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Literature for peptidase S08.012: PfSUB1 peptidase

Summary Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates

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

    2025
  1. Puszko,A.K., Batista,F.A., Ejjoummany,A., Bouillon,A., Maurel,M., Adler,P., Legru,A., Martinez,M., Ortega Varga,L., Hadjadj,M., Alzari,P.M., Blondel,A., Haouz,A., Barale,J.C. and Hernandez,J.F.<br>Towards Improved Peptidic alpha-Ketoamide Inhibitors of the Plasmodial Subtilisin-Like SUB1: Exploration of N-Terminal Extensions and Cyclic Constraints<br>ChemMedChem (2025) , e202400924-e202400924. PubMed  Europe PubMed DOI
    2. 2024
  2. Legru,A., Batista,F.A., Puszko,A.K., Bouillon,A., Maurel,M., Martinez,M., Ejjoummany,A., Ortega Varga,L., Adler,P., Mechaly,A., Hadjadj,M., Sosnowski,P., Hopfgartner,G., Alzari,P.M., Blondel,A., Haouz,A., Barale,J.C. and Hernandez,J.F.<br>Insights from structure-activity relationships and the binding mode of peptidic alpha-ketoamide inhibitors of the malaria drug target subtilisin-like SUB1<br>Eur J Med Chem (2024) 269, 116308-116308. PubMed  Europe PubMed DOI  I
  3. Martinez,M., Bouillon,A., Brule,S., Raynal,B., Haouz,A., Alzari,P.M. and Barale,J.C.<br>Prodomain-driven enzyme dimerization: a pH-dependent autoinhibition mechanism that controls Plasmodium Sub1 activity before merozoite egress<br>MBio (2024) 15, e0019824-e0019824. PubMed  Europe PubMed DOI  PMC  EPMC
  4. Withers-Martinez,C., George,R., Maslen,S., Jean,L., Hackett,F., Skehel,M. and Blackman,M.J.<br>The malaria parasite egress protease SUB1 is activated through precise, plasmepsin X-mediated cleavage of the SUB1 prodomain<br>Biochim Biophys Acta Gen Subj (2024) 1868, 130665-130665. PubMed  Europe PubMed DOI
    5. 2023
  5. Martinez,M., Batista,F.A., Maurel,M., Bouillon,A., Ortega Varga,L., Wehenkel,A.M., Le Chevalier-Sontag,L., Blondel,A., Haouz,A., Hernandez,J.F., Alzari,P.M. and Barale,J.C.<br>3D structures of the Plasmodium vivax subtilisin-like drug target SUB1 reveal conformational changes to accommodate a substrate-derived alpha-ketoamide inhibitor<br>Acta Crystallogr D Struct Biol (2023) 79, 721-734. PubMed  Europe PubMed DOI  I
  6. Mukherjee,S., Nasamu,A.S., Rubiano,K. and Goldberg,D.E.<br>Activation of the Plasmodium egress effector subtilisin-like protease 1 is achieved by plasmepsin X destruction of the propiece<br>bioRxiv (2023) PubMed  Europe PubMed DOI  PMC  EPMC  K
    7. 2022
  7. Lidumniece,E., Withers-Martinez,C., Hackett,F., Blackman,M.J. and Jirgensons,A.<br>Subtilisin-like Serine Protease 1 (SUB1) as an Emerging Antimalarial Drug Target: Current Achievements in Inhibitor Discovery<br>J Med Chem (2022) 65, 12535-12545. PubMed  Europe PubMed DOI
    8. 2021
  8. Lidumniece,E., Withers-Martinez,C., Hackett,F., Collins,C.R., Perrin,A.J., Koussis,K., Bisson,C., Blackman,M.J. and Jirgensons,A.<br>Peptidic boronic acids are potent cell-permeable inhibitors of the malaria parasite egress serine protease SUB1<br>Proc Natl Acad Sci U S A (2021) 118 PubMed  Europe PubMed DOI  PMC  EPMC  I
    9. 2020
  9. Burrows,J.N. and Soldati-Favre,D.<br>Targeting plasmepsins - an Achilles' Heel of the malaria parasite<br>Cell Host Microbe (2020) 27, 496-498. PubMed  Europe PubMed DOI  I
