DERKSEN RESEARCH GROUP
PUBLICATIONS
2024
31) Development of Tetrahydroquinoline-Based Inhibitors for Chronic Pain
Patel, K. V.; Gadotti, V. M.; Garcia-Caballero, A.; Antunes, F. T. T.; Ali, M. Y.; Zamponi, G. W.; Derksen, D. J. Development of Tetrahydroquinoline-Based Inhibitors for Chronic Pain. ACS Chem. Neurosci. 2024, acschemneuro.4c00316.
30) Pannexin-1 Channel Inhibition Alleviates Opioid Withdrawal in Rodents by Modulating Locus Coeruleus to Spinal Cord Circuitry
Kwok, C. H. T.; Harding, E. K.; Burma, N. E.; Markovic, T.; Massaly, N.; Van Den Hoogen, N. J.; Stokes-Heck, S.; Gambeta, E.; Komarek, K.; Yoon, H. J.; Navis, K. E.; McAllister, B. B.; Canet-Pons, J.; Fan, C.; Dalgarno, R.; Gorobets, E.; Papatzimas, J. W.; Zhang, Z.; Kohro, Y.; Anderson, C. L.; Thompson, R. J.; Derksen, D. J.; Morón, J. A.; Zamponi, G. W.; Trang, T. Pannexin-1 Channel Inhibition Alleviates Opioid Withdrawal in Rodents by Modulating Locus Coeruleus to Spinal Cord Circuitry. Nat. Commun. 2024, 15 (1), 6264.
29) Leveraging Pyrazolium Ylide Reactivity to Access Indolizine and 1,2-Dihydropyrimidine Derivatives
Tran, R.; Brownsey, D. K.; O’Sullivan, L.; Brandow, C. M. J.; Chang, E. S.; Zhou, W.; Patel, K. V.; Gorobets, E.; Derksen, D. J. Leveraging Pyrazolium Ylide Reactivity to Access Indolizine and 1,2‐Dihydropyrimidine Derivatives. Chem. – Eur. J. 2024, 30, (28), e202400421
2023
28) Utilising the intrinsic fluorescence of pomalidomide for imaging applications
Brownsey, D. K.; Gafuik, C. J.; Kim, D.-S.; O'Sullivan, L.; Gorobets, E.; Krukowski, S.; Turk, M.; Jenne, C. N.; Mahoney, D. J.; Derksen, D. J. Chem. Commun. 2023, 59, 14532-14545.
https://doi.org/10.1039/D3CC04314B
This article is part of the 2023 Pioneering Investigators themed collection
27) macroH2A2 antagonizes epigenetic programs of stemness in glioblastoma
Ana Nikolic, Francesca Maule, Anna Bobyn, Katrina Ellestad, Seungil Paik, Sajid A. Marhon, Parinaz Mehdipour, Xueqing Lun, Huey-Miin Chen, Claire Mallard, Alexander J. Hay, Michael J. Johnston, Christopher J. Gafuik, Franz J. Zemp, Yaoqing Shen, Nicoletta Ninkovic, Katalin Osz, Elodie Labit, N. Daniel Berger, Duncan K. Brownsey, John J. Kelly, Jeff Biernaskie, Peter B. Dirks, Darren J. Derksen, Steven J. M. Jones, Donna L. Senger, Jennifer A. Chan, Douglas J. Mahoney, Daniel D. De Carvalho, Marco Gallo. Nat. Commun. 2023, 14, 3062.
2022
26) Identification of ligand linkage vectors for the development of p300/CBP degraders
Brownsey, D. K.; Rowley, B. C.; Gorobets, E.; Mihara, K.; Maity, R.; Papatzimas, J. W.; Gelfand, B. S.; Hollenberg, M. D.; Bahlis, N. J.; Derksen, D. J.* RSC Med. Chem. 2022, 13, 726-730.
https://doi.org/10.1039/D1MD00070E
This article is part of the Emerging Investigators themed collection.
25) A Vinylogous Norrish Reaction as a Strategy for Light-Mediated Ring Expansion
Gorobets, E.; Papatzimas, J. W.; Dourado, J.; Yousefalizadeh, G.; Lee, J.; Brownsey, D. K. Stamplecoskie, K.* Davis, R. ;* Derksen, D. J.* Chem. Commun. 2022, 58, 2910-2913.
