The University of Queensland

Naturally occurring disulfide-rich cyclic peptides from plants and animals: Synthesis and biosynthesis

de Veer, Simon J. and Craik, David J. (2017). Naturally occurring disulfide-rich cyclic peptides from plants and animals: Synthesis and biosynthesis. Chemical biology of natural products. (pp. 491-529) edited by David J. Newman, Gordon M. Cragg and Paul Grothaus. Boca Raton, FL United States: CRC Press. doi: 10.1201/9781315117089-14

Natural, engineered and synthetic inhibitors of kallikrein-related peptidases

Swedberg, Joakim E., de Veer, Simon J. and Harris, Jonathan M. (2012). Natural, engineered and synthetic inhibitors of kallikrein-related peptidases. Kallikrein-related peptidases: characterization, regulation, and interactions within the protease web. (pp. 141-160) edited by Viktor Magdolen. Berlin, Germany: De Gruyter.

Tertiary amide bond formation by an engineered asparaginyl ligase

de Veer, Simon J., Zhou, Yan, Durek, Thomas, Craik, David J. and Rehm, Fabian B. H. (2024). Tertiary amide bond formation by an engineered asparaginyl ligase. Chemical Science, 15 (14), 5248-5255. doi: 10.1039/d3sc06352f

Nucleation of a key beta-turn promotes cyclotide oxidative folding

Tian, Sixin, de Veer, Simon J., Durek, Thomas, Wang, Conan K. and Craik, David J. (2024). Nucleation of a key beta-turn promotes cyclotide oxidative folding. Journal of Biological Chemistry, 300 (4) 107125, 107125. doi: 10.1016/j.jbc.2024.107125

Engineering the cyclization loop of MCoTI-II generates targeted cyclotides that potently inhibit factor XIIa

Tian, Sixin, Durek, Thomas, Wang, Conan K., Zdenek, Christina N., Fry, Bryan G., Craik, David J. and de Veer, Simon J. (2022). Engineering the cyclization loop of MCoTI-II generates targeted cyclotides that potently inhibit factor XIIa. Journal of Medicinal Chemistry, 65 (23), 15698-15709. doi: 10.1021/acs.jmedchem.2c01080

Cystine knot peptides with tuneable activity and mechanism

Li, Choi Yi, Rehm, Fabian B. H., Yap, Kuok, Zdenek, Christina N., Harding, Maxim D., Fry, Bryan G., Durek, Thomas, Craik, David J. and Veer, Simon J. (2022). Cystine knot peptides with tuneable activity and mechanism. Angewandte Chemie, 61 (19) e202200951, e202200951. doi: 10.1002/ange.202200951

Enzymatic C‐to‐C Protein Ligation

Rehm, Fabian B. H., Tyler, Tristan J., Veer, Simon J., Craik, David J. and Durek, Thomas (2022). Enzymatic C‐to‐C Protein Ligation. Angewandte Chemie International Edition, 134 (11) e202116672, e202116672. doi: 10.1002/anie.202116672

Towards a generic prototyping approach for therapeutically-relevant peptides and proteins in a cell-free translation system

Wu, Yue, Cui, Zhenling, Huang, Yen-Hua, de Veer, Simon J., Aralov, Andrey V., Guo, Zhong, Moradi, Shayli V., Hinton, Alexandra O., Deuis, Jennifer R., Guo, Shaodong, Chen, Kai-En, Collins, Brett M., Vetter, Irina, Herzig, Volker, Jones, Alun, Cooper, Matthew A., King, Glenn F., Craik, David J., Alexandrov, Kirill and Mureev, Sergey (2022). Towards a generic prototyping approach for therapeutically-relevant peptides and proteins in a cell-free translation system. Nature Communications, 13 (1) 260, 260. doi: 10.1038/s41467-021-27854-9

Enzymatic C-terminal protein engineering with amines

Rehm, Fabian B. H., Tyler, Tristan J., Yap, Kuok, de Veer, Simon J., Craik, David J. and Durek, Thomas (2021). Enzymatic C-terminal protein engineering with amines. Journal of the American Chemical Society, 143 (46) jacs.1c08976, 19498-19504. doi: 10.1021/jacs.1c08976

