Merops Switch to
Inhibitors

Peptidase

Family Clan SEARCHES BLAST
MEROPS SUBMISSIONS

Other
information

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.)

    2025
  1. 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.
    Engineering cardiolipin binding to an artificial membrane protein reveals determinants for lipid-mediated stabilization
    elife14, PubMed  Europe PubMed DOI
  2. Fremlen,H. and Burmann,B.M.
    Maintaining the Integral Membrane Proteome: Revisiting the Functional Repertoire of Integral Membrane Proteases
    Chembiocheme202500048-e202500048. PubMed  Europe PubMed DOI  V
    3. 2024
  3. 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.
    Extensive targeting of chemical space at the prime side of ketoamide inhibitors of rhomboid proteases by branched substituents empowers their selectivity and potency
    Eur J Med Chem275, 116606-116606. PubMed  Europe PubMed DOI
  4. Engberg,O., Mathath,A.V., Dobel,V., Frie,C., Lemberg,M.K., Chakraborty,D. and Huster,D.
    Evaluating the Impact of the Membrane Thickness on the Function of the Intramembrane Protease GlpG
    Biophys J PubMed  Europe PubMed DOI
  5. Nimerovsky,E., Kosteletos,S., Lange,S., Becker,S., Lange,A. and Andreas,L.B.
    Homonuclear Simplified Preservation of Equivalent Pathways Spectroscopy
    J Phys Chem Lett15, 6272-6278. PubMed  Europe PubMed DOI
  6. Roberts,C.S., Shannon,A.B., Korotkov,K.V. and Sandkvist,M.
    Differential processing of VesB by two rhomboid proteases in Vibrio cholerae
    MBioe0127024-e0127024. PubMed  Europe PubMed DOI
  7. Sawczyc,H., Tatsuta,T., Oster,C., Kosteletos,S., Lange,S., Bohg,C., Langer,T. and Lange,A.
    Lipid-polymer nanoparticles to probe the native-like environment of intramembrane rhomboid protease GlpG and its activity
    Nat Commun15, 7533-7533. PubMed  Europe PubMed DOI
    8. 2023
  8. Bohg,C., Oster,C., Turkaydin,B., Lisurek,M., Sanchez-Carranza,P., Lange,S., Utesch,T., Sun,H. and Lange,A.
    The opening dynamics of the lateral gate regulates the activity of rhomboid proteases
    Sci Adv9, eadh3858-eadh3858. PubMed  Europe PubMed DOI
    9. 2022
  9. Engberg,O., Ulbricht,D., Dobel,V., Siebert,V., Frie,C., Penk,A., Lemberg,M.K. and Huster,D.
    Rhomboid-catalyzed intramembrane proteolysis requires hydrophobic matching with the surrounding lipid bilayer
    Sci Adv8, eabq8303-eabq8303. PubMed  Europe PubMed DOI
    10. 2021
  10. Bohg,C., Oster,C., Utesch,T., Bischoff,S., Lange,S., Shi,C., Sun,H. and Lange,A.
    A combination of solid-state NMR and MD simulations reveals the binding mode of a rhomboid protease inhibitor
    Chem Sci12, 12754-12762. PubMed  Europe PubMed DOI
  11. Mitra,D. and Das Mohapatra,P.K.
    Discovery of Novel Cyclic Salt Bridge in Thermophilic Bacterial Protease and Study of its Sequence and Structure
    Appl Biochem Biotechnol PubMed  Europe PubMed DOI
  12. 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.
    Cys-labeling kinetics of membrane protein GlpG: a role for specific SDS binding and micelle changes?
