The University of Queensland

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

Sortase‐Catalyzed Protein Domain Inversion

Zhou, Yan, Durek, Thomas, Craik, David J. and Rehm, Fabian B. H. (2024). Sortase‐Catalyzed Protein Domain Inversion. Angewandte Chemie, 136 (14). doi: 10.1002/ange.202316777

Sortase‐Catalyzed Protein Domain Inversion

Zhou, Yan, Durek, Thomas, Craik, David J. and Rehm, Fabian B. H. (2024). Sortase‐Catalyzed Protein Domain Inversion. Angewandte Chemie International Edition, 63 (14) e202316777, 1-7. doi: 10.1002/anie.202316777

Development of melanocortin 4 receptor agonists by exploiting animal-derived macrocyclic, disulfide-rich peptide scaffolds

Muratspahić, Edin, Aslanoglou, Despoina, White, Andrew M., Draxler, Claudia, Kozisek, Xaver, Farooq, Zara, Craik, David J., McCormick, Peter J., Durek, Thomas and Gruber, Christian W. (2023). Development of melanocortin 4 receptor agonists by exploiting animal-derived macrocyclic, disulfide-rich peptide scaffolds. ACS Pharmacology and Translational Science, 6 (10), 1373-1381. doi: 10.1021/acsptsci.3c00090

A Chemoenzymatic Approach To Produce a Cyclic Analogue of the Analgesic Drug MVIIA (Ziconotide)

Zhou, Yan, Harvey, Peta J., Koehbach, Johannes, Chan, Lai Yue, Jones, Alun, Andersson, Åsa, Vetter, Irina, Durek, Thomas and Craik, David J. (2023). A Chemoenzymatic Approach To Produce a Cyclic Analogue of the Analgesic Drug MVIIA (Ziconotide). Angewandte Chemie, 135 (29). doi: 10.1002/ange.202302812

A chemo-enzymatic approach to produce a cyclic analogue of the analgesic drug MVIIA (Ziconotide)

Zhou, Yan, Harvey, Peta J., Koehbach, Johannes, Chan, Lai Yue, Jones, Alun, Andersson, Åsa, Vetter, Irina, Durek, Thomas and Craik, David J. (2023). A chemo-enzymatic approach to produce a cyclic analogue of the analgesic drug MVIIA (Ziconotide). Angewandte Chemie, 62 (29) e202302812, e202302812. doi: 10.1002/anie.202302812

Pain-causing stinging nettle toxins target TMEM233 to modulate NaV1.7 function

Jami, Sina, Deuis, Jennifer R., Klasfauseweh, Tabea, Cheng, Xiaoyang, Kurdyukov, Sergey, Chung, Felicity, Okorokov, Andrei L., Li, Shengnan, Zhang, Jiangtao, Cristofori-Armstrong, Ben, Israel, Mathilde R., Ju, Robert J., Robinson, Samuel D., Zhao, Peng, Ragnarsson, Lotten, Andersson, Åsa, Tran, Poanna, Schendel, Vanessa, McMahon, Kirsten L., Tran, Hue N. T., Chin, Yanni K.-Y., Zhu, Yifei, Liu, Junyu, Crawford, Theo, Purushothamvasan, Saipriyaa, Habib, Abdella M., Andersson, David A., Rash, Lachlan D., Wood, John N. ... Vetter, Irina (2023). Pain-causing stinging nettle toxins target TMEM233 to modulate NaV1.7 function. Nature Communications, 14 (1) 2442. doi: 10.1038/s41467-023-37963-2

Native and engineered cyclic disulfide-rich peptides as drug leads

Tyler, Tristan J., Durek, Thomas and Craik, David J. (2023). Native and engineered cyclic disulfide-rich peptides as drug leads. Molecules, 28 (7) 3189, 1-22. doi: 10.3390/molecules28073189

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

Late-stage functionalization with cysteine staples generates potent and selective melanocortin receptor-1 agonists

White, Andrew M., Dellsén, Anita, Larsson, Niklas, Kaas, Quentin, Jansen, Frank, Plowright, Alleyn T., Knerr, Laurent, Durek, Thomas and Craik, David J. (2022). Late-stage functionalization with cysteine staples generates potent and selective melanocortin receptor-1 agonists. Journal of Medicinal Chemistry, 65 (19), 12956-12969. doi: 10.1021/acs.jmedchem.2c00793

Neurotoxic and cytotoxic peptides underlie the painful stings of the tree nettle Urtica ferox

Xie, Jing, Robinson, Samuel D., Gilding, Edward K., Jami, Sina, Deuis, Jennifer R., Rehm, Fabian B.H., Yap, Kuok, Ragnarsson, Lotten, Chan, Lai Yue, Hamilton, Brett R., Harvey, Peta J., Craik, David J., Vetter, Irina and Durek, Thomas (2022). Neurotoxic and cytotoxic peptides underlie the painful stings of the tree nettle Urtica ferox. Journal of Biological Chemistry, 298 (8) 102218, 1-12. doi: 10.1016/j.jbc.2022.102218

