PUBLICATIONS

2022

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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)

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 - 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

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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

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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

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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

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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

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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

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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

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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

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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 

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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 

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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

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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

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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

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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

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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, Accepted

https://doi.org/10.1039/D1MD00070E

This article is part of the Emerging Investigators themed collection.

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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  

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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

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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

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