24) Regioselective Synthesis of C3-Hydroxyarylated Pyrazoles
O'Sullivan, L.; Patel, K. V.; Rowley, B. C.; Brownsey, D. K.; Gorobets, E.; Gelfand, B. S.; Van Humbeck, J. F.; Derksen, D. J.* J. Org. Chem. 2022, 87, 846-854.
2021
23) Metformin prevents hyperglycaemia-associated, oxidative stress-induced vascular endothelial dysfunction: essential role for the orphan nuclear receptor, Nr4a1 (Nur77)
Pulakazhi Venu V. K.; Saifeddine, M; Mihara, K:, Faiza, M;, Gorobets, E; Flewelling, A. J.; Derksen, D. J.; Hirota, S.; Marei, I.; Al-Majid, D.; Motahhary, M.; Ding, H.; Triggle, C. R.; Hollenberg, M. D. Mol. Pharmacol. 2021, 100, 428-455.
22) Rapid Synthesis of Pomalidomide-Conjugates for the Development of Protein Degrader Libraries
Brownsey, D. K.; Rowley, B. C.; Gorobets, E.; Gelfand, B. S.; Derksen, D. J.* Chem. Sci. 2021, 12, 4519-4525.
21) ADAM Protease Inhibition Overcomes Resistance of Breast Cancer Stem-Like Cell to gamma, delta T Cell Immunotherapy
Dutta, I.; Dieters-Castator, D.; Papatzimas, J. W.; Medina, A.; Derksen, D. J.; Lajoie, G.; Postovit, L.-M. Siegers, G. M.* Cancer Lett. 2021, 496, 156-168.
2020
20) Pannexin 1 Channels as a Therapeutic Target: Structure, Inhibition, and Outlook
Navis, Kathleen E.; Fan, Churmy Y.; Trang, Tuan.;Thompson, Roger J.;Derksen, Darren J.* ACS Chemical Neuroscience. 2020, 11, 15, 2163–2172.
2019
19) From Inhibition to Degradation: Targeting the Anti-Apoptotic Protein Myeloid Cell Leukemia 1 (MCL1)
Papatzimas, J. W.; Gorobets, E.; Maity, R.; Muniyat, M. I.; MacCallum, J. L.; Neri, P.; Bahlis, N. J.*; Derksen, D. J.* J. Med. Chem. 2019, 62, 11, 5522-5540.
- Highlighted in Cancer Discovery, News in Depth Article
Targeting MCL1, Companies Aim to Unblock Apoptosis by Elie Dolgin, PhD
doi: 10.1158/2159-8290.CD-ND2019-002
2018
18) Beyond Geminal Diesters: Increasing the Scope of Metal-Mediated Vinylcyclopropane Annulations while Decreasing Pre-activation
Brownsey, D. K.; Gorobets, E.; Derksen, D. J.* Org. Biomol. Chem. 2018, 16, 3506-3523.
doi: 10.1039/C8OB00593A
2017
17) Structure-Activity Relationship (SAR) Studies of Transient Receptor Potential (TRP) Channel Modulators
LeGay, C. M.;Derksen, D. J.* In 2017 Medicinal Chemistry Reviews; Bronson, J. J., Ed.; Medicinal Chemistry Division of the American Chemical Society: Washington, DC, 2017; Vol. 52; pp. 443-463.
16) General Strategy for the Preparation of Thalidomide-Conjugate Linkers
Papatzimas, J. W.; Gorobets, E.; Brownsey, D. K.; Maity, R.; Bahlis, N. J.; Derksen, D. J.*SynLett 2017, 28, 2881-2885. Invited manuscript for special issue dedicated to Professor Victor Snieckus.
15) Divergent Photocyclization/1,4-Sigmatropic Rearrangements for the Synthesis of Sesquiterpenoid Derivatives
Gorobets, E.; Wong, N. E.; Paton, R. S.; Derksen, D. J.* Org. Lett. 2017, 19, 484-487.