Low potency inhibition of NaV1.7 by externally applied QX-314 via a depolarizing shift in the voltage-dependence of activation

Klasfauseweh, Tabea, Israel, Mathilde R., Ragnarsson, Lotten, Cox, James J., Durek, Thomas, Carter, David A., Leffler, Andreas, Vetter, Irina and Deuis, Jennifer R. (2022). Low potency inhibition of NaV1.7 by externally applied QX-314 via a depolarizing shift in the voltage-dependence of activation. European Journal of Pharmacology, 925 175013, 175013. doi: 10.1016/j.ejphar.2022.175013

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

Phage display-based discovery of cyclic peptides against the broad spectrum bacterial anti-virulence target CsrA

Jakob, Valentin, Zoller, Ben G. E., Rinkes, Julia, Wu, Yingwen, Kiefer, Alexander F., Hust, Michael, Polten, Saskia, White, Andrew M., Harvey, Peta J., Durek, Thomas, Craik, David J., Siebert, Andreas, Kazmaier, Uli and Empting, Martin (2022). Phage display-based discovery of cyclic peptides against the broad spectrum bacterial anti-virulence target CsrA. European Journal of Medicinal Chemistry, 231 114148, 114148. doi: 10.1016/j.ejmech.2022.114148

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

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

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

Asparaginyl ligases: new enzymes for the protein engineer's toolbox

Rehm, Fabian B. H., Tyler, Tristan J., Xie, Jing, Yap, Kuok, Durek, Thomas and Craik, David J. (2021). Asparaginyl ligases: new enzymes for the protein engineer's toolbox. ChemBioChem, 22 (12), 2079-2086. doi: 10.1002/cbic.202100071

Effects of backbone cyclization on the pharmacokinetics and drug efficiency of the orally active analgesic conotoxin cVc1.1

Poth, Aaron G., Chiu, Francis C.K., Stalmans, Sofie, Hamilton, Brett R., Huang, Yen-Hua, Shackleford, David M., Patil, Rahul, Le, Thao T., Kan, Meng-Wei, Durek, Thomas, Wynendaele, Evelien, De Spiegeleer, Bart, Powell, Andrew K., Venter, Deon J., Clark, Richard J., Charman, Susan A. and Craik, David J. (2021). Effects of backbone cyclization on the pharmacokinetics and drug efficiency of the orally active analgesic conotoxin cVc1.1. Medicine in Drug Discovery, 10 100087, 1-10. doi: 10.1016/j.medidd.2021.100087

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

Improved asparaginyl‐ligase‐catalyzed transpeptidation via selective nucleophile quenching

Rehm, Fabian B. H., Tyler, Tristan J., Yap, Kuok, Durek, Thomas and Craik, David J. (2020). Improved asparaginyl‐ligase‐catalyzed transpeptidation via selective nucleophile quenching. Angewandte Chemie, 133 (8) ange.202013584, 4050-4054. doi: 10.1002/ange.202013584

Make it or break it: plant AEPs on stage in biotechnology

Jackson, Mark A., Nguyen, Linh T. T., Gilding, Edward K., Durek, Thomas and Craik, David J. (2020). Make it or break it: plant AEPs on stage in biotechnology. Biotechnology Advances, 45 107651, 107651. doi: 10.1016/j.biotechadv.2020.107651

Two for the price of one: heterobivalent ligand design targeting two binding sites on voltage-gated sodium channels slows ligand dissociation and enhances otency

Peschel, Alicia, Cardoso, Fernanda C., Walker, Andrew A., Durek, Thomas, Stone, M Rhia L., Braga Emidio, Nayara, Dawson, Philip E., Muttenthaler, Markus and King, Glenn F. (2020). Two for the price of one: heterobivalent ligand design targeting two binding sites on voltage-gated sodium channels slows ligand dissociation and enhances otency. Journal of Medicinal Chemistry, 63 (21), 12773-12785. doi: 10.1021/acs.jmedchem.0c01107

Neurotoxic peptides from the venom of the giant Australian stinging tree

Gilding, Edward K., Jami, Sina, Deuis, Jennifer R., Israel, Mathilde R., Harvey, Peta J., Poth, Aaron G., Rehm, Fabian B. H., Stow, Jennifer L., Robinson, Samuel D., Yap, Kuok, Brown, Darren L., Hamilton, Brett R., Andersson, David, Craik, David J., Vetter, Irina and Durek, Thomas (2020). Neurotoxic peptides from the venom of the giant Australian stinging tree. Science Advances, 6 (38) eabb8828, 1-10. doi: 10.1126/sciadv.abb8828

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

Characterization of synthetic Tf2 as a NaV1.3 selective pharmacological probe

Israel, Mathilde R., Dash, Thomas S., Bothe, Stefanie N., Robinson, Samuel D., Deuis, Jennifer R., Craik, David J., Lampert, Angelika, Vetter, Irina and Durek, Thomas (2020). Characterization of synthetic Tf2 as a NaV1.3 selective pharmacological probe. Biomedicines, 8 (6) 155, 155. doi: 10.3390/biomedicines8060155

