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Literature for peptidase S54.016: GlpG peptidase (Escherichia-type)

Summary Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates

(Topics flags: A Assay, S Structure, P Specificity, I Inhibitor, E Expression, V Review. To select only the references relevant to a single topic, click the link above. See explanation.)

    2026
  1. Bohg,C., Dubanych,Y., Kosteletos,S., Xiao,T., Neuenschwander,M., Utesch,T., Lisurek,M., Oster,C., Oder,A., Seyffarth,C., Bach,K., Leone,D.G., Filandr,F., Wegert,M., Lange,S., Sawczyc,H., von Kries,J.P., Hackenberger,C.P.R., Specker,E., Sun,H., Strisovsky,K. and Lange,A.<br>Targeting the Membrane-Embedded Rhomboid Protease GlpG: A Multimodal Strategy for Inhibitor Discovery and Mechanistic Insight<br>Angew Chem Int Ed Engl (2026) , e14067-e14067. PubMed  Europe PubMed DOI
    2. 2025
  2. Abramsson,M.L., Corey,R.A., Skerle,J.L., Persson,L.J., Anden,O., Oluwole,A.O., Howard,R.J., Lindahl,E., Robinson,C.V., Strisovsky,K., Marklund,E.G., Drew,D., Stansfeld,P.J. and Landreh,M.<br>Engineering cardiolipin binding to an artificial membrane protein reveals determinants for lipid-mediated stabilization<br>elife (2025) 14 PubMed  Europe PubMed DOI  PMC  EPMC
  3. Fremlen,H. and Burmann,B.M.<br>Maintaining the Integral Membrane Proteome: Revisiting the Functional Repertoire of Integral Membrane Proteases<br>Chembiochem (2025) , e202500048-e202500048. PubMed  Europe PubMed DOI  V
  4. Lu,J., Arutyunova,E., Hartley,B., Wong,J., Chung,H., Buchan,L., Armstrong,H., Phanse,S., Young,H.S., Wine,E., Babu,M., Chun,J., Elhenawy,W., Julien,O. and Lemieux,M.J.<br>Rhomboid protease GlpG regulates type 1 pili quality control and virulence in pathogenic E. coli<br>Nat Commun (2025) PubMed  Europe PubMed DOI
    5. 2024
  5. Bach,K., Dohnalek,J., Skerlova,J., Kuzmik,J., Polachova,E., Stanchev,S., Majer,P., Fanfrlik,J., Pecina,A., Rezac,J., Lepsik,M., Borshchevskiy,V., Polovinkin,V. and Strisovsky,K.<br>Extensive targeting of chemical space at the prime side of ketoamide inhibitors of rhomboid proteases by branched substituents empowers their selectivity and potency<br>Eur J Med Chem (2024) 275, 116606-116606. PubMed  Europe PubMed DOI
  6. Engberg,O., Mathath,A.V., Dobel,V., Frie,C., Lemberg,M.K., Chakraborty,D. and Huster,D.<br>Evaluating the Impact of the Membrane Thickness on the Function of the Intramembrane Protease GlpG<br>Biophys J (2024) PubMed  Europe PubMed DOI
  7. Nimerovsky,E., Kosteletos,S., Lange,S., Becker,S., Lange,A. and Andreas,L.B.<br>Homonuclear Simplified Preservation of Equivalent Pathways Spectroscopy<br>J Phys Chem Lett (2024) 15, 6272-6278. PubMed  Europe PubMed DOI
  8. Roberts,C.S., Shannon,A.B., Korotkov,K.V. and Sandkvist,M.<br>Differential processing of VesB by two rhomboid proteases in Vibrio cholerae<br>MBio (2024) , e0127024-e0127024. PubMed  Europe PubMed DOI