An ultrapotent and selective cyclic peptide inhibitor of human β-factor XIIa in a cyclotide scaffold

Liu, Wenyu, de Veer, Simon J., Huang, Yen-Hua, Sengoku, Toru, Okada, Chikako, Ogata, Kazuhiro, Zdenek, Christina N., Fry, Bryan G., Swedberg, Joakim E., Passioura, Toby, Craik, David J. and Suga, Hiroaki (2021). An ultrapotent and selective cyclic peptide inhibitor of human β-factor XIIa in a cyclotide scaffold. Journal of the American Chemical Society, 143 (44) jacs.1c07574, 18481-18489. doi: 10.1021/jacs.1c07574

Melanocortin 1 receptor agonists based on a bivalent, bicyclic peptide framework

Durek, Thomas, Kaas, Quentin, White, Andrew M., Weidmann, Joachim, Fuaad, Abdullah Ahmad, Cheneval, Olivier, Schroeder, Christina I., de Veer, Simon J., Dellsén, Anita, Österlund, Torben, Larsson, Niklas, Knerr, Laurent, Bauer, Udo, Plowright, Alleyn T. and Craik, David J. (2021). Melanocortin 1 receptor agonists based on a bivalent, bicyclic peptide framework. Journal of Medicinal Chemistry, 64 (14) acs.jmedchem.1c00095, 9906-9915. doi: 10.1021/acs.jmedchem.1c00095

Yeast-based bioproduction of disulfide-rich peptides and their cyclization via asparaginyl endopeptidases

Yap, Kuok, Du, Junqiao, Rehm, Fabian B. H., Tang, Shyn Ric, Zhou, Yan, Xie, Jing, Wang, Conan K., de Veer, Simon J., Lua, Linda H. L., Durek, Thomas and Craik, David J. (2021). Yeast-based bioproduction of disulfide-rich peptides and their cyclization via asparaginyl endopeptidases. Nature Protocols, 16 (3), 1-23. doi: 10.1038/s41596-020-00483-0

Der Sonnenblumen‐Trypsin‐Inhibitor 1 (SFTI‐1) in der Chemie und Biologie

Veer, Simon J., White, Andrew M. and Craik, David J. (2020). Der Sonnenblumen‐Trypsin‐Inhibitor 1 (SFTI‐1) in der Chemie und Biologie. Angewandte Chemie, 133 (15), 8128-8151. doi: 10.1002/ange.202006919

Sunflower trypsin inhibitor-1 (SFTI-1): sowing seeds in the fields of chemistry and biology

de Veer, Simon J., White, Andrew M. and Craik, David (2020). Sunflower trypsin inhibitor-1 (SFTI-1): sowing seeds in the fields of chemistry and biology. Angewandte Chemie (International Edition), 59 (15), 2-24. doi: 10.1002/anie.202006919

An environmentally sustainable biomimetic production of cyclic disulfide-rich peptides

Yap, Kuok, Du, Junqiao, Looi, Fong Yang, Tang, Shyn Ric, de Veer, Simon J., Bony, Anuja R., Rehm, Fabian B. H., Xie, Jing, Chan, Lai Yue, Wang, Conan K., Adams, David J., Lua, Linda H. L., Durek, Thomas and Craik, David J. (2020). An environmentally sustainable biomimetic production of cyclic disulfide-rich peptides. Green Chemistry, 22 (15), 5002-5016. doi: 10.1039/d0gc01366h

Innentitelbild: Application and Structural Analysis of Triazole‐Bridged Disulfide Mimetics in Cyclic Peptides (Angew. Chem. 28/2020)

White, Andrew M., Veer, Simon J., Wu, Guojie, Harvey, Peta J., Yap, Kuok, King, Gordon J., Swedberg, Joakim E., Wang, Conan K., Law, Ruby H. P., Durek, Thomas and Craik, David J. (2020). Innentitelbild: Application and Structural Analysis of Triazole‐Bridged Disulfide Mimetics in Cyclic Peptides (Angew. Chem. 28/2020). Angewandte Chemie, 132 (28), 11258-11258. doi: 10.1002/ange.202006713

Inside Cover: Application and Structural Analysis of Triazole‐Bridged Disulfide Mimetics in Cyclic Peptides (Angew. Chem. Int. Ed. 28/2020)