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

A bifunctional asparaginyl endopeptidase efficiently catalyzes both cleavage and cyclization of cyclic trypsin inhibitors

Du, Junqiao, Yap, Kuok, Chan, Lai Yue, Rehm, Fabian B. H., Looi, Fong Yang, Poth, Aaron G., Gilding, Edward K., Kaas, Quentin, Durek, Thomas and Craik, David J. (2020). A bifunctional asparaginyl endopeptidase efficiently catalyzes both cleavage and cyclization of cyclic trypsin inhibitors. Nature Communications, 11 (1) 1575, 1-11. doi: 10.1038/s41467-020-15418-2

Potent thiophene antagonists of human complement C3a receptor with anti-inflammatory activity

Rowley, Jessica A., Reid, Robert C., Poon, Eunice K. Y., Wu, Kai-Chen, Lim, Junxian, Lohman, Rink-Jan, Hamidon, Johan K., Yau, Mei-Kwan, Halili, Maria A., Durek, Thomas, Iyer, Abishek and Fairlie, David P. (2020). Potent thiophene antagonists of human complement C3a receptor with anti-inflammatory activity. Journal of Medicinal Chemistry, 63 (2) acs.jmedchem.9b00927, 529-541. doi: 10.1021/acs.jmedchem.9b00927

Site-specific sequential protein labeling catalyzed by a single recombinant ligase

Rehm, Fabian B. H., Harmand, Thibault J., Yap, Kuok, Durek, Thomas, Craik, David J. and Ploegh, Hidde L. (2019). Site-specific sequential protein labeling catalyzed by a single recombinant ligase. Journal of the American Chemical Society, 141 (43) jacs.9b09166, 17388-17393. doi: 10.1021/jacs.9b09166

A suite of kinetically superior AEP ligases can cyclise an intrinsically disordered protein

Harris, Karen S., Guarino, Rosemary F., Dissanayake, Ravindu S., Quimbar, Pedro, McCorkelle, Owen C., Poon, Simon, Kaas, Quentin, Durek, Thomas, Gilding, Edward K., Jackson, Mark A., Craik, David J., van der Weerden, Nicole L., Anders, Robin F. and Anderson, Marilyn A. (2019). A suite of kinetically superior AEP ligases can cyclise an intrinsically disordered protein. Scientific Reports, 9 (1) 10820, 10820. doi: 10.1038/s41598-019-47273-7

Rapid and scalable plant-based production of a potent plasmin inhibitor peptide

Jackson, Mark A., Yap, Kuok, Poth, Aaron G., Gilding, Edward K., Swedberg, Joakim E., Poon, Simon, Qu, Haiou, Durek, Thomas, Harris, Karen, Anderson, Marilyn A. and Craik, David J. (2019). Rapid and scalable plant-based production of a potent plasmin inhibitor peptide. Frontiers in Plant Science, 10 602, 602. doi: 10.3389/fpls.2019.00602

NaV1.6 regulates excitability of mechanosensitive sensory neurons

Israel, Mathilde R., Tanaka, Brian S., Castro, Joel, Thongyoo, Panumart, Robinson, Samuel D., Zhao, Peng, Deuis, Jennifer R., Craik, David J., Durek, Thomas, Brierley, Stuart M., Waxman, Stephen G, Dib-Hajj, Sulayman D. and Vetter, Irina (2019). NaV1.6 regulates excitability of mechanosensitive sensory neurons. Journal of Physiology, 597 (14), 3751-3768. doi: 10.1113/JP278148

Papain-like cysteine proteases prepare plant cyclic peptide precursors for cyclization

Rehm, Fabian B. H., Jackson, Mark A., De Geyter, Ewout, Yap, Kuok, Gilding, Edward K., Durek, Thomas and Craik, David J. (2019). Papain-like cysteine proteases prepare plant cyclic peptide precursors for cyclization. Proceedings of the National Academy of Sciences, 116 (16), 7831-7836. doi: 10.1073/pnas.1901807116

A centipede toxin family defines an ancient class of CSαβ defensins

Dash, Thomas S., Shafee, Thomas, Harvey, Peta J., Zhang, Chuchu, Peigneur, Steve, Deuis, Jennifer R., Vetter, Irina, Tytgat, Jan, Anderson, Marilyn A., Craik, David J., Durek, Thomas and Undheim, Eivind A. B. (2019). A centipede toxin family defines an ancient class of CSαβ defensins. Structure, 27 (2), 315-326. doi: 10.1016/j.str.2018.10.022

Highly potent and selective plasmin inhibitors based on the sunflower trypsin inhibitor-1 scaffold attenuate fibrinolysis in plasma

Swedberg, Joakim E., Wu, Guojie, Mahatmanto, Tunjung, Durek, Thomas, Caradoc-Davies, Tom T., Whisstock, James C., Law, Ruby H. P. and Craik, David J. (2019). Highly potent and selective plasmin inhibitors based on the sunflower trypsin inhibitor-1 scaffold attenuate fibrinolysis in plasma. Journal of Medicinal Chemistry, 62 (2), 552-560. doi: 10.1021/acs.jmedchem.8b01139