  9. Sawczyc,H., Tatsuta,T., Oster,C., Kosteletos,S., Lange,S., Bohg,C., Langer,T. and Lange,A.<br>Lipid-polymer nanoparticles to probe the native-like environment of intramembrane rhomboid protease GlpG and its activity<br>Nat Commun (2024) 15, 7533-7533. PubMed  Europe PubMed DOI  PMC  EPMC
    10. 2023
  10. Bohg,C., Oster,C., Turkaydin,B., Lisurek,M., Sanchez-Carranza,P., Lange,S., Utesch,T., Sun,H. and Lange,A.<br>The opening dynamics of the lateral gate regulates the activity of rhomboid proteases<br>Sci Adv (2023) 9, eadh3858-eadh3858. PubMed  Europe PubMed DOI  PMC  EPMC
    11. 2022
  11. Engberg,O., Ulbricht,D., Dobel,V., Siebert,V., Frie,C., Penk,A., Lemberg,M.K. and Huster,D.<br>Rhomboid-catalyzed intramembrane proteolysis requires hydrophobic matching with the surrounding lipid bilayer<br>Sci Adv (2022) 8, eabq8303-eabq8303. PubMed  Europe PubMed DOI  PMC  EPMC
    12. 2021
  12. Bohg,C., Oster,C., Utesch,T., Bischoff,S., Lange,S., Shi,C., Sun,H. and Lange,A.<br>A combination of solid-state NMR and MD simulations reveals the binding mode of a rhomboid protease inhibitor<br>Chem Sci (2021) 12, 12754-12762. PubMed  Europe PubMed DOI  PMC  EPMC
  13. Mitra,D. and Das Mohapatra,P.K.<br>Discovery of Novel Cyclic Salt Bridge in Thermophilic Bacterial Protease and Study of its Sequence and Structure<br>Appl Biochem Biotechnol (2021) PubMed  Europe PubMed DOI
  14. Otzen,D.E., Pedersen,J.N., Somavarapu,A.K., Clement,A., Ji,M., Petersen,E.H., Pedersen,J.S., Urban,S. and Schafer,N.P.<br>Cys-labeling kinetics of membrane protein GlpG: a role for specific SDS binding and micelle changes?<br>Biophys J (2021) PubMed  Europe PubMed DOI
    15. 2020
  15. Bondar,A.N.<br>Phosphatidylglyerol Lipid Binding at the Active Site of an Intramembrane Protease<br>J Membr Biol (2020) 253, 563-576. PubMed  Europe PubMed DOI  PMC  EPMC  V
  16. Guo,R., Cang,Z., Yao,J., Kim,M., Deans,E., Wei,G., Kang,S.G. and Hong,H.<br>Structural cavities are critical to balancing stability and activity of a membrane-integral enzyme<br>Proc Natl Acad Sci U S A (2020) 117, 22146-22156. PubMed  Europe PubMed DOI  PMC  EPMC
  17. Knopf,J.D. and Lemberg,M.K.<br>Derlins with scissors: primordial ERAD in bacteria<br>EMBO J (2020) , e105012-e105012. PubMed  Europe PubMed DOI
    18. 2019
  18. Almeida-Hernandez,Y. and Tidow,H.<br>Soluble regions of GlpG influence protein-lipid interactions and lipid distribution<br>J Phys Chem B (2019) 123, 7852-7858. PubMed  Europe PubMed DOI
  19. Bondar,A.N.<br>Mechanisms by which lipids influence conformational dynamics of the GlpG intramembrane protease<br>J Phys Chem B (2019) 123, 4159-4172. PubMed  Europe PubMed DOI
  20. Cho,S., Baker,R.P., Ji,M. and Urban,S.<br>Ten catalytic snapshots of rhomboid intramembrane proteolysis from gate opening to peptide release<br>Nat Struct Mol Biol (2019) 26, 910-918. PubMed  Europe PubMed DOI  S
  21. Gaffney,K.A. and Hong,H.<br>The rhomboid protease GlpG has weak interaction energies in its active site hydrogen bond network<br>J Gen Physiol (2019) 151, 282-291. PubMed  Europe PubMed DOI
