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Structural characterization of the stem-stem dimerization interface between prolactin receptor chains complexed with the natural hormone.

van Agthoven J, Zhang C, Tallet E, Raynal B, Hoos S, Baron B, England P, Goffin V, Broutin I
J Mol Biol 404 112-26 (2010)
Cited: 24 times
EuropePMC logo PMID: 20875426

Abstract

The most promising approach to targeting the tumor-growth-promoting actions of prolactin (PRL) mediated by its autocrine/paracrine pathway has been the development of specific PRL receptor (PRLR) antagonists. However, the optimization of such antagonists requires a thorough understanding of the activation mechanism of PRLR. We have thus conducted a systematic X-ray crystallographic study in order to visualize the successive steps of PRLR activation by PRL. We report here the structure at 3.35 Å resolution of the 1:2 complex between natural PRL and two PRLR chains (PRLR1 and PRLR2), corresponding to the final activated state of PRLR. Further than our previously published structure involving an affinity-matured PRL variant, this structure allowed to visualize for the first time the loop L5 spanning PRLR2 residues Thr133-Phe140, revealing its central implication for the three intermolecular interfaces of the complex. We equally succeeded in obtaining a comprehensive picture of the PRLR-PRLR dimerization interface, also called stem-stem interface. Site-directed mutagenesis was conducted to probe the energetic importance of stem-stem contacts highlighted by the structure. Surprisingly, in spite of significant structural differences between the PRL/PRLR(2) complex and the 1:2 growth hormone/growth hormone receptor complex, our mutational data suggest that hot-spot residues that stabilize the receptor dimerization interface are equivalent in the two complexes. This study provides a new overall picture of the structural features of PRLR involved in stabilizing its complex with PRL.

Reviews - 3npz mentioned but not cited (1)

  1. (S)Pinning down protein interactions by NMR. Teilum K, Kunze MB, Erlendsson S, Kragelund BB. Protein Sci 26 436-451 (2017)

Articles - 3npz mentioned but not cited (8)

  1. A common model for cytokine receptor activation: combined scissor-like rotation and self-rotation of receptor dimer induced by class I cytokine. Pang X, Zhou HX. PLoS Comput Biol 8 e1002427 (2012)
  2. Engineering synthetic antibody binders for allosteric inhibition of prolactin receptor signaling. Rizk SS, Kouadio JL, Szymborska A, Duguid EM, Mukherjee S, Zheng J, Clevenger CV, Kossiakoff AA. Cell Commun Signal 13 1 (2015)
  3. Rationalizing 5000-fold differences in receptor-binding rate constants of four cytokines. Pang X, Qin S, Zhou HX. Biophys J 101 1175-1183 (2011)
  4. Investigation of prolactin receptor activation and blockade using time-resolved fluorescence resonance energy transfer. Tallet E, Fernandez I, Zhang C, Salsac M, Gregor N, Ayoub MA, Pin JP, Trinquet E, Goffin V. Front Endocrinol (Lausanne) 2 29 (2011)
  5. Impact of subdomain D1 of the short form S1b of the human prolactin receptor on its inhibitory action on the function of the long form of the receptor induced by prolactin. Kang JH, Hassan SA, Zhao P, Tsai-Morris CH, Dufau ML. Biochim Biophys Acta 1840 2272-2280 (2014)
  6. A Residue Quartet in the Extracellular Domain of the Prolactin Receptor Selectively Controls Mitogen-activated Protein Kinase Signaling. Zhang C, Nygaard M, Haxholm GW, Boutillon F, Bernadet M, Hoos S, England P, Broutin I, Kragelund BB, Goffin V. J Biol Chem 290 11890-11904 (2015)
  7. Identification of prolactin receptor variants with diverse effects on receptor signalling. Gorvin CM, Newey PJ, Thakker RV. J Mol Endocrinol 70 e220164 (2023)
  8. research-article Structural modeling of cytokine-receptor-JAK2 signaling complexes using AlphaFold Multimer. Pogozheva ID, Cherepanov S, Park SJ, Raghavan M, Im W, Lomize AL. bioRxiv 2023.06.14.544971 (2023)