NMR structure of µ-conotoxin GIIIC: Leucine 18 induces local repacking of the N-terminus resulting in reduced Nav channel potency

Harvey, Peta J., Kurniawan, Nyoman D., Finol-Urdaneta, Rocio K., McArthur, Jeffrey R., Van Lysebetten, Dorien, Dash, Thomas S., Hill, Justine M., Adams, David J., Durek, Thomas and Craik, David J. (2018). NMR structure of µ-conotoxin GIIIC: Leucine 18 induces local repacking of the N-terminus resulting in reduced Nav channel potency. Molecules, 23 (10) molecules23102715, 2715. doi: 10.3390/molecules23102715

Targeted delivery of cyclotides via conjugation to a nanobody

Kwon, Soohyun, Duarte, Joao N., Li, Zeyang, Ling, Jingjing J., Cheneval, Olivier, Durek, Thomas, Schroeder, Christina I., Craik, David J. and Ploegh, Hidde L. (2018). Targeted delivery of cyclotides via conjugation to a nanobody. ACS Chemical Biology, 13 (10), 2973-2980. doi: 10.1021/acschembio.8b00653

Molecular basis for the production of cyclic peptides by plant asparaginyl endopeptidases

Jackson, M. A., Gilding, E. K., Shafee, T., Harris, K. S., Kaas, Q., Poon, S., Yap, K., Jia, H., Guarino, R., Chan, L. Y., Durek, T., Anderson, M. A. and Craik, D. J. (2018). Molecular basis for the production of cyclic peptides by plant asparaginyl endopeptidases. Nature Communications, 9 (1) 2411, 2411. doi: 10.1038/s41467-018-04669-9

Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1

Durek, Thomas, Cromm, Philipp M., White, Andrew M., Schroeder, Christina I., Kaas, Quentin, Weidmann, Joachim, Ahmad Fuaad, Abdullah, Cheneval, Olivier, Harvey, Peta J., Daly, Norelle L., Zhou, Yang, Dellsén, Anita, Österlund, Torben, Larsson, Niklas, Knerr, Laurent, Bauer, Udo, Kessler, Horst, Cai, Minying, Hruby, Victor J., Plowright, Alleyn T. and Craik, David J. (2018). Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. Journal of Medicinal Chemistry, 61 (8), 3674-3684. doi: 10.1021/acs.jmedchem.8b00170

The E15R Point Mutation in Scorpion Toxin Cn2 Uncouples Its Depressant and Excitatory Activities on Human NaV1.6

Israel, Mathilde R., Thongyoo, Panumart, Deuis, Jennifer R., Craik, David J., Vetter, Irina and Durek, Thomas (2018). The E15R Point Mutation in Scorpion Toxin Cn2 Uncouples Its Depressant and Excitatory Activities on Human NaV1.6. Journal of Medicinal Chemistry, 61 (4), 1730-1736. doi: 10.1021/acs.jmedchem.7b01609

Co-expression of a cyclizing asparaginyl endopeptidase enables efficient production of cyclic peptides in planta

Poon, Simon, Harris, Karen S, Jackson, Mark A, McCorkelle, Owen C, Gilding, Edward K, Durek, Thomas, van der Weerden, Nicole L, Craik, David J and Anderson, Marilyn A (2017). Co-expression of a cyclizing asparaginyl endopeptidase enables efficient production of cyclic peptides in planta. Journal of experimental botany, 69 (3), 633-641. doi: 10.1093/jxb/erx422

Interaction of Synthetic Human SLURP-1 with the Nicotinic Acetylcholine Receptors

Durek, Thomas, Shelukhina, Irina V., Tae, Han-Shen, Thongyoo, Panumart, Spirova, Ekaterina N., Kudryavtsev, Denis S., Kasheverov, Igor E., Faure, Grazyna, Corringer, Pierre-Jean, Craik, David J., Adams, David J. and Tsetlin, Victor I. (2017). Interaction of Synthetic Human SLURP-1 with the Nicotinic Acetylcholine Receptors. Scientific Reports, 7 (1) 16606, 16606. doi: 10.1038/s41598-017-16809-0

Europium-labeled synthetic C3a protein as a novel fluorescent probe for human complement C3a receptor

Dantas de Araujo, Aline, Wu, Chongyang, Wu, Kai-Chen, Reid, Robert C., Durek, Thomas, Lim, Junxian and Fairlie, David P. (2017). Europium-labeled synthetic C3a protein as a novel fluorescent probe for human complement C3a receptor. Bioconjugate Chemistry, 28 (6), 1669-1676. doi: 10.1021/acs.bioconjchem.7b00132

The tarantula toxin β/δ-TRTX-Pre1a highlights the importance of the S1-S2 voltage-sensor region for sodium channel subtype selectivity.

