Linking Ubiquitin Research to Drug Discovery

Featured Publications of Interest

20 Publications

Ubiquigent services highlighted below:
DUBprofiler
High-throughput small molecule IDOL screening assay

  • A review of drug discovery opportunities across deubiquitylating (DUB) enzymes
    Harrigan et al. (2018) Deubiquitylating enzymes and drug discovery: emerging opportunities. Nat Rev Drug Discov (1):57-78. doi: 10.1038/nrd.2017.152. Epub 2017 Sep 29.
  • Arguing the value of target class focussed drug discovery; building a target class-specific assay and chemistry platform
    Barnash et al. (2017) Target class drug discovery. Nat Chem Biol. 13(10):1053-1056. doi: 10.1038/nchembio.2473.
  • DUB targeting small molecule drug discovery by Genentech
    Di Lello et al. (2017) Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques. J Med Chem. 60(24):10056-10070. doi: 10.1021/acs.jmedchem.7b01293. Epub 2017 Dec 8.
  • The application of Ubiquigent’s DUBprofiler service in DUB targeting small molecule drug discovery by Almac Discovery
    Gavory et al. (2017) Discovery and characterization of highly potent and selective allosteric USP7 inhibitors. Nat Chem Biol. doi: 10.1038/nchembio.2528. [Epub ahead of print]
  • DUB targeting small molecule drug discovery by Genentech
    Kategaya et al. (2017) USP7 small-molecule inhibitors interfere with ubiquitin binding. Nature. 550(7677):534-538. doi: 10.1038/nature24006. Epub 2017 Oct 18.
  • The application of Ubiquigent’s DUBprofiler service in DUB targeting small molecule drug discovery by the Dana-Farber Cancer Institute and Harvard Medical School
    Lamberto et al. (2017) Structure-Guided Development of a Potent and Selective Non-covalent Active-Site Inhibitor of USP7. Cell Chem Biol. pii: S2451-9456(17)30329-X. doi: 10.1016/j.chembiol.2017.09.003. [Epub ahead of print]
  • DUB targeting small molecule drug discovery by Progenra, University of Connecticut and Yale University
    Pozhidaeva et al. (2017) USP7-Specific Inhibitors Target and Modify the Enzyme's Active Site via Distinct Chemical Mechanisms. Cell Chem Biol. pii: S2451-9456(17)30330-6. doi: 10.1016/j.chembiol.2017.09.004. [Epub ahead of print]
  • The application of Ubiquigent’s DUBprofiler service in DUB targeting small molecule drug discovery by FORMA Therapeutics
    Turnbull et al. (2017) Molecular basis of USP7 inhibition by selective small-molecule inhibitors. Nature. 550(7677):481-486. doi: 10.1038/nature24451. Epub 2017 Oct 18.
  • The application of Ubiquigent’s DUBprofiler service in DUB targeting small molecule drug discovery by Almac Discovery and Astra Zeneca
    Wrigley et al. (2017) Identification and characterisation of dual inhibitors of the USP25/28 Deubiquitinating enzyme subfamily. ACS Chem Biol DOI: 10.1021/acschembio.7b00334
  • The DUB USP5 as a potential target for inflammatory and neuropathic pain.
    Gadotti et al. (2015) Small organic molecule disruptors of Cav3.2 - USP5 interactions reverse inflammatory and neuropathic pain. Mol Pain. 11. doi: 10.1186/s12990-015-0011-8. Epub 2015 Mar 14. VM1, Caballero AG, Berger ND, Gladding CM, Chen L, Pfeifer TA, Zamponi GW.
  • Seminal paper associating the targeting of USP30 to the regulation of parkin-mediated mitophagy in the context of Parkinson’s disease
    Bingol et al. (2014) The mitochondrial deubiquitinase USP30 opposes parkin-mediated mitophagy. Nature. 510(7505):370-5. doi: 10.1038/nature13418. Epub 2014 Jun 4.
  • Discussion paper by Ubiquigent’s Scientific Director and Chairman addressing the need for targeted chemical libraries to enable ubiquitin system drug discovery
    Brown and Treherne (2014 ) Targeted chemical libraries: the keys to unlock the ubiquitin system Is novel chemistry the final frontier for ubiquitin system drug discovery? Drug Discovery World 66-74
  • A review of drug targeting opportunities across the ubiquitin system
    Bedford, L., et al. (2012) Ubiquitin-like protein conjugation and the ubiquitin-proteasome system as drug targets. Nat. Rev. Drug Disc. 10, 1-19.
  • The elucidation of the mechanics of the lysosomal and ubiquitin proteasome systems
    Ciechanover, A. (2012) Intracellular protein degradation: From a vague idea thru the lysosome and the ubiquitin-proteasome system and onto human diseases and drug targeting. Biochim Biophys Acta 1824(1): 3-13.
  • Small molecule targeting of the immuno- and constitutive proteasome
    Huber and Groll (2012) Inhibitors for the Immuno- and Constitutive Proteasome: Current and Future Trends in Drug Development. Angew Chem Int Ed Engl. doi: 10.1002/anie.201201616. [Epub ahead of print]
  • Therapeutic opportunities provided by the targeting of autophagy
    Rubinsztein et al. (2012) Autophagy modulation as a potential therapeutic target for diverse diseases. Nat Rev Drug Discov 11(9), 709-730.
  • Small molecule E1 inhibitors
    Ungermannova et al. (2012) Largazole and its derivatives selectively inhibit ubiquitin activating enzyme (e1). PLoS One7, e29208.
  • A review of ubiquitin-like proteins
    van der Veen and Ploegh (2012) Ubiquitin-Like Proteins. Annu Rev Biochem 81, 323-357.
  • Kinases and the ubiquitin system: A comparative review of drug discovery opportunities by Ubiquigent’s SAB Chairman
    Cohen, P. and M. Tcherpakov (2010) Will the ubiquitin system furnish as many drug targets as protein kinases? Cell 143(5): 686-693. Uploaded: 13 February 2012
  • The E3 ubiquitin ligase IDOL regulates cellular LDL uptake: See Ubiquigent’s high-throughput small molecule IDOL screening assay
    Zelcer et al. (2009) LXR regulates cholesterol uptake through Idol-dependent ubiquitination of the LDL receptor. Science 325(5936), 100-104.