  10. Fierro,M.A., Asady,B., Brooks,C.F., Cobb,D.W., Villegas,A., Moreno,S.N.J. and Muralidharan,V.<br>An endoplasmic reticulum CREC family protein regulates the egress proteolytic cascade in malaria parasites<br>MBio (2020) 11 PubMed  Europe PubMed DOI
  11. Tarr,S.J., Withers-Martinez,C., Flynn,H.R., Snijders,A.P., Masino,L., Koussis,K., Conway,D.J. and Blackman,M.J.<br>A malaria parasite subtilisin propeptide-like protein is a potent inhibitor of the egress protease SUB1<br>Biochem J (2020) 477, 525-540. PubMed  Europe PubMed DOI
    12. 2019
  12. Pace,T., Grasso,F., Camarda,G., Suarez,C., Blackman,M.J., Ponzi,M. and Olivieri,A.<br>The Plasmodium berghei serine protease PbSUB1 plays an important role in male gamete egress<br>Cell Microbiol (2019) , e13028-e13028. PubMed  Europe PubMed DOI
  13. Zogota,R., Kinena,L., Withers-Martinez,C., Blackman,M.J., Bobrovs,R., Pantelejevs,T., Kanepe-Lapsa,I., Ozola,V., Jaudzems,K., Suna,E. and Jirgensons,A.<br>Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D<br>Eur J Med Chem (2019) 163, 344-352. PubMed  Europe PubMed DOI
    14. 2018
  14. Thomas,J.A., Tan,M.S.Y., Bisson,C., Borg,A., Umrekar,T.R., Hackett,F., Hale,V.L., Vizcay-Barrena,G., Fleck,R.A., Snijders,A.P., Saibil,H.R. and Blackman,M.J.<br>A protease cascade regulates release of the human malaria parasite Plasmodium falciparum from host red blood cells<br>Nat Microbiol (2018) 3, 447-455. PubMed  Europe PubMed DOI
    15. 2017
  15. Collins,C.R., Hackett,F., Atid,J., Tan,M.S.Y. and Blackman,M.J.<br>The Plasmodium falciparum pseudoprotease SERA5 regulates the kinetics and efficiency of malaria parasite egress from host erythrocytes<br>PLoS Pathog (2017) 13, e1006453-e1006453. PubMed  Europe PubMed DOI  PMC  EPMC
    16. 2016
  16. Brogi,S., Giovani,S., Brindisi,M., Gemma,S., Novellino,E., Campiani,G., Blackman,M.J. and Butini,S.<br>In silico study of subtilisin-like protease 1 (SUB1) from different Plasmodium species in complex with peptidyl-difluorostatones and characterization of potent pan-SUB1 inhibitors<br>J Mol Graph Model (2016) 64, 121-130. PubMed  Europe PubMed DOI  I
  17. Subathra Devi,C., Verma,P., Srivastava,S., Ravikumar,P., Kalwani,V., Tandon,A. and Mohanasrinivasan,V.<br>Development of a novel malarial vaccine design: a hypothetical approach<br>Curr Drug Discov Technol (2016) 11, 239-242. PubMed  Europe PubMed  I
    18. 2015
  18. Das,S., Hertrich,N., Perrin,A.J., Withers-Martinez,C., Collins,C.R., Jones,M.L., Watermeyer,J.M., Fobes,E.T., Martin,S.R., Saibil,H.R., Wright,G.J., Treeck,M., Epp,C. and Blackman,M.J.<br>Processing of Plasmodium falciparum merozoite surface protein MSP1 activates a spectrin-binding function enabling parasite egress from RBCs<br>Cell Host Microbe (2015) 18, 433-444. PubMed  Europe PubMed DOI
  19. Giovani,S., Penzo,M., Butini,S., Brindisi,M., Gemma,S., Novellino,E., Campiani,G., Blackman,M.J. and Brogi,S.<br>Plasmodium falciparum subtilisin-like protease 1: discovery of potent difluorostatone-based inhibitors<br>Chem Soc Rev (2015) 5, 22431-22448. DOI  I
  20. Kher,S.S., Penzo,M., Fulle,S., Ebejer,J.P., Finn,P.W., Blackman,M.J. and Jirgensons,A.<br>Quinoxaline-based inhibitors of malarial protease PfSUB1<br>Chem Heterocycl Compd (2015) 50, 1457-1463. DOI  I
    21. 2014