  22. Shi,C., Oster,C., Bohg,C., Li,L., Lange,S., Chevelkov,V. and Lange,A.<br>Structure and dynamics of the rhomboid protease GlpG in liposomes studied by solid-state NMR<br>J Am Chem Soc (2019) 141, 17314-17321. PubMed  Europe PubMed DOI  S
    23. 2018
  23. Brown,M.C., Abdine,A., Chavez,J., Schaffner,A., Torres-Arancivia,C., Lada,B., JiJi,R.D., Osman,R., Cooley,J.W. and Ubarretxena-Belandia,I.<br>Unwinding of the substrate transmembrane helix in intramembrane proteolysis<br>Biophys J (2018) 114, 1579-1589. PubMed  Europe PubMed DOI
  24. Yang,J., Barniol-Xicota,M., Nguyen,M.T.N., Ticha,A., Strisovsky,K. and Verhelst,S.H.L.<br>Benzoxazin-4-ones as novel, easily accessible inhibitors for rhomboid proteases<br>Bioorg Med Chem Lett (2018) 28, 1423-1427. PubMed  Europe PubMed DOI  I
  25. Yang,Y., Guo,R., Gaffney,K., Kim,M., Muhammednazaar,S., Tian,W., Wang,B., Liang,J. and Hong,H.<br>Folding-degradation relationship of a membrane protein mediated by the universally conserved ATP-dependent protease FtsH<br>J Am Chem Soc (2018) 140, 4656-4665. PubMed  Europe PubMed DOI
    26. 2017
  26. Arutyunova,E., Panigrahi,R., Strisovsky,K. and Lemieux,M.J.<br>Production of recombinant rhomboid proteases<br>Methods Enzymol (2017) 584, 255-278. PubMed  Europe PubMed DOI  E
  27. Cordier,B. and Lemberg,M.K.<br>Probing the activity of eukaryotic rhomboid proteases in vitro<br>Methods Enzymol (2017) 584, 99-126. PubMed  Europe PubMed DOI  A  E
  28. Goel,P., Jumpertz,T., Mikles,D.C., Ticha,A., Nguyen,M.T.N., Verhelst,S., Hubalek,M., Johnson,D.C., Bachovchin,D.A., Ogorek,I., Pietrzik,C.U., Strisovsky,K., Schmidt,B. and Weggen,S.<br>Discovery and biological evaluation of potent and selective N-methylene saccharin-derived inhibitors for rhomboid intramembrane proteases<br>Biochemistry (2017) 56, 6713-6725. PubMed  Europe PubMed DOI  I
  29. Russell,C.W., Richards,A.C., Chang,A.S. and Mulvey,M.A.<br>The rhomboid protease GlpG promotes the persistence of extraintestinal pathogenic Escherichia coli within the gut<br>Infect Immun (2017) 85, e00866-16-e00866-16. PubMed  Europe PubMed DOI
  30. Shokhen,M. and Albeck,A.<br>How does the exosite of rhomboid protease affect substrate processing and inhibition?<br>Protein Sci (2017) 26, 2355-2366. PubMed  Europe PubMed DOI
  31. Ticha,A., Stanchev,S., Vinothkumar,K.R., Mikles,D.C., Pachl,P., Began,J., Skerle,J., Svehlova,K., Nguyen,M.T.N., Verhelst,S.H.L., Johnson,D.C., Bachovchin,D.A., Lepsik,M., Majer,P. and Strisovsky,K.<br>General and modular strategy for designing potent, selective, and pharmacologically compliant inhibitors of rhomboid proteases<br>Cell Chem Biol (2017) 24, 1523-1536. PubMed  Europe PubMed DOI  S  I
    32. 2016
  32. Cho,S., Dickey,S.W. and Urban,S.<br>Crystal structures and inhibition kinetics reveal a two-stage catalytic mechanism with drug design implications for rhomboid proteolysis<br>Mol Cell (2016) 61, 329-340. PubMed  Europe PubMed DOI  I