2016
14) Thiaporphyrin-mediated Photocatalysis Using Red Light
Lee, J.; Papatzimas, J. W.; Bromby, A. D.; Gorobets, E.; Derksen, D. J.* RSC Adv. 2016, 6, 59269-59272.
doi: 10.1039/c6ra11374e
13) Natural-Product-Derived Transient Receptor Potential Melastatin 8 (TRPM8) Channel Modulators
LeGay, C. M.; Gorobets, E.; Iftinca, M.; Ramachandran, R.; Altier, C.; Derksen, D. J.* Org. Lett. 2016, 18, 2746-2749.
12) Generation of Benzyne Species from Diphenylphosphoryl Derivatives - Simultaneous Exchange of Three Functional Groups
Gorobets, E.; Parvez, M.; Derksen, D. J.; Keay, B. A.* Chem. Eur. J. 2016, 22, 8479-8482.
2014
11) Synthesis and Evaluation of Anti-inflammatory Activity of Derivatives of the Marine Natural Products Fuscol and Eunicol
Kerr, R. G.*; Brophy, S.; Derksen, D. J.* Bioorg. Med. Chem. Lett. 2014, 24, 4804-4806.
10) Inhibition of Serine and Proline Racemases by Substrate-Product Analogues
Harty, M.; Nagar, M.; Atkinson, L.; LeGay, C. M.; Derksen, D. J.* Bearne, S. L.*Bioorg. Med. Chem. Lett. 2014, 24, 390-393.
2013
9) Interactions of Protamine with the Marine Bacterium, Pseudoalteromonas sp.
Pustam, A.; Smith, C.; Deering, C.; Grosicki, K.; Leng, T.-Y.; Yang, J.; Lin, S.; Pink, D.; Gill, T.; Graham, L.; Derksen, D.; Bishop, C.; Demont, M.; Wyeth, R.; Smith-Palmer, T.* NCIMB 2021. Lett. Appl. Microbiol. 2013, 58, 225-230.
doi: 10.1111/lam.12177
8) Elucidating Absolute Configuration of Unsaturated Alcohols via Enantioselective Acylation Reactions
LeGay, C. M.; Boudreau, C. G.; Derksen, D. J.* Org. Biomol. Chem. 2013, 11, 3432-3435.
doi: 10.1039/C3OB40709H
2010
7) Preparation and Use of Cysteine Orthoesters for Solid-Supported Synthesis of Peptides
2008
6) The Role of Hydrophobic Interactions in the N-terminus of Leucocin A and Pediocin PA-1
Derksen, D. J.; Boudreau, M. A.; Vederas, J. C. Chembiochem, 2008, 9, 1898-1901.
2007
5) Structure Function Relationship of Inducer Peptide Pheromones Involved in Bacteriocin Production in Carnobacterium maltaromaticum and Enterococcus faecium
Van Belkum, M. J.; Derksen, D. J.; Franz, C. M. A. P.; Vederas, J. C. Microbiology, 2007, 153, 3660-3666.
4) Multiple On-Resin Olefin Metathesis to Form Ring Expanded Analogues of the Lantibiotic Peptide, Lacticin 3147 A2
Pattabiraman, V. R.; Stymiest, J. L.; Derksen, D. J.; Martin, N. I.; Vederas, J. C. Org. Lett. 2007, 9, 699-702.
doi: 10.1021/ol063133j
2006
3) Antimicrobial Leucocin Analogues with a Disulfide Bridge Replaced by a Carbocycle or by Noncovalent Interactions of Allyl Glycine Residues
Derksen, D. J.; Stymiest, J. L.; Vederas, J. C. J. Am. Chem. Soc. 2006, 128, 14252-14253.
doi: 10.1021/ja066203q
2) Production of Piscicolin 126 by Carnobacterium maltaromaticum UAL26 is Controlled by Temperature and Induction Peptide Concentration
Gursky, L. J.; Martin, N. I.; Derksen, D. J.; van Belkum, M. J.; Kaur, K.; Vederas, J. C.; Stiles, M. E.; McMullen, L. M. Arch. Microbiol. 2006, 186, 317-325.
1) Photolysis of Diacyl Peroxides: A Radical Based Approach for the Synthesis of Functionalized Amino Acids
Spantulescu, M. D.; Jain, R. P.; Derksen, D. J.; Vederas, J. C. Org. Lett. 2003, 5, 2963-2965.
doi: 10.1021/ol035125y
