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2017

Journal Article

Helixconstraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta-arrestin 2 signaling

Plisson, Fabien, Hill, Timothy A., Mitchell, Justin M., Hoang, Huy N., de Araujo, Aline D., Xu, Weijun, Cotterell, Adam, Edmonds, David J., Stanton, Robert V., Derksen, David R., Loria, Paula M., Griffith, David A., Price, David A., Liras, Spiros and Fairlie, David P. (2017). Helixconstraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta-arrestin 2 signaling. European Journal of Medicinal Chemistry, 127, 703-714. doi: 10.1016/j.ejmech.2016.10.044

Helixconstraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta-arrestin 2 signaling

2017

Journal Article

Alpha helix nucleation by a simple cyclic tetrapeptide

Hoang, Huy N., Wu, Chongyang, Beyer, Renee L., Hill, Timothy A. and Fairlie, David P. (2017). Alpha helix nucleation by a simple cyclic tetrapeptide. Australian Journal of Chemistry, 70 (2), 213-219. doi: 10.1071/CH16591

Alpha helix nucleation by a simple cyclic tetrapeptide

2017

Journal Article

Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain

Odell, Luke R., Abdel-Hamid, Mohammed K., Hill, Timothy A., Ngoc Chau, , Young, Kelly A., Deane, Fiona M., Sakoff, Jennette A., Andersson, Sofia, Daniel, James A., Robinson, Phillip J. and McCluskey, Adam (2017). Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain. Journal of Medicinal Chemistry, 60 (1), 349-361. doi: 10.1021/acs.jmedchem.6b01422

Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain

2016

Journal Article

Helix nucleation by the smallest known α-helix in water

Hoang, Huy N., Driver, Russell W., Beyer, Renee L., Hill, Timothy A., de Araujo, Aline D., Plisson, Fabien, Harrison, Rosemary S., Goedecke, Lena, Shepherd, Nicholas E. and Fairlie, David P. (2016). Helix nucleation by the smallest known α-helix in water. Angewandte Chemie (International Edition), 55 (29), 8275-8279. doi: 10.1002/anie.201602079

Helix nucleation by the smallest known α-helix in water

2015

Journal Article

Flexibility versus rigidity for orally bioavailable cyclic hexapeptides

Nielsen, Daniel S., Lohman, Rink-Jan, Hoang, Huy Ngoc, Hill, Timothy A., Jones, Alun, Lucke, Andrew J. and Fairlie, David P. (2015). Flexibility versus rigidity for orally bioavailable cyclic hexapeptides. Chembiochem, 16 (16), 2289-2293. doi: 10.1002/cbic.201500441

Flexibility versus rigidity for orally bioavailable cyclic hexapeptides

2015

Journal Article

Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists

Hoang, Huy N., Song, Kun, Hill, Timothy A., Derksen, David R., Edmonds, David J., Kok, W. Mei, Limberakis, Chris, Liras, Spiros, Loria, Paula M., Mascitti, Vincent, Mathiowetz, Alan M., Mitchell, Justin M., Piotrowski, David W., Price, David A., Stanton, Robert V., Suen, Jacky Y., Withka, Jane M., Griffith, David A. and Fairlie, David P. (2015). Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists. Journal of Medicinal Chemistry, 58 (9), 4080-4085. doi: 10.1021/acs.jmedchem.5b00166

Short hydrophobic peptides with cyclic constraints are potent glucagon-like peptide-1 receptor (GLP-1R) agonists

2014

Journal Article

Improving on nature: making a cyclic heptapeptide orally bioavailable

Nielsen, Daniel S., Hoang, Huy N., Lohman, Rink-Jan, Hill, Timothy A., Lucke, Andrew J., Craik, David J., Edmonds, David J., Griffith, David A., Rotter, Charles J., Ruggeri, Roger B., Price, David A., Liras, Spiros and Fairlie, David P. (2014). Improving on nature: making a cyclic heptapeptide orally bioavailable. Angewandte Chemie - International Edition, 53 (45), 12059-12063. doi: 10.1002/anie.201405364