  21. Alam,A.<br>Serine proteases of malaria parasite Plasmodium falciparum: potential as antimalarial drug targets<br>Interdiscip Perspect Infect Dis (2014) 2014, 453186-453186. PubMed  Europe PubMed DOI  PMC  EPMC  V
  22. Bastianelli,G., Bouillon,A., Nguyen,C., Le-Nguyen,D., Nilges,M. and Barale,J.C.<br>Computational design of protein-based inhibitors of Plasmodium vivax subtilisin-like 1 protease<br>PLoS ONE (2014) 9, e109269-e109269. PubMed  Europe PubMed DOI  PMC  EPMC
  23. Giganti,D., Bouillon,A., Tawk,L., Robert,F., Martinez,M., Crublet,E., Weber,P., Girard-Blanc,C., Petres,S., Haouz,A., Hernandez,J.F., Mercereau-Puijalon,O., Alzari,P.M. and Barale,J.C.<br>A novel Plasmodium-specific prodomain fold regulates the malaria drug target SUB1 subtilase<br>Nat Commun (2014) 5, 4833-4833. PubMed  Europe PubMed DOI  S
  24. Giovani,S., Penzo,M., Brogi,S., Brindisi,M., Gemma,S., Novellino,E., Savini,L., Blackman,M.J., Campiani,G. and Butini,S.<br>Rational design of the first difluorostatone-based PfSUB1 inhibitors<br>Bioorg Med Chem Lett (2014) 24, 3582-3586. PubMed  Europe PubMed DOI  I
  25. Kher,S.S., Penzo,M., Fulle,S., Finn,P.W., Blackman,M.J. and Jirgensons,A.<br>Substrate derived peptidic alpha-ketoamides as inhibitors of the malarial protease PfSUB1<br>Bioorg Med Chem Lett (2014) 24, 4486-4489. PubMed  Europe PubMed DOI  I
  26. Withers-Martinez,C., Strath,M., Hackett,F., Haire,L.F., Howell,S.A., Walker,P.A., Christodoulou,E., Evangelos,C., Dodson,G.G. and Blackman,M.J.<br>The malaria parasite egress protease SUB1 is a calcium-dependent redox switch subtilisin<br>Nat Commun (2014) 5, 3726-3726. PubMed  Europe PubMed DOI  S
    27. 2013
  27. Agarwal,S., Singh,M.K., Garg,S., Chitnis,C.E. and Singh,S.<br>Ca(2+)-mediated exocytosis of subtilisin-like protease 1: a key step in egress of Plasmodium falciparum merozoites<br>Cell Microbiol (2013) 15, 910-921. PubMed  Europe PubMed DOI
  28. Bouillon,A., Giganti,D., Benedet,C., Gorgette,O., Petres,S., Crublet,E., Girard-Blanc,C., Witkowski,B., Menard,D., Nilges,M., Mercereau-Puijalon,O., Stoven,V. and Barale,J.C.<br>In silico screening on the three-dimensional model of the Plasmodium vivax SUB1 protease leads to the validation of a novel anti-parasite compound<br>J Biol Chem (2013) 288, 18561-18573. PubMed  Europe PubMed DOI  I
  29. Collins,C.R., Hackett,F., Strath,M., Penzo,M., Withers-Martinez,C., Baker,D.A. and Blackman,M.J.<br>Malaria parasite cGMP-dependent protein kinase regulates blood stage merozoite secretory organelle discharge and egress<br>PLoS Pathog (2013) 9, e1003344-e1003344. PubMed  Europe PubMed DOI  PMC  EPMC
  30. Fulle,S., Withers-Martinez,C., Blackman,M.J., Morris,G.M. and Finn,P.W.<br>Molecular determinants of binding to the Plasmodium subtilisin-like protease 1<br>J Chem Inf Model (2013) 53, 573-583. PubMed  Europe PubMed DOI
  31. Suarez,C., Volkmann,K., Gomes,A.R., Billker,O. and Blackman,M.J.<br>The malarial serine protease SUB1 plays an essential role in parasite liver stage development<br>PLoS Pathog (2013) 9, e1003811-e1003811. PubMed  Europe PubMed DOI  PMC  EPMC
  32. Tawk,L., Lacroix,C., Gueirard,P., Kent,R., Gorgette,O., Thiberge,S., Mercereau-Puijalon,O., Menard,R. and Barale,J.C.<br>A key role for Plasmodium subtilisin-like SUB1 protease in egress of malaria parasites from host hepatocytes<br>J Biol Chem (2013) 288, 33336-33346. PubMed  Europe PubMed DOI