Wingerd, Joshua S., Mozar, Christine A., Ussing, Christine A., Murali, Swetha S., Chin, Yanni K. -Y., Cristofori-Armstrong, Ben, Durek, Thomas, Gilchrist, John, Vaughan, Christopher W., Bosmans, Frank, Adams, David J., Lewis, Richard J., Alewood, Paul F., Mobli, Mehdi, Christie, Macdonald J. and Rash, Lachlan D. (2017). The tarantula toxin β/δ-TRTX-Pre1a highlights the importance of the S1-S2 voltage-sensor region for sodium channel subtype selectivity.. Scientific Reports, 7 (1) 974, 974. doi: 10.1038/s41598-017-01129-0

Mapping of voltage sensor positions in resting and inactivated mammalian sodium channels by LRET

Kubota, Tomoya, Durek, Thomas, Dang, Bobo, Finol-Urdaneta, Rocio K., Craik, David J., Kent, Stephen B. H., French, Robert J., Bezanilla, Francisco and Correa, Ana M. (2017). Mapping of voltage sensor positions in resting and inactivated mammalian sodium channels by LRET. Proceedings of the National Academy of Sciences, 114 (10), E1857-E1865. doi: 10.1073/pnas.1700453114

Synthesis and protein engineering applications of cyclotides

Qu, Haiou, Smithies, Bronwyn J. , Durek, Thomas and Craik, David J. (2017). Synthesis and protein engineering applications of cyclotides. Australian Journal of Chemistry, 70 (2), 152-161. doi: 10.1071/CH16589

Combining sense and nonsense codon reassignment for site-selective protein modification with unnatural amino acids

Cui, Zhenling, Mureev, Sergey, Polinkovsky, Mark E., Tnimov, Zakir, Guo, Zhong, Durek, Thomas, Jones, Alun and Alexandrov, Kirill (2016). Combining sense and nonsense codon reassignment for site-selective protein modification with unnatural amino acids. ACS Synthetic Biology, 6 (3), 535-544. doi: 10.1021/acssynbio.6b00245

Isolation of two insecticidal toxins from venom of the Australian theraphosid spider Coremiocnemis tropix

Ikonomopoulou, Maria P., Smith, Jennifer J., Herzig, Volker, Pineda, Sandy S., Dziemborowicz, Sławomir, Er, Sing-Yan, Durek, Thomas, Gilchrist, John, Alewood, Paul F., Nicholson, Graham M., Bosmans, Frank and King, Glenn F. (2016). Isolation of two insecticidal toxins from venom of the Australian theraphosid spider Coremiocnemis tropix. Toxicon, 123, 62-70. doi: 10.1016/j.toxicon.2016.10.013

Nicotiana alata defensin chimeras reveal differences in the mechanism of fungal and tumor cell killing and an enhanced antifungal variant

Bleackley, Mark R., Payne, Jennifer A. E., Hayes, Brigitte M. E, Durek, Thomas, Craik, David J., Shafee, Thomas M. A., Poon, Ivan K. H., Hulett, Mark D., Van Der Weerden, Nicole L. and Anderson, Marilyn A. (2016). Nicotiana alata defensin chimeras reveal differences in the mechanism of fungal and tumor cell killing and an enhanced antifungal variant. Antimicrobial Agents and Chemotherapy, 60 (10), 6302-6312. doi: 10.1128/AAC.01479-16

Constrained cyclic peptides as immunomodulatory inhibitors of the CD2:CD58 protein-protein interaction

Sable, Rushikesh, Durek, Thomas, Taneja, Veena, Craik, David J., Pallerla, Sandeep, Gauthier, Ted and Jois, Seetharama (2016). Constrained cyclic peptides as immunomodulatory inhibitors of the CD2:CD58 protein-protein interaction. ACS Chemical Biology, 11 (8), 2366-2374. doi: 10.1021/acschembio.6b00486

Analgesic effects of GpTx-1, PF-04856264 and CNV1014802 in a mouse model of NaV1.7-Mediated pain

Deuis, Jennifer R., Wingerd, Joshua S., Winter, Zoltan, Durek, Thomas, Dekan, Zoltan, Sousa, Silmara R., Zimmermann, Katharina, Hoffmann, Tali, Weidner, Christian, Nassar, Mohammed A., Alewood, Paul F., Lewis, Richard J. and Vetter, Irina (2016). Analgesic effects of GpTx-1, PF-04856264 and CNV1014802 in a mouse model of NaV1.7-Mediated pain. Toxins, 8 (3) 78, 78. doi: 10.3390/toxins8030078

Modulation of human Nav1.7 channel gating by synthetic alpha-scorpion toxin OD1 and its analogs

Motin, Leonid, Durek, Thomas and Adams, David J. (2016). Modulation of human Nav1.7 channel gating by synthetic alpha-scorpion toxin OD1 and its analogs. Channels, 10 (2), 139-147. doi: 10.1080/19336950.2015.1120392

Approaches to the stabilization of bioactive epitopes by grafting and peptide cyclization