    Biophys J PubMed  Europe PubMed DOI
    13. 2020
  13. Bondar,A.N.
    Phosphatidylglyerol Lipid Binding at the Active Site of an Intramembrane Protease
    J Membr Biol253, 563-576. PubMed  Europe PubMed DOI  V
  14. Guo,R., Cang,Z., Yao,J., Kim,M., Deans,E., Wei,G., Kang,S.G. and Hong,H.
    Structural cavities are critical to balancing stability and activity of a membrane-integral enzyme
    Proc Natl Acad Sci U S A117, 22146-22156. PubMed  Europe PubMed DOI
  15. Knopf,J.D. and Lemberg,M.K.
    Derlins with scissors: primordial ERAD in bacteria
    EMBO Je105012-e105012. PubMed  Europe PubMed DOI
    16. 2019
  16. Almeida-Hernandez,Y. and Tidow,H.
    Soluble regions of GlpG influence protein-lipid interactions and lipid distribution
    J Phys Chem B123, 7852-7858. PubMed  Europe PubMed DOI
  17. Bondar,A.N.
    Mechanisms by which lipids influence conformational dynamics of the GlpG intramembrane protease
    J Phys Chem B123, 4159-4172. PubMed  Europe PubMed DOI
  18. Cho,S., Baker,R.P., Ji,M. and Urban,S.
    Ten catalytic snapshots of rhomboid intramembrane proteolysis from gate opening to peptide release
    Nat Struct Mol Biol26, 910-918. PubMed  Europe PubMed DOI  S
  19. Gaffney,K.A. and Hong,H.
    The rhomboid protease GlpG has weak interaction energies in its active site hydrogen bond network
    J Gen Physiol151, 282-291. PubMed  Europe PubMed DOI
  20. Shi,C., Oster,C., Bohg,C., Li,L., Lange,S., Chevelkov,V. and Lange,A.
    Structure and dynamics of the rhomboid protease GlpG in liposomes studied by solid-state NMR
    J Am Chem Soc141, 17314-17321. PubMed  Europe PubMed DOI  S
    21. 2018
  21. 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.
    Unwinding of the substrate transmembrane helix in intramembrane proteolysis
    Biophys J114, 1579-1589. PubMed  Europe PubMed DOI
  22. Yang,J., Barniol-Xicota,M., Nguyen,M.T.N., Ticha,A., Strisovsky,K. and Verhelst,S.H.L.
    Benzoxazin-4-ones as novel, easily accessible inhibitors for rhomboid proteases
    Bioorg Med Chem Lett28, 1423-1427. PubMed  Europe PubMed DOI  I
  23. Yang,Y., Guo,R., Gaffney,K., Kim,M., Muhammednazaar,S., Tian,W., Wang,B., Liang,J. and Hong,H.
    Folding-degradation relationship of a membrane protein mediated by the universally conserved ATP-dependent protease FtsH
    J Am Chem Soc140, 4656-4665. PubMed  Europe PubMed DOI
    24. 2017
  24. Arutyunova,E., Panigrahi,R., Strisovsky,K. and Lemieux,M.J.
    Production of recombinant rhomboid proteases
    Methods Enzymol584, 255-278. PubMed  Europe PubMed DOI  E
  25. Cordier,B. and Lemberg,M.K.
    Probing the activity of eukaryotic rhomboid proteases in vitro
    Methods Enzymol584, 99-126. PubMed  Europe PubMed DOI  A  E
  26. 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.
    Discovery and biological evaluation of potent and selective N-methylene saccharin-derived inhibitors for rhomboid intramembrane proteases
    Biochemistry56, 6713-6725. PubMed  Europe PubMed DOI  I
  27. Russell,C.W., Richards,A.C., Chang,A.S. and Mulvey,M.A.
    The rhomboid protease GlpG promotes the persistence of extraintestinal pathogenic Escherichia coli within the gut
    Infect Immun85, e00866-16-e00866-16. PubMed  Europe PubMed DOI
  28. Shokhen,M. and Albeck,A.
    How does the exosite of rhomboid protease affect substrate processing and inhibition?
    Protein Sci26, 2355-2366. PubMed  Europe PubMed DOI
  29. 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.