    33. 2012
  33. Gemma,S., Giovani,S., Brindisi,M., Tripaldi,P., Brogi,S., Savini,L., Fiorini,I., Novellino,E., Butini,S., Campiani,G., Penzo,M. and Blackman,M.J.<br>Quinolylhydrazones as novel inhibitors of Plasmodium falciparum serine protease PfSUB1<br>Bioorg Med Chem Lett (2012) 22, 5317-5321. PubMed  Europe PubMed DOI  I
  34. Ruecker,A., Shea,M., Hackett,F., Suarez,C., Hirst,E.M., Milutinovic,K., Withers-Martinez,C. and Blackman,M.J.<br>Proteolytic activation of the essential parasitophorous vacuole cysteine protease SERA6 accompanies malaria parasite egress from its host erythrocyte<br>J Biol Chem (2012) 287, 37949-37963. PubMed  Europe PubMed DOI
  35. Silmon de Monerri,N.C., Ruecker,A. and Blackman,M.J.<br>Plasmodium subtilisins<br>[ISSN:978-0-12-407742-3] (2012) 3, 3260-3265. DOI
  36. Withers-Martinez,C., Suarez,C., Fulle,S., Kher,S., Penzo,M., Ebejer,J.P., Koussis,K., Hackett,F., Jirgensons,A., Finn,P. and Blackman,M.J.<br>Plasmodium subtilisin-like protease 1 (SUB1): insights into the active-site structure, specificity and function of a pan-malaria drug target<br>Int J Parasitol (2012) 42, 597-612. PubMed  Europe PubMed DOI  I
    37. 2011
  37. Bastianelli,G., Bouillon,A., Nguyen,C., Crublet,E., Petres,S., Gorgette,O., Le-Nguyen,D., Barale,J.C. and Nilges,M.<br>Computational reverse-engineering of a spider-venom derived peptide active against Plasmodium falciparum SUB1<br>PLoS ONE (2011) 6, e21812-e21812. PubMed  Europe PubMed DOI  PMC  EPMC  I
  38. Moneriz,C., Mestres,J., Bautista,J.M., Diez,A. and Puyet,A.<br>Multi-targeted activity of maslinic acid as an antimalarial natural compound<br>FEBS J (2011) 278, 2951-2961. PubMed  Europe PubMed DOI  I
  39. Silmon de Monerri,N.C., Flynn,H.R., Campos,M.G., Hackett,F., Koussis,K., Withers-Martinez,C., Skehel,J.M. and Blackman,M.J.<br>Global identification of multiple substrates for Plasmodium falciparum SUB1, an essential malarial processing protease<br>Infect Immun (2011) 79, 1086-1097. PubMed  Europe PubMed DOI
    40. 2010
  40. Child,M.A., Epp,C., Bujard,H. and Blackman,M.J.<br>Regulated maturation of malaria merozoite surface protein-1 is essential for parasite growth<br>Mol Microbiol (2010) 78, 187-202. PubMed  Europe PubMed DOI
    41. 2009
  41. Koussis,K., Withers-Martinez,C., Yeoh,S., Child,M., Hackett,F., Knuepfer,E., Juliano,L., Woehlbier,U., Bujard,H. and Blackman,M.J.<br>A multifunctional serine protease primes the malaria parasite for red blood cell invasion<br>EMBO J (2009) 28, 725-735. PubMed  Europe PubMed DOI  PMC  EPMC
    42. 2008
  42. Arastu-Kapur,S., Ponder,E.L., Fonovic,U.P., Yeoh,S., Yuan,F., Fonovic,M., Grainger,M., Phillips,C.I., Powers,J.C. and Bogyo,M.<br>Identification of proteases that regulate erythrocyte rupture by the malaria parasite Plasmodium falciparum<br>Nat Chem Biol (2008) 4, 203-213. PubMed  Europe PubMed DOI  I
  43. Blackman,M.J.<br>Malarial proteases and host cell egress: an 'emerging' cascade<br>Cell Microbiol (2008) 10, 1925-1934. PubMed  Europe PubMed DOI  PMC  EPMC  T
    44. 2007
  44. Janse,C.J. and Waters,A.P.<br>The exoneme helps malaria parasites to break out of blood cells<br>Cell (2007) 131, 1036-1038. PubMed  Europe PubMed DOI
