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Keywords: inhibitor
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Biochem Soc Trans (2020) 48 (2): 479–497.
Published: 20 March 2020
... understood. In this review, we will provide an overview of the current status of selected small molecule ubiquitin system inhibitors. We will further discuss the unique challenges of targeting this ubiquitous and highly complex machinery, and explore and highlight potential ways in which these challenges...
Biochem Soc Trans (2016) 44 (4): 979–986.
Published: 15 August 2016
... pathways and crucially, several members have been shown to be down-regulated in common cancers (such as breast and prostate). In the present study we focus on the development of lysine (K) acetyltransferase inhibitors (KATi) targeting the MYST family member Tip60 (Kat5), an essential protein, designed...
Biochem Soc Trans (2016) 44 (1): 88–93.
Published: 09 February 2016
... on the available OGT inhibitors and summarizes advantages, limitations and future challenges. 1 These authors contributed equally to this work. 2 To whom correspondence should be addressed ( d.m.f.vanaalten@dundee.ac.uk ). 20 11 2015 © 2016 Authors; published by Portland Press Limited...
Biochem Soc Trans (2015) 43 (5): 1095–1103.
Published: 09 October 2015
...′-triphosphate (ATP) inhibitor ligand pseudokinase tribbles tribbles 2 (TRIB2) Protein pseudokinases are components of essentially all sequenced kinomes and are defined as lacking at least one of the conserved amino acids that are required for efficient ATP binding and/or catalysis...
Biochem Soc Trans (2014) 42 (5): 1343–1348.
Published: 18 September 2014
... to their corresponding discovery. The hexagon represents the inositol headgroup, with phosphates being represented as red circles. The lower part contains the timeline for the discovery of inositol lipids (black) and chemical intervention tools (3-kinase and 3-phosphatase inhibitors; red). 1 email...
Biochem Soc Trans (2013) 41 (6): 1551–1556.
Published: 20 November 2013
... acid oxidase inhibitor neuromodulator N -methyl- D -aspartate (NMDA) receptor regulation D -serine metabolism Recombinant hDAAO (human DAAO) was expressed in Escherichia coli and purified as a stable and active holoenzyme [ 28 , 29 ]. The protomer (347 residues, ~40 kDa) displays...
Biochem Soc Trans (2008) 36 (6): 1414–1417.
Published: 19 November 2008
... thermodynamics, and mutational analysis Chem. Rev. 1997 97 1233 1250 2 Stockwin L.H. Holmes S. Antibodies as therapeutic agents: vive la renaissance! Expert Opin Biol. Ther. 2003 3 1133 1152 3 Arkin M.R. Wells J.A. Small-molecule inhibitors of protein–protein...
Biochem Soc Trans (2007) 35 (3): 559–560.
Published: 22 May 2007
... through the inactivation of LEI (leucocyte elastase inhibitor) via translational modification. Inhibition of AP24 is observed by overexpression of Bcl-2 in HL-60 cells [ 13 ]. Studies demonstrating the effect of the naturally occurring serine proteinase inhibitors (serpins) in regulating apoptosis...
Biochem Soc Trans (2005) 33 (2): 343–345.
Published: 01 April 2005
...A.J. Bridges The development of kinase and phosphatase inhibitors as novel therapeutic agents has been stimulated by the discovery that most biological processes are controlled by the reversible phosphorylation of proteins. Most of the early results in this area were generated in oncology...
Biochem Soc Trans (2004) 32 (2): 348–349.
Published: 01 April 2004
... and the phosphatidylinositol 3-phosphatase PTEN (phosphatase and tensin homologue deleted on chromosome 10). Specific inhibitors targeting phosphoinositide 3-kinase and protein phosphatases have been described and characterized, but no small-molecule tools for phosphoinositide phosphatases are currently available. The present...
Biochem Soc Trans (2004) 32 (1): 17–20.
Published: 01 February 2004
... inhibitors. An imbalance between the active enzymes and their natural inhibitors leads to the accelerated destruction of connective tissue associated with the pathology of diseases such as arthritis, cancer, multiple sclerosis and cardiovascular diseases. The potential for using specific enzyme inhibitors...
Biochem Soc Trans (2003) 31 (6): 1378–1382.
Published: 01 December 2003
... classes of tumoricidal agents that specifically target this elementary detoxification pathway in order to induce elevated concentrations of cytotoxic methylglyoxal in tumour cells. Special emphasis is placed on structure- and mechanism-based inhibitors of GlxI (glyoxalase I), the first enzyme...
Biochem Soc Trans (2003) 31 (2): 393–396.
Published: 01 April 2003
... for the polyamines in cancer development, treatment and/or prevention. The recognition that polyamines are critical for the growth of cancer cells, and consequently the identification of their metabolic pathways as a target for therapeutic intervention, led to the development of a number of useful inhibitors...
Biochem Soc Trans (2000) 28 (4): 455–460.
Published: 01 August 2000
...V. Dive; K. Lucet-Levannier; D. Georgiadis; J. Cotton; S. Vassiliou; P. Cuniasse; A. Yiotakis The development of the combinatorial chemistry of phosphinic peptides has led to the discovery of both highly potent and selective inhibitors of various zinc metalloproteinases. Several properties...