    General and modular strategy for designing potent, selective, and pharmacologically compliant inhibitors of rhomboid proteases
    Cell Chem Biol24, 1523-1536. PubMed  Europe PubMed DOI  S  I
    30. 2016
  30. Cho,S., Dickey,S.W. and Urban,S.
    Crystal structures and inhibition kinetics reveal a two-stage catalytic mechanism with drug design implications for rhomboid proteolysis
    Mol Cell61, 329-340. PubMed  Europe PubMed DOI  I
  31. Guo,R., Gaffney,K., Yang,Z., Kim,M., Sungsuwan,S., Huang,X., Hubbell,W.L. and Hong,H.
    Steric trapping reveals a cooperativity network in the intramembrane protease GlpG
    Nat Chem Biol12, 353-360. PubMed  Europe PubMed DOI
  32. Schafer,N.P., Truong,H.H., Otzen,D.E., Lindorff-Larsen,K. and Wolynes,P.G.
    Topological constraints and modular structure in the folding and functional motions of GlpG, an intramembrane protease
    Proc Natl Acad Sci U S A113, 2098-2103. PubMed  Europe PubMed DOI
  33. Uritsky,N., Shokhen,M. and Albeck,A.
    Stepwise versus concerted mechanisms in general-base catalysis by serine proteases
    Angew Chem Int Ed Engl55, 1680-1684. PubMed  Europe PubMed DOI
  34. Wolf,E.V. and Verhelst,S.H.
    Inhibitors of rhomboid proteases
    Biochimie122, 38-47. PubMed  Europe PubMed DOI  I
    35. 2015
  35. Foo,A.C., Harvey,B.G., Metz,J.J. and Goto,N.K.
    Influence of hydrophobic mismatch on the catalytic activity of Escherichia coli GlpG rhomboid protease
    Protein Sci24, 464-473. PubMed  Europe PubMed DOI
  36. Min,D., Jefferson,R.E., Bowie,J.U. and Yoon,T.Y.
    Mapping the energy landscape for second-stage folding of a single membrane protein
    Nat Chem Biol11, 981-987. PubMed  Europe PubMed DOI
  37. Paslawski,W., Lillelund,O.K., Kristensen,J.V., Schafer,N.P., Baker,R.P., Urban,S. and Otzen,D.E.
    Cooperative folding of a polytopic alpha-helical membrane protein involves a compact N-terminal nucleus and nonnative loops
    Proc Natl Acad Sci U S A112, 7978-7983. PubMed  Europe PubMed DOI
    38. 2014
  38. Ghasriani,H., Kwok,J.K., Sherratt,A.R., Foo,A.C., Qureshi,T. and Goto,N.K.
    Micelle-catalyzed domain swapping in the GlpG rhomboid protease cytoplasmic domain
    Biochemistry53, 5907-5915. PubMed  Europe PubMed DOI
  39. Zoll,S., Stanchev,S., Began,J., Skerle,J., Lepsik,M., Peclinovska,L., Majer,P. and Strisovsky,K.
    Substrate binding and specificity of rhomboid intramembrane protease revealed by substrate-peptide complex structures
    EMBO J33, 2408-2421. PubMed  Europe PubMed DOI  S  I
    40. 2013
  40. Brooks,C.L. and Lemieux,M.J.
    Untangling structure-function relationships in the rhomboid family of intramembrane proteases
    Biochim Biophys Acta1828, 2862-2872. PubMed  Europe PubMed DOI  V  S
  41. Ha,Y., Akiyama,Y. and Xue,Y.
    Structure and mechanism of rhomboid protease
    J Biol Chem288, 15430-15436. PubMed  Europe PubMed DOI
  42. Lazareno-Saez,C., Arutyunova,E., Coquelle,N. and Lemieux,M.J.
    Domain swapping in the cytoplasmic domain of the Escherichia coli rhomboid protease