  45. Yeoh,S., O'Donnell,R.A., Koussis,K., Dluzewski,A.R., Ansell,K.H., Osborne,S.A., Hackett,F., Withers-Martinez,C., Mitchell,G.H., Bannister,L.H., Bryans,J.S., Kettleborough,C.A. and Blackman,M.J.<br>Subcellular discharge of a serine protease mediates release of invasive malaria parasites from host erythrocytes<br>Cell (2007) 131, 1072-1083. PubMed  Europe PubMed DOI
    46. 2005
  46. [YEAR:22-9-2005]Jean,L., Withers-Martinez,C., Hackett,F. and Blackman,M.J.<br>Unique insertions within Plasmodium falciparum subtilisin-like protease-1 are crucial for enzyme maturation and activity<br>Mol Biochem Parasitol (22-9-2005) 144, 187-197. PubMed  Europe PubMed DOI
    47. 2004
  47. Blackman,M.J.<br>Plasmodium subtilisins<br>[ISSN:0-12-079610-4] (2004) 2, 1841-1844.  V
  48. Withers-Martinez,C., Jean,L. and Blackman,M.J.<br>Subtilisin-like proteases of the malaria parasite<br>Mol Microbiol (2004) 53, 55-63. PubMed  Europe PubMed DOI
    49. 2003
  49. [YEAR:1-8-2003]Jean,L., Hackett,F., Martin,S.R. and Blackman,M.J.<br>Functional characterization of the propeptide of Plasmodium falciparum subtilisin-like protease-1<br>J Biol Chem (1-8-2003) 278, 28572-28579. PubMed  Europe PubMed DOI
    50. 2002
  50. [YEAR:8-10-2002]Blackman,M.J., Corrie,J.E., Croney,J.C., Kelly,G., Eccleston,J.F. and Jameson,D.M.<br>Structural and biochemical characterization of a fluorogenic rhodamine-labeled malarial protease substrate<br>Biochemistry (8-10-2002) 41, 12244-12252. PubMed  Europe PubMed DOI  A
  51. [YEAR:16-8-2002]Withers-Martinez,C., Saldanha,J.W., Ely,B., Hackett,F., O'Connor,T. and Blackman,M.J.<br>Expression of recombinant Plasmodium falciparum subtilisin-like protease-1 in insect cells. Characterization, comparison with the parasite protease, and homology modeling<br>J Biol Chem (16-8-2002) 277, 29698-29709. PubMed  Europe PubMed DOI  E
    52. 2000
  52. Blackman,M.J.<br>Proteases involved in erythrocyte invasion by the malaria parasite: function and potential as chemotherapeutic targets<br>Curr Drug Targets (2000) 1, 59-83. PubMed  Europe PubMed
  53. [YEAR:7-1-2000]Sajid,M., Withers-Martinez,C. and Blackman,M.J.<br>Maturation and specificity of Plasmodium falciparum subtilisin-like protease-1, a malaria merozoite subtilisin-like serine protease<br>J Biol Chem (7-1-2000) 275, 631-641. PubMed  Europe PubMed DOI
    54. 1999
  54. Withers-Martinez,C., Carpenter,E.P., Hackett,F., Ely,B., Sajid,M., Grainger,M. and Blackman,M.J.<br>PCR-based gene synthesis as an efficient approach for expression of the A+T-rich malaria genome<br>Protein Eng (1999) 12, 1113-1120. PubMed  Europe PubMed
    55. 1998
  55. [YEAR:4-9-1998]Blackman,M.J., Fujioka,H., Stafford,W.H., Sajid,M., Clough,B., Fleck,S.L., Aikawa,M., Grainger,M. and Hackett,F.<br>A subtilisin-like protein in secretory organelles of Plasmodium falciparum merozoites<br>J Biol Chem (4-9-1998) 273, 23398-23409. PubMed  Europe PubMed DOI
    56. 1993
  56. Blackman,M.J., Chappel,J.A., Shai,S. and Holder,A.A.<br>A conserved parasite serine protease processes the Plasmodium falciparum merozoite surface protein-1<br>Mol Biochem Parasitol (1993) 62, 103-114. PubMed  Europe PubMed DOI

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