schrøder TJ, Christensen S, Strandbygård D, Pallesen LT, García-Alai MM, Lindberg S, Langgård M, Eskildsen JC, David L, Tagmose L, Simonsen KB, Maltas PJ, Rønn LC, de Jong IE, Malik IJ, Egebjerg J, Karlsson JJ, Uppalanchi S, Sakumudi DR, Eradi P, Watson SP, Thirup S. Acta Crystallogr. D Biol. Crystallogr. 70 451-460 (2014)
  2. Pocket detection and interaction-weighted ligand-similarity search yields novel high-affinity binders for Myocilin-OLF, a protein implicated in glaucoma. Srinivasan B, Tonddast-Navaei S, Skolnick J. Bioorg Med Chem Lett 27 4133-4139 (2017)
  3. Structural insights into SorCS2-Nerve Growth Factor complex formation. Leloup N, Chataigner LMP, Janssen BJC. Nat Commun 9 2979 (2018)


Reviews citing this publication (2)

  1. Sortilin and Its Multiple Roles in Cardiovascular and Metabolic Diseases. Goettsch C, Kjolby M, Aikawa E. Arterioscler. Thromb. Vasc. Biol. 38 19-25 (2018)
  2. Sorting through the extensive and confusing roles of sortilin in metabolic disease. Mitok KA, Keller MP, Attie AD. J Lipid Res 63 100243 (2022)

Articles citing this publication (12)

  1. Sortilin is associated with breast cancer aggressiveness and contributes to tumor cell adhesion and invasion. Roselli S, Pundavela J, Demont Y, Faulkner S, Keene S, Attia J, Jiang CC, Zhang XD, Walker MM, Hondermarck H. Oncotarget 6 10473-10486 (2015)
  2. Anti-sortilin1 Antibody Up-Regulates Progranulin via Sortilin1 Down-Regulation. Miyakawa S, Sakuma H, Warude D, Asanuma S, Arimura N, Yoshihara T, Tavares D, Hata A, Ida K, Hori Y, Okuzono Y, Yamamoto S, Iida K, Shimizu H, Kondo S, Sato S. Front Neurosci 14 586107 (2020)
  3. Diacerein-mediated inhibition of IL-6/IL-6R signaling induces apoptotic effects on breast cancer. Bharti R, Dey G, Ojha PK, Rajput S, Jaganathan SK, Sen R, Mandal M. Oncogene 35 3965-3975 (2016)
  4. Low pH-induced conformational change and dimerization of sortilin triggers endocytosed ligand release. Leloup N, Lössl P, Meijer DH, Brennich M, Heck AJR, Thies-Weesie DME, Janssen BJC. Nat Commun 8 1708 (2017)
  5. Crystal structure of the ligand-free form of the Vps10 ectodomain of dimerized Sortilin at acidic pH. Yabe-Wada T, Matsuba S, Unno M, Onai N. FEBS Lett. 592 2647-2657 (2018)
  6. Development of a Cell-Based Assay to Assess Binding of the proNGF Prodomain to Sortilin. Malik I, Christensen S, Stavenhagen JB, Dietz GPH. Cell. Mol. Neurobiol. 38 827-840 (2018)
  7. Multi-ancestry genome-wide gene-sleep interactions identify novel loci for blood pressure. Wang H, Noordam R, Cade BE, Schwander K, Winkler TW, Lee J, Sung YJ, Bentley AR, Manning AK, Aschard H, Kilpeläinen TO, Ilkov M, Brown MR, Horimoto AR, Richard M, Bartz TM, Vojinovic D, Lim E, Nierenberg JL, Liu Y, Chitrala K, Rankinen T, Musani SK, Franceschini N, Rauramaa R, Alver M, Zee PC, Harris SE, van der Most PJ, Nolte IM, Munroe PB, Palmer ND, Kühnel B, Weiss S, Wen W, Hall KA, Lyytikäinen LP, O'Connell J, Eiriksdottir G, Launer LJ, de Vries PS, Arking DE, Chen H, Boerwinkle E, Krieger JE, Schreiner PJ, Sidney S, Shikany JM, Rice K, Chen YI, Gharib SA, Bis JC, Luik AI, Ikram MA, Uitterlinden AG, Amin N, Xu H, Levy D, He J, Lohman KK, Zonderman AB, Rice TK, Sims M, Wilson G, Sofer T, Rich SS, Palmas W, Yao J, Guo X, Rotter JI, Biermasz NR, Mook-Kanamori DO, Martin LW, Barac A, Wallace RB, Gottlieb DJ, Komulainen P, Heikkinen S, Mägi R, Milani L, Metspalu A, Starr JM, Milaneschi Y, Waken RJ, Gao C, Waldenberger M, Peters A, Strauch K, Meitinger T, Roenneberg T, Völker U, Dörr M, Shu XO, Mukherjee S, Hillman DR, Kähönen M, Wagenknecht LE, Gieger C, Grabe HJ, Zheng W, Palmer LJ, Lehtimäki T, Gudnason V, Morrison AC, Pereira AC, Fornage M, Psaty BM, van Duijn CM, Liu CT, Kelly TN, Evans MK, Bouchard C, Fox ER, Kooperberg C, Zhu X, Lakka TA, Esko T, North KE, Deary IJ, Snieder H, Penninx BWJH, Gauderman WJ, Rao DC, Redline S, van Heemst D. Mol Psychiatry 26 6293-6304 (2021)
  8. Sortilin and hypertension. Avvisato R, Jankauskas SS, Varzideh F, Kansakar U, Mone P, Santulli G. Curr Opin Nephrol Hypertens 32 134-140 (2023)
  9. Carbonic Anhydrase Robustness for Use in Nanoscale CO2 Capture Technologies. Sharma A, Chiang RA, Manginell M, Nardi I, Coker EN, Vanegas JM, Rempe SB, Bachand GD. ACS Omega 8 37830-37841 (2023)
  10. PAK Kinases Target Sortilin and Modulate Its Sorting. Pallesen LT, Gustafsen C, Cramer JF, Petersen SV, Thirup SS, Madsen P, Petersen CM. Mol Cell Biol 40 (2020)
  11. Regional and Cellular Mapping of Sortilin Immunoreactivity in Adult Human Brain. Xu SY, Zhang QL, Zhang Q, Wan L, Jiang J, Tu T, Manavis J, Pan A, Cai Y, Yan XX. Front Neuroanat 13 31 (2019)
  12. Sortilin gates neurotensin and BDNF signaling to control peripheral neuropathic pain. Richner M, Pallesen LT, Ulrichsen M, Poulsen ET, Holm TH, Login H, Castonguay A, Lorenzo LE, Gonçalves NP, Andersen OM, Lykke-Hartmann K, Enghild JJ, Rønn LCB, Malik IJ, De Koninck Y, Bjerrum OJ, Vægter CB, Nykjær A. Sci Adv 5 eaav9946 (2019)


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