White, Andrew M., Veer, Simon J., Wu, Guojie, Harvey, Peta J., Yap, Kuok, King, Gordon J., Swedberg, Joakim E., Wang, Conan K., Law, Ruby H. P., Durek, Thomas and Craik, David J. (2020). Inside Cover: Application and Structural Analysis of Triazole‐Bridged Disulfide Mimetics in Cyclic Peptides (Angew. Chem. Int. Ed. 28/2020). Angewandte Chemie International Edition, 59 (28), 11162-11162. doi: 10.1002/anie.202006713

Application and structural analysis of triazole‐bridged disulfide mimetics in cyclic peptides

White, Andrew M., Veer, Simon J., Wu, Guojie, Harvey, Peta J., Yap, Kuok, King, Gordon J., Swedberg, Joakim E., Wang, Conan K., Law, Ruby H. P., Durek, Thomas and Craik, David J. (2020). Application and structural analysis of triazole‐bridged disulfide mimetics in cyclic peptides. Angewandte Chemie International Edition, 132 (28) anie.202003435, 11369-11373. doi: 10.1002/anie.202003435

Binding loop substitutions in the cyclic peptide SFTI-1 generate potent and selective chymase inhibitors

Li, Choi Yi, Yap, Kuok, Swedberg, Joakim E., Craik, David J. and de Veer, Simon J. (2020). Binding loop substitutions in the cyclic peptide SFTI-1 generate potent and selective chymase inhibitors. Journal of Medicinal Chemistry, 63 (2) acs.jmedchem.9b01811, 816-826. doi: 10.1021/acs.jmedchem.9b01811

Cyclotides: from structure to function

de Veer, Simon J., Kan, Meng-Wei and Craik, David J. (2019). Cyclotides: from structure to function. Chemical Reviews, 119 (24) acs.chemrev.9b00402, 12375-12421. doi: 10.1021/acs.chemrev.9b00402

Iterative optimization of the cyclic peptide SFTI-1 yields potent inhibitors of neutrophil proteinase 3

Tian, Sixin, Swedberg, Joakim E., Li, Choi Yi, Craik, David J. and de Veer, Simon J. (2019). Iterative optimization of the cyclic peptide SFTI-1 yields potent inhibitors of neutrophil proteinase 3. ACS Medicinal Chemistry Letters, 10 (8) acsmedchemlett.9b00253, 1234-1239. doi: 10.1021/acsmedchemlett.9b00253

KLK4 inhibition by cyclic and acyclic peptides: structural and dynamical insights into standard-mechanism protease inhibitors

Riley, Blake T., Ilyichova, Olga, de Veer, Simon J., Swedberg, Joakim E., Wilson, Emily, Hoke, David E., Harris, Jonathan M. and Buckle, Ashley M. (2019). KLK4 inhibition by cyclic and acyclic peptides: structural and dynamical insights into standard-mechanism protease inhibitors. Biochemistry, 58 (21), 2524-2533. doi: 10.1021/acs.biochem.9b00191

Amino acid scanning at P5′ within the Bowman–Birk inhibitory loop reveals specificity trends for diverse serine proteases

Li, Choi Yi, de Veer, Simon J., White, Andrew M., Chen, Xingchen, Harris, Jonathan M., Swedberg, Joakim E. and Craik, David J. (2019). Amino acid scanning at P5′ within the Bowman–Birk inhibitory loop reveals specificity trends for diverse serine proteases. Journal of Medicinal Chemistry, 62 (7), 3696-3706. doi: 10.1021/acs.jmedchem.9b00211

Potent, multi-target serine protease inhibition achieved by a simplified β-sheet motif

Chen, Xingchen, Riley, Blake T., De Veer, Simon J., Hoke, David E., Van Haeften, Jessica, Leahy, Darren, Swedberg, Joakim E., Brattsand, Maria, Hartfield, Perry J., Buckle, Ashley M. and Harris, Jonathan M. (2019). Potent, multi-target serine protease inhibition achieved by a simplified β-sheet motif. PLoS ONE, 14 (1) e0210842, e0210842. doi: 10.1371/journal.pone.0210842