  33. Guo,R., Gaffney,K., Yang,Z., Kim,M., Sungsuwan,S., Huang,X., Hubbell,W.L. and Hong,H.<br>Steric trapping reveals a cooperativity network in the intramembrane protease GlpG<br>Nat Chem Biol (2016) 12, 353-360. PubMed  Europe PubMed DOI
  34. Schafer,N.P., Truong,H.H., Otzen,D.E., Lindorff-Larsen,K. and Wolynes,P.G.<br>Topological constraints and modular structure in the folding and functional motions of GlpG, an intramembrane protease<br>Proc Natl Acad Sci U S A (2016) 113, 2098-2103. PubMed  Europe PubMed DOI
  35. Uritsky,N., Shokhen,M. and Albeck,A.<br>Stepwise versus concerted mechanisms in general-base catalysis by serine proteases<br>Angew Chem Int Ed Engl (2016) 55, 1680-1684. PubMed  Europe PubMed DOI
  36. Wolf,E.V. and Verhelst,S.H.<br>Inhibitors of rhomboid proteases<br>Biochimie (2016) 122, 38-47. PubMed  Europe PubMed DOI  I
    37. 2015
  37. Foo,A.C., Harvey,B.G., Metz,J.J. and Goto,N.K.<br>Influence of hydrophobic mismatch on the catalytic activity of Escherichia coli GlpG rhomboid protease<br>Protein Sci (2015) 24, 464-473. PubMed  Europe PubMed DOI
  38. Min,D., Jefferson,R.E., Bowie,J.U. and Yoon,T.Y.<br>Mapping the energy landscape for second-stage folding of a single membrane protein<br>Nat Chem Biol (2015) 11, 981-987. PubMed  Europe PubMed DOI
  39. Paslawski,W., Lillelund,O.K., Kristensen,J.V., Schafer,N.P., Baker,R.P., Urban,S. and Otzen,D.E.<br>Cooperative folding of a polytopic alpha-helical membrane protein involves a compact N-terminal nucleus and nonnative loops<br>Proc Natl Acad Sci U S A (2015) 112, 7978-7983. PubMed  Europe PubMed DOI
    40. 2014
  40. Ghasriani,H., Kwok,J.K., Sherratt,A.R., Foo,A.C., Qureshi,T. and Goto,N.K.<br>Micelle-catalyzed domain swapping in the GlpG rhomboid protease cytoplasmic domain<br>Biochemistry (2014) 53, 5907-5915. PubMed  Europe PubMed DOI
  41. Zoll,S., Stanchev,S., Began,J., Skerle,J., Lepsik,M., Peclinovska,L., Majer,P. and Strisovsky,K.<br>Substrate binding and specificity of rhomboid intramembrane protease revealed by substrate-peptide complex structures<br>EMBO J (2014) 33, 2408-2421. PubMed  Europe PubMed DOI  S  I
    42. 2013
  42. Brooks,C.L. and Lemieux,M.J.<br>Untangling structure-function relationships in the rhomboid family of intramembrane proteases<br>Biochim Biophys Acta (2013) 1828, 2862-2872. PubMed  Europe PubMed DOI  V  S
  43. Ha,Y., Akiyama,Y. and Xue,Y.<br>Structure and mechanism of rhomboid protease<br>J Biol Chem (2013) 288, 15430-15436. PubMed  Europe PubMed DOI
  44. Lazareno-Saez,C., Arutyunova,E., Coquelle,N. and Lemieux,M.J.<br>Domain swapping in the cytoplasmic domain of the Escherichia coli rhomboid protease<br>J Mol Biol (2013) 425, 1127-1142. PubMed  Europe PubMed DOI  S
  45. Rather,P.<br>Role of rhomboid proteases in bacteria<br>Biochim Biophys Acta (2013) 1828, 2849-2854. PubMed  Europe PubMed DOI
  46. Vinothkumar,K.R., Pierrat,O.A., Large,J.M. and Freeman,M.<br>Structure of rhomboid protease in complex with beta-lactam inhibitors defines the S2' cavity<br>Structure (2013) 21, 1051-1058. PubMed  Europe PubMed DOI  S  I