    J Mol Biol425, 1127-1142. PubMed  Europe PubMed DOI  S
  43. Rather,P.
    Role of rhomboid proteases in bacteria
    Biochim Biophys Acta1828, 2849-2854. PubMed  Europe PubMed DOI
  44. Vinothkumar,K.R., Pierrat,O.A., Large,J.M. and Freeman,M.
    Structure of rhomboid protease in complex with beta-lactam inhibitors defines the S2' cavity
    Structure21, 1051-1058. PubMed  Europe PubMed DOI  S  I
  45. Vosyka,O., Vinothkumar,K.R., Wolf,E.V., Brouwer,A.J., Liskamp,R.M. and Verhelst,S.H.
    Activity-based probes for rhomboid proteases discovered in a mass spectrometry-based assay
    Proc Natl Acad Sci U S A110, 2472-2477. PubMed  Europe PubMed DOI  S  I
  46. Wolf,E.V., Zeissler,A., Vosyka,O., Zeiler,E., Sieber,S. and Verhelst,S.H.
    A new class of rhomboid protease inhibitors discovered by activity-based fluorescence polarization
    PLoS ONE8, e72307-e72307. PubMed  Europe PubMed DOI  I
  47. Xue,Y. and Ha,Y.
    Large lateral movement of transmembrane helix S5 is not required for substrate access to the active site of rhomboid intramembrane protease
    J Biol Chem288, 16645-16654. PubMed  Europe PubMed DOI  S  I
    48. 2012
  48. Reddy,T. and Rainey,J.K.
    Multifaceted substrate capture scheme of a rhomboid protease
    J Phys Chem B116, 8942-8954. PubMed  Europe PubMed DOI
  49. Sampathkumar,P., Mak,M.W., Fischer-Witholt,S.J., Guigard,E., Kay,C.M. and Lemieux,M.J.
    Oligomeric state study of prokaryotic rhomboid proteases
    Biochim Biophys Acta1818, 3090-3097. PubMed  Europe PubMed DOI
  50. Sherratt,A.R., Blais,D.R., Ghasriani,H., Pezacki,J.P. and Goto,N.K.
    Activity-based protein profiling of the Escherichia coli GlpG rhomboid protein delineates the catalytic core
    Biochemistry51, 7794-7803. PubMed  Europe PubMed DOI
  51. Urban,S.
    Bacterial and protozoan rhomboid proteases
    [ISSN:978-0-12-407742-3]3, 3581-3593. DOI
  52. Xue,Y., Chowdhury,S., Liu,X., Akiyama,Y., Ellman,J. and Ha,Y.
    Conformational change in rhomboid protease GlpG induced by inhibitor binding to Its S' subsites
    Biochemistry51, 3723-3731. PubMed  Europe PubMed DOI  S  I
  53. Xue,Y. and Ha,Y.
    Catalytic mechanism of rhomboid protease GlpG probed by 3,4-dichloroisocoumarin and diisopropyl fluorophosphonate
    J Biol Chem287, 3099-3107. PubMed  Europe PubMed DOI  S
  54. Zhou,Y., Moin,S.M., Urban,S. and Zhang,Y.
    An internal water-retention site in the rhomboid intramembrane protease GlpG ensures catalytic efficiency
    Structure20, 1255-1263. PubMed  Europe PubMed DOI
    55. 2011
  55. Lazareno-Saez,C., Brooks,C.L. and Lemieux,M.J.
    Structural comparison of substrate entry gate for rhomboid intramembrane peptidases
    Biochem Cell Biol89, 216-223. PubMed  Europe PubMed DOI  S
  56. Vinothkumar,K.R.
    Structure of rhomboid protease in a lipid environment
    J Mol Biol407, 232-247. PubMed  Europe PubMed DOI  S
    57. 2010
  57. Urban,S.
    Taking the plunge: integrating structural, enzymatic and computational insights into a unified model for membrane-immersed rhomboid proteolysis