Characterising the subsite specificity of urokinase-type plasminogen activator and tissue-type plasminogen activator using a sequence-defined peptide aldehyde library

Li, Choi Yi, de Veer, Simon J., Law, Ruby H. P., Whisstock, James C., Craik, David J. and Swedberg, Joakim E. (2019). Characterising the subsite specificity of urokinase-type plasminogen activator and tissue-type plasminogen activator using a sequence-defined peptide aldehyde library. ChemBioChem, 19 (1), 46-50. doi: 10.1002/cbic.201800395

Potent, selective, and cell-penetrating inhibitors of Kallikrein-related peptidase 4 based on the cyclic peptide MCoTI-II

Swedberg, Joakim E., Ghani, Hafiza Abdul, Harris, Jonathan M., de Veer, Simon J. and Craik, David J. (2018). Potent, selective, and cell-penetrating inhibitors of Kallikrein-related peptidase 4 based on the cyclic peptide MCoTI-II. ACS Medicinal Chemistry Letters, 9 (12) acsmedchemlett.8b00422, 1258-1262. doi: 10.1021/acsmedchemlett.8b00422

Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1

de Veer, Simon J., Li, Choi Yi, Swedberg, Joakim E., Schroeder, Christina I. and Craik, David J. (2018). Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1. European Journal of Medicinal Chemistry, 155, 695-704. doi: 10.1016/j.ejmech.2018.06.029

Kallikrein-related peptidase 5 contributes to H3N2 influenza virus infection in human lungs

Magnen, Melia, Gueugnon, Fabien, Guillon, Antoine, Baranek, Thomas, Thibault, Virginie C., Petit-Courty, Agnes, de Veer, Simon J., Harris, Jonathan, Humbles, Alison A., Si-Tahar, Mustapha and Courty, Yves (2017). Kallikrein-related peptidase 5 contributes to H3N2 influenza virus infection in human lungs. Journal of Virology, 91 (16) e00421-17. doi: 10.1128/JVI.00421-17

Cyclotides as tools in chemical biology

de Veer, Simon J., Weidmann, Joachim and Craik, David J. (2017). Cyclotides as tools in chemical biology. Accounts of Chemical Research, 50 (7), 1557-1565. doi: 10.1021/acs.accounts.7b00157

Selective substrates and inhibitors for kallikrein-related peptidase 7 (KLK7) shed light on KLK proteolytic activity in the stratum corneum

de Veer, Simon J., Furio, Laetitia, Swedberg, Joakim E., Munro, Christopher A., Brattsand, Maria, Clements, Judith A., Hovnanian, Alain and Harris, Jonathan M. (2017). Selective substrates and inhibitors for kallikrein-related peptidase 7 (KLK7) shed light on KLK proteolytic activity in the stratum corneum. The Journal of Investigative Dermatology, 137 (2), 430-439. doi: 10.1016/j.jid.2016.09.017

Design of potent and selective cathepsin G inhibitors based on the sunflower trypsin inhibitor-1 scaffold

Swedberg, Joakim E., Li, Choi Yi, De Veer, Simon J., Wang, Conan K. and Craik, David J. (2017). Design of potent and selective cathepsin G inhibitors based on the sunflower trypsin inhibitor-1 scaffold. Journal of Medicinal Chemistry, 60 (2), 658-667. doi: 10.1021/acs.jmedchem.6b01509

Attenuated kallikrein-related peptidase activity disrupts desquamation and leads to stratum corneum thickening in human skin equivalent models

McGovern, J. A., Meinert, C., de Veer, S. J., Hollier, B. G., Parker, T. J. and Upton, Z. (2017). Attenuated kallikrein-related peptidase activity disrupts desquamation and leads to stratum corneum thickening in human skin equivalent models. British Journal of Dermatology, 176 (1), 145-158. doi: 10.1111/bjd.14879

Exploring the active site binding specificity of kallikrein-related peptidase 5 (KLK5) guides the design of new peptide substrates and inhibitors

De Veer, Simon J., Swedberg, Joakim E., Brattsand, Maria, Clements, Judith A. and Harris, Jonathan M. (2016). Exploring the active site binding specificity of kallikrein-related peptidase 5 (KLK5) guides the design of new peptide substrates and inhibitors. Biological Chemistry, 397 (12), 1237-1249. doi: 10.1515/hsz-2016-0112