Conibear, Anne C., Chaousis, Stephanie, Durek, Thomas, Rosengren, K. Johan, Craik, David J. and Schroeder, Christina I. (2016). Approaches to the stabilization of bioactive epitopes by grafting and peptide cyclization. Biopolymers, 106 (1), 89-100. doi: 10.1002/bip.22767

Efficient backbone cyclization of linear peptides by a recombinant asparaginyl endopeptidase

Harris, Karen S., Durek, Thomas, Kaas, Quentin, Poth, Aaron G., Gilding, Edward K., Conlan, Brendon F., Saska, Ivana, Daly, Norelle L., Van Der Weerden, Nicole L., Craik, David J. and Anderson, Marilyn A. (2015). Efficient backbone cyclization of linear peptides by a recombinant asparaginyl endopeptidase. Nature Communications, 6 (10199) 10199, 10199. doi: 10.1038/ncomms10199

Potent complement C3a receptor agonists derived from oxazole amino acids: structure-activity relationships

Singh, Ranee, Reed, Anthony N., Chu, Peifei, Scully, Conor C. G., Yau, Mei-Kwan, Suen, Jacky Y., Durek, Thomas, Reid, Robert C. and Fairlie, David P. (2015). Potent complement C3a receptor agonists derived from oxazole amino acids: structure-activity relationships. Bioorganic and Medicinal Chemistry Letters, 25 (23), 5604-5608. doi: 10.1016/j.bmcl.2015.10.038

Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists

Swedberg, Joakim E., Schroeder, Christina I., Mitchell, Justin M., Durek, Thomas, Fairlie, David P., Edmonds, David J., Griffith, David A., Ruggeri, Roger B., Derksen, David R., Loria, Paula M., Liras, Spiros, Price, David A. and Craik, David J. (2015). Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists. European Journal of Medicinal Chemistry, 103, 175-184. doi: 10.1016/j.ejmech.2015.08.046

Therapeutic conotoxins: a US patent literature survey

Durek, Thomas and Craik, David J. (2015). Therapeutic conotoxins: a US patent literature survey. Expert Opinion in Therapeutic Patents, 25 (10), 1159-1173. doi: 10.1517/13543776.2015.1054095

Fmoc-based synthesis of disulfide-rich cyclic peptides

Cheneval, Olivier, Schroeder, Christina I., Durek, Thomas, Walsh, Phillip, Huang, Yen-Hua, Liras, Spiros, Price, David A. and Craik, David J. (2014). Fmoc-based synthesis of disulfide-rich cyclic peptides. Journal of Organic Chemistry, 79 (12), 5538-5544. doi: 10.1021/jo500699m

Isolation and structural and pharmacological characterization of α-elapitoxin-Dpp2d, an amidated three finger toxin from black mamba venom

Wang, Ching-I Anderson, Reeks, Timothy, Vetter, Irina, Vergara, Irene, Kovtun, Oleksiy, Lewis, Richard J., Alewood, Paul F. and Durek, Thomas (2014). Isolation and structural and pharmacological characterization of α-elapitoxin-Dpp2d, an amidated three finger toxin from black mamba venom. Biochemistry, 53 (23), 3758-3766. doi: 10.1021/bi5004475

Isolation, synthesis and characterization of omega-TRTX-Cc1a, a novel tarantula venom peptide that selectively targets L-type CaV channels

Klint, Julie K., Berecki, Géza, Durek, Thomas, Mobli, Mehdi, Knapp, Oliver, King, Glenn F., Adams, David J., Alewood, Paul F. and Rash, Lachlan D. (2014). Isolation, synthesis and characterization of omega-TRTX-Cc1a, a novel tarantula venom peptide that selectively targets L-type CaV channels. Biochemical Pharmacology, 89 (2), 276-286. doi: 10.1016/j.bcp.2014.02.008

Disulfide-rich macrocyclic peptides as templates in drug design

Northfield, Susan E., Wang, Conan K., Schroeder, Christina I., Durek, Thomas, Kan, Meng-Wei, Swedberg, Joakim E. and Craik, David J. (2014). Disulfide-rich macrocyclic peptides as templates in drug design. European Journal of Medicinal Chemistry, 77 (2), 248-257. doi: 10.1016/j.ejmech.2014.03.011

Chemical synthesis, 3D structure and ASIC binding site of mambalgin-2

Schroeder, Christina I., Rash, Lachlan D., Vila-Farrés, Xavier, Rosengren, K. Johan, Mobli, Mehdi, King, Glenn F., Alewood, Paul F., Craik, David J. and Durek, Thomas (2014). Chemical synthesis, 3D structure and ASIC binding site of mambalgin-2. Angewandte Chemie International Edition, 53 (4), 1017-1020. doi: 10.1002/anie.201308898

Chemical synthesis, 3D structure, and ASIC binding site of the toxin mambalgin-2

Schroeder, Christina I., Rash, Lachlan D., Vila-Farrés, Xavier, Rosengren, K. Johan, Mobli, Mehdi, King, Glenn F., Alewood, Paul F., Craik, David J. and Durek, Thomas (2014). Chemical synthesis, 3D structure, and ASIC binding site of the toxin mambalgin-2. Angewandte Chemie, 126 (4), 1035-1038. doi: 10.1002/ange.201308898

