Publications

2023

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.

https://doi.org/10.1038/s41467-023-38919-2

2022

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.

doi: 10.1021/acs.jmedchem.9b00455

19) From Inhibition to Degradation: Targeting the Anti-Apoptotic Protein Myeloid Cell Leukemia 1 (MCL1)

- 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.

doi: 10.1055/s-0036-1588539

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.

doi: 10.1021/acs.orglett.6b03635

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.

doi: 10.1021/acs.orglett.6b01222

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.

doi: 10.1002/chem.201601370

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.

doi: 10.1016/j.bmcl.2014.09.008

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.

doi: 10.1016/j.bmcl.2013.10.061

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

2013

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

7) Preparation and Use of Cysteine Orthoesters for Solid-Supported Synthesis of Peptides

Huang, Z.; Derksen, D. J.; Vederas, J. C. Org. Lett. 2010, 12, 2282-2285.

doi: 10.1021/ol100645t

2010

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.

doi: 10.1002/cbic.200800272

2019

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.

https://doi.org/10.1021/acschemneuro.0c00333

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.

https://doi.org/10.1016/j.canlet.2020.10.013

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.

https://doi.org/10.1039/D0SC05442A

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.

https://doi.org/10.1124/molpharm.120.000148

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.

https://doi.org/10.1021/acs.joc.1c02518

2021

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.

https://doi.org/10.1039/D2CC00513A

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.

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.

doi: 10.1099/mic.0.2007/009183-0

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.

doi: 10.1007/s00203-006-0147-z

2006

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