  47. Vosyka,O., Vinothkumar,K.R., Wolf,E.V., Brouwer,A.J., Liskamp,R.M. and Verhelst,S.H.<br>Activity-based probes for rhomboid proteases discovered in a mass spectrometry-based assay<br>Proc Natl Acad Sci U S A (2013) 110, 2472-2477. PubMed  Europe PubMed DOI  S  I
  48. Wolf,E.V., Zeissler,A., Vosyka,O., Zeiler,E., Sieber,S. and Verhelst,S.H.<br>A new class of rhomboid protease inhibitors discovered by activity-based fluorescence polarization<br>PLoS ONE (2013) 8, e72307-e72307. PubMed  Europe PubMed DOI  PMC  EPMC  I
  49. Xue,Y. and Ha,Y.<br>Large lateral movement of transmembrane helix S5 is not required for substrate access to the active site of rhomboid intramembrane protease<br>J Biol Chem (2013) 288, 16645-16654. PubMed  Europe PubMed DOI  S  I
    50. 2012
  50. Reddy,T. and Rainey,J.K.<br>Multifaceted substrate capture scheme of a rhomboid protease<br>J Phys Chem B (2012) 116, 8942-8954. PubMed  Europe PubMed DOI
  51. Sampathkumar,P., Mak,M.W., Fischer-Witholt,S.J., Guigard,E., Kay,C.M. and Lemieux,M.J.<br>Oligomeric state study of prokaryotic rhomboid proteases<br>Biochim Biophys Acta (2012) 1818, 3090-3097. PubMed  Europe PubMed DOI
  52. Sherratt,A.R., Blais,D.R., Ghasriani,H., Pezacki,J.P. and Goto,N.K.<br>Activity-based protein profiling of the Escherichia coli GlpG rhomboid protein delineates the catalytic core<br>Biochemistry (2012) 51, 7794-7803. PubMed  Europe PubMed DOI
  53. Urban,S.<br>Bacterial and protozoan rhomboid proteases<br>[ISSN:978-0-12-407742-3] (2012) 3, 3581-3593. DOI
  54. Xue,Y. and Ha,Y.<br>Catalytic mechanism of rhomboid protease GlpG probed by 3,4-dichloroisocoumarin and diisopropyl fluorophosphonate<br>J Biol Chem (2012) 287, 3099-3107. PubMed  Europe PubMed DOI  S
  55. Xue,Y., Chowdhury,S., Liu,X., Akiyama,Y., Ellman,J. and Ha,Y.<br>Conformational change in rhomboid protease GlpG induced by inhibitor binding to Its S' subsites<br>Biochemistry (2012) 51, 3723-3731. PubMed  Europe PubMed DOI  S  I
  56. Zhou,Y., Moin,S.M., Urban,S. and Zhang,Y.<br>An internal water-retention site in the rhomboid intramembrane protease GlpG ensures catalytic efficiency<br>Structure (2012) 20, 1255-1263. PubMed  Europe PubMed DOI
    57. 2011
  57. Lazareno-Saez,C., Brooks,C.L. and Lemieux,M.J.<br>Structural comparison of substrate entry gate for rhomboid intramembrane peptidases<br>Biochem Cell Biol (2011) 89, 216-223. PubMed  Europe PubMed DOI  S
  58. Vinothkumar,K.R.<br>Structure of rhomboid protease in a lipid environment<br>J Mol Biol (2011) 407, 232-247. PubMed  Europe PubMed DOI  S
    59. 2010
  59. Urban,S.<br>Taking the plunge: integrating structural, enzymatic and computational insights into a unified model for membrane-immersed rhomboid proteolysis<br>Biochem J (2010) 425, 501-512. PubMed  Europe PubMed DOI  V
  60. Vinothkumar,K.R., Strisovsky,K., Andreeva,A., Christova,Y., Verhelst,S. and Freeman,M.<br>The structural basis for catalysis and substrate specificity of a rhomboid protease<br>EMBO J (2010) 29, 3797-3809. PubMed  Europe PubMed DOI  S  I