Chemical engineering and structural and pharmacological characterization of the alpha-scorpion toxin OD1

Durek, Thomas, Vetter, Irina, Wang, Ching-I Anderson, Motin, Leonid, Knapp, Oliver, Adams, David J., Lewis, Richard J. and Alewood, Paul F. (2013). Chemical engineering and structural and pharmacological characterization of the alpha-scorpion toxin OD1. ACS Chemical Biology, 8 (6), 1215-1222. doi: 10.1021/cb400012k

Solid phase synthesis of peptide-selenoesters

Ghassemian, Artin, Vila-Farres, Xavier, Alewood, Paul F. and Durek, Thomas (2013). Solid phase synthesis of peptide-selenoesters. Bioorganic and Medicinal Chemistry, 21 (12), 3473-3478. doi: 10.1016/j.bmc.2013.03.076

Efficient chemical synthesis of human complement protein C3a

Ghassemian, Artin, Wang, Ching-I Anderson, Yau, Mei-Kwan, Reid, Robert C., Lewis, Richard J., Fairlie, David P., Alewood, Paul F. and Durek, Thomas (2013). Efficient chemical synthesis of human complement protein C3a. Chemical Communications, 49 (23), 2356-2358. doi: 10.1039/c3cc40537k

Characterisation of Na-v types endogenously expressed in human SH-SY5Y neuroblastoma cells

Vetter, Irina, Mozar, Christine A., Durek, Thomas, Wingerd, Joshua S., Alewood, Paul F., Christie, Macdonald J. and Lewis, Richard J. (2012). Characterisation of Na-v types endogenously expressed in human SH-SY5Y neuroblastoma cells. Biochemical Pharmacology, 83 (11), 1562-1571. doi: 10.1016/j.bcp.2012.02.022

Preformed selenoesters enable rapid native chemical ligation at intractable sites

Durek, Thomas and Alewood, Paul F. (2011). Preformed selenoesters enable rapid native chemical ligation at intractable sites. Angewandte Chemie International Edition, 50 (50), 12042-12045. doi: 10.1002/anie.201105512

Chemical synthesis and structure of the prokineticin Bv8

Morales, Rodrigo A. V., Daly, Norelle L., Vetter, Irina, Mobli, Mehdi, Napier, Ian A., Craik, David J., Lewis, Richard J., Christie, MacDonald J., King, Glenn F., Alewood, Paul F. and Durek, Thomas (2010). Chemical synthesis and structure of the prokineticin Bv8. ChemBioChem, 11 (13), 1882-1888. doi: 10.1002/cbic.201000330

Chemical synthesis and folding of APETx2, a potent and selective inhibitor of acid sensing ion channel 3

Jensen, J. E., Durek, T, Alewood, P. F., Adams, D. J., King, G. F. and Rash, L. D. (2009). Chemical synthesis and folding of APETx2, a potent and selective inhibitor of acid sensing ion channel 3. TOXICON, 54 (1), 56-61. doi: 10.1016/j.toxicon.2009.03.014

Synthesis of photoactive analogues of a cystine knot trypsin inhibitor protein

Durek, Thomas, Zhang, Junliang, He, Chuan and Kent, Stephen B.H. (2007). Synthesis of photoactive analogues of a cystine knot trypsin inhibitor protein. Organic Letters, 9 (26), 5497-5500. doi: 10.1021/ol702461z

Convergent chemical synthesis and high-resolution x-ray structure of human lysozyme

Durek, Thomas, Torbeev, Vladimir Yu and Kent, Stephen B. H. (2007). Convergent chemical synthesis and high-resolution x-ray structure of human lysozyme. Proceedings of the National Academy of Sciences of the United States of America, 104 (2), 4846-4851. doi: 10.1073/pnas.0610630104

Total Chemical Synthesis, Folding, and Assay of a Small Protein on a Water-Compatible Solid Support

Johnson, Erik C. B., Durek, Thomas and Kent, Stephen B. H. (2006). Total Chemical Synthesis, Folding, and Assay of a Small Protein on a Water-Compatible Solid Support. Angewandte Chemie International Edition, 45 (20), 3283-3287. doi: 10.1002/anie.200600381

Structure of doubly prenylated Ypt1:GDI complex and the mechanism of GDI-mediated Rab recycling

Pylypenko, Olena, Rak, Alexey, Durek, Thomas, Kushnir, Susanna, Dursina, Beatrice E., Thomae, Nicolas H., Constantinescu, Alexandru T., Brunsveld, Luc, Watzke, Anja, Waldmann, Herbert, Goody, Roger S. and Alexandrov, Kirill (2006). Structure of doubly prenylated Ypt1:GDI complex and the mechanism of GDI-mediated Rab recycling. The EMBO Journal, 25 (1), 13-23. doi: 10.1038/sj.emboj.7600921

