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Two independent histidines, one in human prolactin and one in its receptor, are critical for pH-dependent receptor recognition and activation.

Kulkarni MV, Tettamanzi MC, Murphy JW, Keeler C, Myszka DG, Chayen NE, Lolis EJ, Hodsdon ME
J Biol Chem 285 38524-33 (2010)
Related entries: 3mzg, 3n06, 3n0p, 3ncb, 3ncc, 3ncf

Cited: 21 times
EuropePMC logo PMID: 20889499

Abstract

Human prolactin (hPRL), a member of the family of hematopoietic cytokines, functions as both an endocrine hormone and autocrine/paracrine growth factor. We have previously demonstrated that recognition of the hPRL·receptor depends strongly on solution acidity over the physiologic range from pH 6 to pH 8. The hPRL·receptor binding interface contains four histidines whose protonation is hypothesized to regulate pH-dependent receptor recognition. Here, we systematically dissect its molecular origin by characterizing the consequences of His to Ala mutations on pH-dependent receptor binding kinetics, site-specific histidine protonation, and high resolution structures of the intermolecular interface. Thermodynamic modeling of the pH dependence to receptor binding affinity reveals large changes in site-specific protonation constants for a majority of interface histidines upon complexation. Removal of individual His imidazoles reduces these perturbations in protonation constants, which is most likely explained by the introduction of solvent-filled, buried cavities in the crystallographic structures without inducing significant conformational rearrangements.

Articles - 3nce mentioned but not cited (2)

  1. Two independent histidines, one in human prolactin and one in its receptor, are critical for pH-dependent receptor recognition and activation. Kulkarni MV, Tettamanzi MC, Murphy JW, Keeler C, Myszka DG, Chayen NE, Lolis EJ, Hodsdon ME. J Biol Chem 285 38524-38533 (2010)
  2. The dipeptidyl peptidase IV inhibitors vildagliptin and K-579 inhibit a phospholipase C: a case of promiscuous scaffolds in proteins. Chakraborty S, Rendón-Ramírez A, Ásgeirsson B, Dutta M, Ghosh AS, Oda M, Venkatramani R, Rao BJ, Dandekar AM, Goñi FM. F1000Res 2 286 (2013)


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  1. Molecular mechanisms of disease-causing missense mutations. Stefl S, Nishi H, Petukh M, Panchenko AR, Alexov E. J Mol Biol 425 3919-3936 (2013)
  2. Implications of receptor-mediated endocytosis and intracellular trafficking dynamics in the development of antibody drug conjugates. Ritchie M, Tchistiakova L, Scott N. MAbs 5 13-21 (2013)
  3. Molecular mechanisms of prolactin and its receptor. Brooks CL. Endocr Rev 33 504-525 (2012)
  4. Functional peptides for siRNA delivery. Tai W, Gao X. Adv Drug Deliv Rev 110-111 157-168 (2017)

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  1. SKEMPI 2.0: an updated benchmark of changes in protein-protein binding energy, kinetics and thermodynamics upon mutation. Jankauskaite J, Jiménez-García B, Dapkunas J, Fernández-Recio J, Moal IH. Bioinformatics 35 462-469 (2019)
  2. A combinatorial histidine scanning library approach to engineer highly pH-dependent protein switches. Murtaugh ML, Fanning SW, Sharma TM, Terry AM, Horn JR. Protein Sci 20 1619-1631 (2011)
  3. 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)
  4. A generic approach to engineer antibody pH-switches using combinatorial histidine scanning libraries and yeast display. Schröter C, Günther R, Rhiel L, Becker S, Toleikis L, Doerner A, Becker J, Schönemann A, Nasu D, Neuteboom B, Kolmar H, Hock B. MAbs 7 138-151 (2015)
  5. Phylogenetic and functional analysis of histidine residues essential for pH-dependent multimerization of von Willebrand factor. Dang LT, Purvis AR, Huang RH, Westfield LA, Sadler JE. J Biol Chem 286 25763-25769 (2011)
  6. Structural mechanism of ER retrieval of MHC class I by cowpox. McCoy WH, Wang X, Yokoyama WM, Hansen TH, Fremont DH. PLoS Biol 10 e1001432 (2012)
  7. 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)
  8. Prolactin Signaling Stimulates Invasion via Na(+)/H(+) Exchanger NHE1 in T47D Human Breast Cancer Cells. Pedraz-Cuesta E, Fredsted J, Jensen HH, Bornebusch A, Nejsum LN, Kragelund BB, Pedersen SF. Mol Endocrinol 30 693-708 (2016)
  9. In silico investigation of pH-dependence of prolactin and human growth hormone binding to human prolactin receptor. Wang L, Witham S, Zhang Z, Li L, Hodsdon ME, Alexov E. Commun Comput Phys 13 207-222 (2013)
  10. Prolactin-Stat5 signaling in breast cancer is potently disrupted by acidosis within the tumor microenvironment. Yang N, Liu C, Peck AR, Girondo MA, Yanac AF, Tran TH, Utama FE, Tanaka T, Freydin B, Chervoneva I, Hyslop T, Kovatich AJ, Hooke JA, Shriver CD, Rui H. Breast Cancer Res 15 R73 (2013)
  11. Isolation of a pH-Sensitive IgNAR Variable Domain from a Yeast-Displayed, Histidine-Doped Master Library. Könning D, Zielonka S, Sellmann C, Schröter C, Grzeschik J, Becker S, Kolmar H. Mar Biotechnol (NY) 18 161-167 (2016)
  12. Improving the accuracy of high-throughput protein-protein affinity prediction may require better training data. Dias R, Kolaczkowski B. BMC Bioinformatics 18 102 (2017)
  13. Engineering an Anti-Transferrin Receptor ScFv for pH-Sensitive Binding Leads to Increased Intracellular Accumulation. Tillotson BJ, Goulatis LI, Parenti I, Duxbury E, Shusta EV. PLoS One 10 e0145820 (2015)
  14. 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)
  15. Identification of prolactin receptor variants with diverse effects on receptor signalling. Gorvin CM, Newey PJ, Thakker RV. J Mol Endocrinol 70 e220164 (2023)


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