    61. 2009
  61. Bondar,A.N., del Val,C. and White,S.H.<br>Rhomboid protease dynamics and lipid interactions<br>Structure (2009) 17, 395-405. PubMed  Europe PubMed DOI  PMC  EPMC  S
  62. Erez,E. and Bibi,E.<br>Cleavage of a multispanning membrane protein by an intramembrane serine protease<br>Biochemistry (2009) 48, 12314-12322. PubMed  Europe PubMed DOI  P
    63. 2008
  63. Urban,S. and Baker,R.P.<br>In vivo analysis reveals substrate-gating mutants of a rhomboid intramembrane protease display increased activity in living cells<br>Biol Chem (2008) 389, 1107-1115. PubMed  Europe PubMed DOI
    64. 2007
  64. Akiyama,Y. and Maegawa,S.<br>Sequence features of substrates required for cleavage by GlpG, an Escherichia coli rhomboid protease<br>Mol Microbiol (2007) 64, 1028-1037. PubMed  Europe PubMed DOI
  65. Baker,R.P., Young,K., Feng,L., Shi,Y. and Urban,S.<br>Enzymatic analysis of a rhomboid intramembrane protease implicates transmembrane helix 5 as the lateral substrate gate<br>Proc Natl Acad Sci U S A (2007) 104, 8257-8262. PubMed  Europe PubMed DOI  PMC  EPMC
  66. Ben-Shem,A., Fass,D. and Bibi,E.<br>Structural basis for intramembrane proteolysis by rhomboid serine proteases<br>Proc Natl Acad Sci U S A (2007) 104, 462-466. PubMed  Europe PubMed DOI  PMC  EPMC  S
  67. Maegawa,S., Koide,K., Ito,K. and Akiyama,Y.<br>The intramembrane active site of GlpG, an E. coli rhomboid protease, is accessible to water and hydrolyses an extramembrane peptide bond of substrates<br>Mol Microbiol (2007) 64, 435-447. PubMed  Europe PubMed DOI
  68. [YEAR:13-2-2007]Wang,Y. and Ha,Y.<br>Open-cap conformation of intramembrane protease GlpG<br>Proc Natl Acad Sci U S A (13-2-2007) 104, 2098-2102. PubMed  Europe PubMed DOI  PMC  EPMC  S
  69. Wang,Y., Maegawa,S., Akiyama,Y. and Ha,Y.<br>The role of L1 Loop in the mechanism of rhomboid intramembrane protease GlpG<br>J Mol Biol (2007) 374, 1104-1113. PubMed  Europe PubMed DOI  PMC  EPMC
    70. 2006
  70. Clemmer,K.M., Sturgill,G.M., Veenstra,A. and Rather,P.N.<br>Functional characterization of Escherichia coli GlpG and additional rhomboid proteins using an aarA mutant of Providencia stuartii<br>J Bacteriol (2006) 188, 3415-3419. PubMed  Europe PubMed DOI  PMC  EPMC
  71. [YEAR:11-10-2006]Wang,Y., Zhang,Y. and Ha,Y.<br>Crystal structure of a rhomboid family intramembrane protease<br>Nature (11-10-2006) 444, 179-180. PubMed  Europe PubMed DOI  S
  72. Wu,Z., Yan,N., Feng,L., Oberstein,A., Yan,H., Baker,R.P., Gu,L., Jeffrey,P.D., Urban,S. and Shi,Y.<br>Structural analysis of a rhomboid family intramembrane protease reveals a gating mechanism for substrate entry<br>Nat Struct Mol Biol (2006) 13, 1084-1091. PubMed  Europe PubMed DOI  S
    73. 2005
  73. [YEAR:18-10-2005]Maegawa,S., Ito,K. and Akiyama,Y.<br>Proteolytic action of GlpG, a rhomboid protease in the Escherichia coli cytoplasmic membrane<br>Biochemistry (18-10-2005) 44, 13543-13552. PubMed  Europe PubMed DOI

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