Direct and indirect mechanisms of KLK4 inhibition revealed by structure and dynamics

Riley, Blake T., Ilyichova, Olga, Costa, Mauricio G. S., Porebski, Benjamin T., De Veer, Simon J., Swedberg, Joakim E., Kass, Itamar, Harris, Jonathan M., Hoke, David E. and Buckle, Ashley M. (2016). Direct and indirect mechanisms of KLK4 inhibition revealed by structure and dynamics. Scientific Reports, 6 (1) 35385, 35385. doi: 10.1038/srep35385

Substrate-guided design of selective FXIIa inhibitors based on the plant-derived Momordica cochinchinensis trypsin inhibitor-II (MCoTI-II) scaffold

Swedberg, Joakim E., Mahatmanto, Tunjung, Ghani, Hafiza Abdul, de Veer, Simon J., Schroeder, Christina I., Harris, Jonathan M. and Craik, David J. (2016). Substrate-guided design of selective FXIIa inhibitors based on the plant-derived Momordica cochinchinensis trypsin inhibitor-II (MCoTI-II) scaffold. Journal of Medicinal Chemistry, 59 (15), 7287-7292. doi: 10.1021/acs.jmedchem.6b00557

Improving the selectivity of engineered protease inhibitors: optimizing the P2 prime residue using a versatile cyclic peptide library

de Veer, Simon J., Wang, Conan, Harris, Jonathan M., Craik, David J. and Swedberg, Joakim E. (2015). Improving the selectivity of engineered protease inhibitors: optimizing the P2 prime residue using a versatile cyclic peptide library. Journal of Medicinal Chemistry, 58 (20), 8257-8268. doi: 10.1021/acs.jmedchem.5b01148

Engineered protease inhibitors based on sunflower trypsin inhibitor-1 (SFTI-1) provide insights into the role of sequence and conformation in Laskowski mechanism inhibition

de Veer, Simon J., Swedberg, Joakim E., Akcan, Muharrem, Rosengren, K. Johan, Brattsand, Maria, Craik, David J. and Harris, Jonathan M. (2015). Engineered protease inhibitors based on sunflower trypsin inhibitor-1 (SFTI-1) provide insights into the role of sequence and conformation in Laskowski mechanism inhibition. Biochemical Journal, 469 (2), 243-253. doi: 10.1042/BJ20150412

Olmsted syndrome with erythromelalgia caused by recessive TRPV3 mutations

Duchatelet, S., Guibbal, L., de Veer, S., Fraitag, S., Nitschké, P., Zarhrate, M., Bodemer, C. and Hovnanian, A. (2014). Olmsted syndrome with erythromelalgia caused by recessive TRPV3 mutations. British Journal of Dermatology, 171 (3), 675-678. doi: 10.1111/bjd.12951

Proteases and proteomics: cutting to the core of human skin pathologies

de Veer, Simon J., Furio, Laetitia, Harris, Jonathan M. and Hovnanian, Alain (2014). Proteases and proteomics: cutting to the core of human skin pathologies. Proteomics - Clinical Applications, 8 (5-6), 389-402. doi: 10.1002/prca.201300081

A new TRPV3 missense mutation in a patient with Olmsted syndrome and erythromelalgia

Duchatelet, Sabine, Pruvost, Solenn, de Veer, Simon, Fraitag, Sylvie, Nitschké, Patrick, Bole-Feysot, Christine, Bodemer, Christine and Hovnanian, Alain (2014). A new TRPV3 missense mutation in a patient with Olmsted syndrome and erythromelalgia. JAMA Dermatology, 150 (3), 303-306. doi: 10.1001/jamadermatol.2013.8709

Proteases: common culprits in human skin disorders

de Veer, Simon J., Furio, Laetitia, Harris, Jonathan M. and Hovnanian, Alain (2014). Proteases: common culprits in human skin disorders. Trends in Molecular Medicine, 20 (3), 166-178. doi: 10.1016/j.molmed.2013.11.005

Transgenic kallikrein 5 mice reproduce major cutaneous and systemic hallmarks of Netherton syndrome