Improving on nature: making a cyclic heptapeptide orally bioavailable

2014

Journal Article

Helical cyclic pentapeptides constrain HIV-1 Rev peptide for enhanced RNA binding

Harrison, Rosemary S., Shepherd, Nicholas E., Hoang, Huy N., Beyer, Renee L., Ruiz-Gomez, Gloria, Kelso, Michael J., Mei Kok, W., Hill, Timothy A., Abbenante, Giovanni and Fairlie, David P. (2014). Helical cyclic pentapeptides constrain HIV-1 Rev peptide for enhanced RNA binding. Tetrahedron, 70 (42), 7645-7650. doi: 10.1016/j.tet.2014.07.096

Helical cyclic pentapeptides constrain HIV-1 Rev peptide for enhanced RNA binding

2014

Journal Article

Cyclic penta- and hexaleucine peptides without N-methylation are orally absorbed

Hill, Timothy A., Lohman, Rink-Jan, Hoang, Huy N., Nielsen, Daniel S., Scully, Conor C. G., Kok, W. Mei, Liu, Ligong, Lucke, Andrew J., Stoermer, Martin J., Schroeder, Christina I., Chaousis, Stephanie, Colless, Barbara, Bernhardt, Paul V., Edmonds, David J., Griffith, David A., Rotter, Charles J., Ruggeri, Roger B., Price, David A., Liras, Spiros, Craik, David J. and Fairlie, David P. (2014). Cyclic penta- and hexaleucine peptides without N-methylation are orally absorbed. ACS Medicinal Chemistry Letters, 5 (10), 1148-1151. doi: 10.1021/ml5002823

Cyclic penta- and hexaleucine peptides without N-methylation are orally absorbed

2014

Journal Article

Constraining cyclic peptides to mimic protein structure motifs

Hill, Timothy A., Shepherd, Nicholas E., Diness, Frederik and Fairlie, David P. (2014). Constraining cyclic peptides to mimic protein structure motifs. Angewandte Chemie (International Edition), 53 (48), 13020-13041. doi: 10.1002/anie.201401058

Constraining cyclic peptides to mimic protein structure motifs

2014

Journal Article

Fixierung cyclischer Peptide: Mimetika von Proteinstrukturmotiven

Hill, Timothy A., Shepherd, Nicholas E., Diness, Frederik and Fairlie, David P. (2014). Fixierung cyclischer Peptide: Mimetika von Proteinstrukturmotiven. Angewandte Chemie, 126 (48), 13234-13257. doi: 10.1002/ange.201401058

Fixierung cyclischer Peptide: Mimetika von Proteinstrukturmotiven

2014

Journal Article

Comparative α-Helicity of Cyclic Pentapeptides in Water

de Araujo, Aline D., Hoang, Huy N., Kok, W. Mei, Diness, Frederik, Gupta, Praveer, Hill, Timothy A., Driver, Russell W., Price, David A., Liras, Spiros and Fairlie, David P. (2014). Comparative α-Helicity of Cyclic Pentapeptides in Water. Angewandte Chemie International Edition, 53 (27), 6965-6969. doi: 10.1002/anie.201310245/abstract

Comparative α-Helicity of Cyclic Pentapeptides in Water

2013

Journal Article

A novel class of anticancer compounds targets the actin cytoskeleton in tumor cells

Stehn, Justine R., Haass, Nikolas K., Bonello, Teresa, Desouza, Melissa, Kottyan, Gregg, Treutlein, Herbert, Zeng, Jun, Nascimento, Paula R. B. B., Sequeira, Vanessa B., Butler, Tanya L., Allanson, Munif, Fath, Thomas, Hill, Timothy A., McCluskey, Adam, Schevzov, Galina, Palmer, Stephen J., Hardeman, Edna C., Winlaw, David, Reeve, Vivienne E., Dixon, Ian, Weninger, Wolfgang, Cripe, Timothy P. and Gunning, Peter W. (2013). A novel class of anticancer compounds targets the actin cytoskeleton in tumor cells. Cancer Research, 73 (16), 5169-5182. doi: 10.1158/0008-5472.CAN-12-4501