    Biochem J425, 501-512. PubMed  Europe PubMed DOI  V
  58. Vinothkumar,K.R., Strisovsky,K., Andreeva,A., Christova,Y., Verhelst,S. and Freeman,M.
    The structural basis for catalysis and substrate specificity of a rhomboid protease
    EMBO J29, 3797-3809. PubMed  Europe PubMed DOI  S  I
    59. 2009
  59. Bondar,A.N., del Val,C. and White,S.H.
    Rhomboid protease dynamics and lipid interactions
    Structure17, 395-405. PubMed  Europe PubMed DOI  S
  60. Erez,E. and Bibi,E.
    Cleavage of a multispanning membrane protein by an intramembrane serine protease
    Biochemistry48, 12314-12322. PubMed  Europe PubMed DOI  P
    61. 2008
  61. Urban,S. and Baker,R.P.
    In vivo analysis reveals substrate-gating mutants of a rhomboid intramembrane protease display increased activity in living cells
    Biol Chem389, 1107-1115. PubMed  Europe PubMed DOI
    62. 2007
  62. Akiyama,Y. and Maegawa,S.
    Sequence features of substrates required for cleavage by GlpG, an Escherichia coli rhomboid protease
    Mol Microbiol64, 1028-1037. PubMed  Europe PubMed DOI
  63. Baker,R.P., Young,K., Feng,L., Shi,Y. and Urban,S.
    Enzymatic analysis of a rhomboid intramembrane protease implicates transmembrane helix 5 as the lateral substrate gate
    Proc Natl Acad Sci U S A104, 8257-8262. PubMed  Europe PubMed DOI
  64. Ben-Shem,A., Fass,D. and Bibi,E.
    Structural basis for intramembrane proteolysis by rhomboid serine proteases
    Proc Natl Acad Sci U S A104, 462-466. PubMed  Europe PubMed DOI  S
  65. Maegawa,S., Koide,K., Ito,K. and Akiyama,Y.
    The intramembrane active site of GlpG, an E. coli rhomboid protease, is accessible to water and hydrolyses an extramembrane peptide bond of substrates
    Mol Microbiol64, 435-447. PubMed  Europe PubMed DOI
  66. Wang,Y., Maegawa,S., Akiyama,Y. and Ha,Y.
    The role of L1 Loop in the mechanism of rhomboid intramembrane protease GlpG
    J Mol Biol374, 1104-1113. PubMed  Europe PubMed DOI
  67. [YEAR:13-2-2007]Wang,Y. and Ha,Y.
    Open-cap conformation of intramembrane protease GlpG
    Proc Natl Acad Sci U S A104, 2098-2102. PubMed  Europe PubMed DOI  S
    68. 2006
  68. Clemmer,K.M., Sturgill,G.M., Veenstra,A. and Rather,P.N.
    Functional characterization of Escherichia coli GlpG and additional rhomboid proteins using an aarA mutant of Providencia stuartii
    J Bacteriol188, 3415-3419. PubMed  Europe PubMed DOI
  69. [YEAR:11-10-2006]Wang,Y., Zhang,Y. and Ha,Y.
    Crystal structure of a rhomboid family intramembrane protease
    Nature444, 179-180. PubMed  Europe PubMed DOI  S
  70. Wu,Z., Yan,N., Feng,L., Oberstein,A., Yan,H., Baker,R.P., Gu,L., Jeffrey,P.D., Urban,S. and Shi,Y.
    Structural analysis of a rhomboid family intramembrane protease reveals a gating mechanism for substrate entry
    Nat Struct Mol Biol13, 1084-1091. PubMed  Europe PubMed DOI  S
    71. 2005
  71. [YEAR:18-10-2005]Maegawa,S., Ito,K. and Akiyama,Y.
    Proteolytic action of GlpG, a rhomboid protease in the Escherichia coli cytoplasmic membrane
    Biochemistry44, 13543-13552. PubMed  Europe PubMed DOI

feedback
Page created 8-September-2023

EMBL-EBI logo

© 2025 EBI
Terms of use