Synthesis of functionalized Rab GTPases by a combination of solution- or solid-phase lipopeptide synthesis with expressed protein ligation

Brunsveld, Luc, Watzke, Anja, Durek, Thomas, Alexandrov, Kirill, Goody, Roger S. and Waldmann, Herbert (2005). Synthesis of functionalized Rab GTPases by a combination of solution- or solid-phase lipopeptide synthesis with expressed protein ligation. Chemistry: A European Journal, 11 (9), 2756-2772. doi: 10.1002/chem.200401041

Chemical biology of protein lipidation: Semi-synthesis and structure elucidation of prenylated RabGTPases

Watzke, Anja, Brunsveld, Luc, Durek, Thomas, Alexandrov, Kirill, Rak, Alexey, Goody, Roger S. and Waldmann, Herbert (2005). Chemical biology of protein lipidation: Semi-synthesis and structure elucidation of prenylated RabGTPases. Organic and Biomolecular Chemistry, 3 (7), 1157-1164. doi: 10.1039/b417573e

Application of protein semisynthesis for the construction of functionalized posttranslationally modified Rab GTPases

Goody, Roger S., Durek, Thomas, Waldmann, Herbert, Brunsveld, Lucas and Alexandrov, Kirill (2005). Application of protein semisynthesis for the construction of functionalized posttranslationally modified Rab GTPases. Methods in Enzymology, 403 4, 29-42. doi: 10.1016/S0076-6879(05)03004-1

Protein semi-synthesis: new proteins for functional and structural studies

Durek, Thomas and Becker, Christian F. W. (2005). Protein semi-synthesis: new proteins for functional and structural studies. Biomolecular Engineering, 22 (5-6), 153-172. doi: 10.1016/j.bioeng.2005.07.004

Synthesis of fluorescently labeled mono- and diprenylated Rab7 GTPase

Durek, Thomas, Alexandrov, Kirill, Goody, Roger S., Hildebrand, Alexandra, Heinemann, Ines and Waldmann, Herbert (2004). Synthesis of fluorescently labeled mono- and diprenylated Rab7 GTPase. Journal of American Chemical Society, 126 (50), 16368-16378. doi: 10.1021/ja046164n

In vitro semi-synthesis and applications of C-terminally modified Rab proteins

Durek, Thomas, Goody, Roger S. and Alexandrov, Kirill (2004). In vitro semi-synthesis and applications of C-terminally modified Rab proteins. Methods in Molecular Biology, 283, 233-244. doi: 10.1385/1-59259-813-7:233

Structure of Rab GDP-dissociation inhibitor in complex with prenylated YPT1 GTPase

Rak, A., Pylypenko, O., Durek, T., Watzke, A., Kushnir, S., Brunsveld, L., Waldmann, H., Goody, R. S. and Alexandrov, K. (2003). Structure of Rab GDP-dissociation inhibitor in complex with prenylated YPT1 GTPase. Science, 302 (5645), 646-650. doi: 10.1126/science.1087761

Intein-Mediated Synthesis of Geranylgeranylated Rab7 Protein in Vitro

Alexandrov, Kirill, Heinemann, Ines, Durek, Thomas, Sidorovitch, Vadim, Goody, Roger S. and Waldmann, Herbert (2002). Intein-Mediated Synthesis of Geranylgeranylated Rab7 Protein in Vitro. Journal of the American Chemical Society, 124 (20), 5648-5649. doi: 10.1021/ja017799e

Development of serine protease inhibitors using the 1,2,3-triazole motif as a disulfide mimetic in the cyclic peptide sunflower trypsin inhibitor-1

White, Andrew, Deveer, Simon, Swedberg, Joakim, Durek, Thomas and Craik, David (2018). Development of serine protease inhibitors using the 1,2,3-triazole motif as a disulfide mimetic in the cyclic peptide sunflower trypsin inhibitor-1. 35th European Peptide Symposium, Dublin City University, Ireland, 26-31 August 2018. Oxford, United Kingdom: John Wiley & Sons. doi: 10.1002/psc.3127

Probing voltage-dependent structural changes of the VSD in mammalian Nav with LRET

Kubota, Tomoya, Durek, Thomas, Finol-Urdaneta, Rocio K., Craik, David J., French, Robert J., Bezanilla, Francisco and Correa, Ana M. (2016). Probing voltage-dependent structural changes of the VSD in mammalian Nav with LRET. 60th Annual Meeting of the Biophysical Society, Los Angeles, United States, Feb 27-Mar 02, 2016. St. Louis, United States: Cell Press. doi: 10.1016/j.bpj.2015.11.665

Protein semi-synthesis and its application to studies of structure and function of GTPases

Rak, A, Pylypenko, O, Durek, T, Watzke, A, Waldmann, H, Goody, RS and Alexandrov, K (2005). Protein semi-synthesis and its application to studies of structure and function of GTPases. 19th American Peptide Symposium, San Diego, U.S., 18-23 June 2005. Hoboken, U.S.: Wiley Interscience.