Furio, Laetitia, de Veer, Simon, Jaillet, Madeleine, Briot, Anais, Robin, Aurelie, Deraison, Celine and Hovnanian, Alain (2014). Transgenic kallikrein 5 mice reproduce major cutaneous and systemic hallmarks of Netherton syndrome. The Journal of Experimental Medicine, 211 (3), 499-513. doi: 10.1084/jem.20131797

Mechanism-based selection of a potent kallikrein-related peptidase 7 inhibitor from a versatile library based on the sunflower trypsin inhibitor SFTI-1

de Veer, Simon J., Ukolova, Svetlana S., Munro, Christopher A., Swedberg, Joakim E., Buckle, Ashley M. and Harris, Jonathan M. (2013). Mechanism-based selection of a potent kallikrein-related peptidase 7 inhibitor from a versatile library based on the sunflower trypsin inhibitor SFTI-1. Biopolymers, 100 (5), 510-518. doi: 10.1002/bip.22231

Selective cleavage of human sex hormone-binding globulin by kallikrein-related peptidases and effects on androgen action in LNCaP prostate cancer cells

Sanchez, Washington Y., de Veer, Simon J., Swedberg, Joakim E., Hong, Eui-Ju, Reid, Janet C., Walsh, Terry P., Hooper, John D., Hammond, Geoffrey L., Clements, Judith A. and Harris, Jonathan M. (2012). Selective cleavage of human sex hormone-binding globulin by kallikrein-related peptidases and effects on androgen action in LNCaP prostate cancer cells. Endocrinology, 153 (7), 3179-3189. doi: 10.1210/en.2012-1011

Mastering the canonical loop of serine protease inhibitors: Enhancing potency by optimising the internal hydrogen bond network

Swedberg, Joakim, de Veer, Simon J., Sit, Kei C., Reboul, Cyril F., Buckle, Ashley M. and Harris, Jonathan M. (2011). Mastering the canonical loop of serine protease inhibitors: Enhancing potency by optimising the internal hydrogen bond network. PLoS One, 6 (4) e19302, e19302.1-e19302.11. doi: 10.1371/journal.pone.0019302

Substrate-guided design of a potent and selective kallikrein-related peptidase inhibitor for kallikrein 4

Swedberg, Joakim E., Nigon, Laura V., Reid, Janet C., de Veer, Simon J., Walpole, Carina M., Stephens, Carson R., Walsh, Terry P., Takayama, Thomas K., Hooper, John D., Clements, Judith A., Buckle, Ashley M. and Harris, Jonathan M. (2009). Substrate-guided design of a potent and selective kallikrein-related peptidase inhibitor for kallikrein 4. Chemistry and Biology, 16 (6), 633-643. doi: 10.1016/j.chembiol.2009.05.008

Dominant and recessive Olmsted syndrome with erythromelalgia due to TRPV3 mutations

Duchatelet, S., de Veer, S., Guibbal, L., Freitag, S., Nitschke, P., Bole-Feysot, C., Bodemers, C. and Hovnanian, A. (2014). Dominant and recessive Olmsted syndrome with erythromelalgia due to TRPV3 mutations. 44th Annual Meeting of the European-Society-for-Dermatological-Research (ESDR), Copenhagen Denmark, Sep 10-13, 2014. NEW YORK: NATURE PUBLISHING GROUP.

Non-combinatorial library screening reveals subsite cooperativity and identifies new high-efficiency substrates for kallikrein-related peptidase 14

de Veer, Simon J., Swedberg, Joakim E., Parker, Edward A. and Harris, Jonathan M. (2012). Non-combinatorial library screening reveals subsite cooperativity and identifies new high-efficiency substrates for kallikrein-related peptidase 14. *, *, *. Berlin, Germany: Walter de Gruyter. doi: 10.1515/BC-2011-250

Natural and engineered kallikrein inhibitors: An emerging pharmacopeia

Swedberg, Joakim E., de Veer, Simon J. and Harris, Jonathan M. (2010). Natural and engineered kallikrein inhibitors: An emerging pharmacopeia. IKS 2009: 3rd International Symposium on Kallikreins and Kallikrein-Related Peptidases, Munich, Germany, 30 August-2 September 2009. Berlin, Germany: Walter de Gruyter. doi: 10.1515/BC.2010.037