A novel class of anticancer compounds targets the actin cytoskeleton in tumor cells

2013

Journal Article

Pyrimidyn compounds: dual-action small molecule pyrimidine-based dynamin inhibitors

McGeachie, Andrew B., Odell, Luke R., Quan, Annie, Daniel, James A., Chau, Ngoc, Hill, Timothy A., Gorgani, Nick N., Keating, Damien J., Cousin, Michael A., van Dam, Ellen M., Mariana, Anna, Whiting, Ainslie, Perera, Swetha, Novelle, Aimee, Young, Kelly A., Deane, Fiona M., Gilbert, Jayne, Sakoff, Jennette A., Chircop, Megan, McCluskey, Adam and Robinson, Phillip J. (2013). Pyrimidyn compounds: dual-action small molecule pyrimidine-based dynamin inhibitors. ACS Chemical Biology, 8 (7), 1507-1518. doi: 10.1021/cb400137p

Pyrimidyn compounds: dual-action small molecule pyrimidine-based dynamin inhibitors

2013

Journal Article

Truncated and Helix-Constrained Peptides with High Affinity and Specificity for the cFos Coiled-Coil of AP-1

Rao, Tara, Ruiz-Gomez, Gloria, Hill, Timothy A., Hoang, Huy N., Fairlie, David P. and Mason, Jody M. (2013). Truncated and Helix-Constrained Peptides with High Affinity and Specificity for the cFos Coiled-Coil of AP-1. PLoS One, 8 (3) e59415, e59415.1-e59415.12. doi: 10.1371/journal.pone.0059415

Truncated and Helix-Constrained Peptides with High Affinity and Specificity for the cFos Coiled-Coil of AP-1

2012

Journal Article

Folding pentapeptides into left and right handed alpha helices

Hoang, Huy N., Abbenante, Giovanni, Hill, Timothy A., Ruiz-Gomez, Gloria and Fairlie, David P. (2012). Folding pentapeptides into left and right handed alpha helices. Tetrahedron, 68 (23), 4513-4516. doi: 10.1016/j.tet.2011.10.108

Folding pentapeptides into left and right handed alpha helices

2011

Journal Article

An Ugi-intramolecular Diels-Alder route to highly substituted tetrahydroepoxyisoindole carboxamides

Gordon, Christopher P., Young, Kelly A., Robertson, Mark J., Hill, Timothy A. and McCluskey, Adam (2011). An Ugi-intramolecular Diels-Alder route to highly substituted tetrahydroepoxyisoindole carboxamides. Tetrahedron, 67 (2), 554-561. doi: 10.1016/j.tet.2010.10.042

An Ugi-intramolecular Diels-Alder route to highly substituted tetrahydroepoxyisoindole carboxamides

2010

Journal Article

Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice

Harrison, Rosemary S., Ruiz-Gomez, Gloria, Hill, Timothy A., Chow, Shiao Y., Shepherd, Nicholas E., Lohman, Rink-Jan, Abbenante, Giovanni, Hoang, Huy N. and Fairlie, David P. (2010). Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice. Journal of Medicinal Chemistry, 53 (23), 8400-8408. doi: 10.1021/jm101139f

Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice

2010

Journal Article

The antiplasmodial activity of norcantharidin analogs

Bajsa, Joanna, McCluskey, Adam, Gordon, Christopher P., Stewart, Scott G., Hill, Timothy A., Sahu, Rajnish, Duke, Stephen O. and Tekwani, Babu L. (2010). The antiplasmodial activity of norcantharidin analogs. Bioorganic and Medicinal Chemistry Letters, 20 (22), 6688-6695. doi: 10.1016/j.bmcl.2010.09.004

The antiplasmodial activity of norcantharidin analogs

2010

Journal Article

Update 1 of: Beta-strand mimetics

Loughlin, Wendy A., Tyndall, Joel D. A., Glenn, Matthew P., Hill, Timothy A. and Fairlie, David P. (2010). Update 1 of: Beta-strand mimetics. Chemical Reviews, 110 (6), 1-38. doi: 10.1021/cr900395y

Update 1 of: Beta-strand mimetics