Reviews citing this publication (6)

  1. Molecular mechanisms of prolactin and its receptor. Brooks CL. Endocr Rev 33 504-525 (2012)
  2. JAK2 activation by growth hormone and other cytokines. Waters MJ, Brooks AJ. Biochem J 466 1-11 (2015)
  3. Understanding cytokine and growth factor receptor activation mechanisms. Atanasova M, Whitty A. Crit Rev Biochem Mol Biol 47 502-530 (2012)
  4. Prolactin receptor targeting in breast and prostate cancers: New insights into an old challenge. Goffin V. Pharmacol Ther 179 111-126 (2017)
  5. Triennial Lactation Symposium: Prolactin: The multifaceted potentiator of mammary growth and function. Trott JF, Schennink A, Petrie WK, Manjarin R, VanKlompenberg MK, Hovey RC. J Anim Sci 90 1674-1686 (2012)
  6. Reproductive actions of prolactin mediated through short and long receptor isoforms. Sangeeta Devi Y, Halperin J. Mol Cell Endocrinol 382 400-410 (2014)

Articles citing this publication (9)

  1. Mutant prolactin receptor and familial hyperprolactinemia. Newey PJ, Gorvin CM, Cleland SJ, Willberg CB, Bridge M, Azharuddin M, Drummond RS, van der Merwe PA, Klenerman P, Bountra C, Thakker RV. N Engl J Med 369 2012-2020 (2013)
  2. A combined computational and structural model of the full-length human prolactin receptor. Bugge K, Papaleo E, Haxholm GW, Hopper JT, Robinson CV, Olsen JG, Lindorff-Larsen K, Kragelund BB. Nat Commun 7 11578 (2016)
  3. Association of prolactin receptor (PRLR) variants with prolactinomas. Gorvin CM, Newey PJ, Rogers A, Stokes V, Neville MJ, Lines KE, Ntali G, Lees P, Morrison PJ, Singhellakis PN, Malandrinou FC, Karavitaki N, Grossman AB, Karpe F, Thakker RV. Hum Mol Genet 28 1023-1037 (2019)
  4. Subdomain 2, Not the Transmembrane Domain, Determines the Dimerization Partner of Growth Hormone Receptor and Prolactin Receptor. Liu Y, Jiang J, Lepik B, Zhang Y, Zinn KR, Frank SJ. Endocrinology 158 3235-3248 (2017)
  5. Growth hormone (GH) receptor (GHR)-specific inhibition of GH-Induced signaling by soluble IGF-1 receptor (sol IGF-1R). Zhang Y, Gc S, Patel SB, Liu Y, Paterson AJ, Kappes JC, Jiang J, Frank SJ. Mol Cell Endocrinol 492 110445 (2019)
  6. Cloning, expression of, and evidence of positive selection for, the prolactin receptor gene in Chinese giant salamander (Andrias davidianus). Hu Q, Meng Y, Tian H, Chen S, Xiao H. J Exp Zool B Mol Dev Evol 324 707-719 (2015)
  7. Short prolactin isoforms are expressed in photoreceptors of canine retinas undergoing retinal degeneration. Sudharsan R, Murgiano L, Tang HY, Olsen TW, Chavali VRM, Aguirre GD, Beltran WA. Sci Rep 11 460 (2021)
  8. In silico prediction of prolactin molecules as a tool for equine genomics reproduction. Neis A, Kremer FS, Pinto LS, Leon PMM. Mol Divers 23 1019-1028 (2019)
  9. Structure of the thrombopoietin-MPL receptor complex is a blueprint for biasing hematopoiesis. Tsutsumi N, Masoumi Z, James SC, Tucker JA, Winkelmann H, Grey W, Picton LK, Moss L, Wilson SC, Caveney NA, Jude KM, Gati C, Piehler J, Hitchcock IS, Garcia KC. Cell 186 4189-4203.e22 (2023)


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