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Keywords: inhibitor
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Biochem J (2023) 480 (16): 1317–1330.
Published: 25 August 2023
... for OTUD1 lacking the unstructured N-terminal region (OTUD1 OTU + UIM ) in an attempt to identify inhibitors bridging the catalytic domain and the UIM containing region. Two UbVs were identified (UbV OD.1 and UbV OD.2 ) with high affinity and specificity for OTUD1. Of the UbVs identified, UbV OD.1 inhibited...
Includes: Supplementary data
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Biochem J (2021) 478 (3): 647–668.
Published: 12 February 2021
... therapies. In severe P. aeruginosa infections, the phospholipase activity of the type 3 secretion system toxin, ExoU, induces lysis of target host cells and results in the poorest clinical outcomes. We have developed an integrated pipeline to evaluate small molecule inhibitors of ExoU in vitro...
Includes: Supplementary data
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Biochem J (2021) 478 (2): 389–406.
Published: 27 January 2021
... (PRMT) has been shown to be up-regulated in various cancers. PRMTs have emerged as attractive targets for the development of new cancer therapies. Here, we describe the identification of a natural compound, licochalcone A, as a novel, reversible and selective inhibitor of PRMT6. Since expression...
Includes: Supplementary data
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Biochem J (2020) 477 (21): 4133–4148.
Published: 05 November 2020
... of blood pressure (BP) in hypertensive animals. The oral administration of RB150 renamed firibastat by WHO, an APA inhibitor prodrug, targeting only the S1 subsite, decreases BP in hypertensive patients from various ethnic origins. To identify new families of potent and selective APA inhibitors, we...
Includes: Supplementary data
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Biochem J (2020) 477 (17): 3329–3347.
Published: 10 September 2020
.... As a well-known allosteric activator of epidermal growth factor receptor family members, and playing a major part in cancer progression, the pseudokinase HER3 is a relevant context in which to address the potential of pseudokinases as drug targets for the development of allosteric inhibitors. In this proof...
Includes: Multimedia, Supplementary data
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Biochem J (2016) 473 (19): 3159–3175.
Published: 27 September 2016
... populations of the PKA catalytic subunit with distinct structural stability and susceptibility to the physiological protein inhibitor PKI. Native MS of reconstituted PKA R 2 C 2 holoenzymes reveals variable subunit stoichiometry and holoenzyme ablation by PKI binding. Finally, we find that although a ‘kinase...
Includes: Supplementary data
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Biochem J (2016) 473 (18): 2757–2762.
Published: 12 September 2016
... kinase, leucine-rich repeat kinase 2 (LRRK2), which is mutated (and probably hyperactive) in a small, but significant, subset of patients. An exciting new approach for personalised therapy is the development of central nervous system (CNS)-active small-molecule kinase inhibitors, which could be employed...
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Biochem J (2016) 473 (11): 1579–1591.
Published: 27 May 2016
... (NP40) lysis buffer supplemented with orthovanadate, PMSF and protease inhibitor cocktail (ThermoFischer Scientific). Lysate samples were analysed by SDS/PAGE using a 4–12% gradient NuPage® NOVEX BisTris Gel (Invitrogen) and transferred to a nitrocellulose membrane. Total JAK2 was detected using Jak2...
Includes: Supplementary data
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Biochem J (2016) 473 (8): 1027–1035.
Published: 08 April 2016
... clustering in cancer cells, but is not essential for normal cells. Therefore, targeting KIFC1 may provide novel insight into selective killing of cancer cells. In the present study, we identified a small-molecule KIFC1 inhibitor, SR31527, which inhibited microtubule (MT)-stimulated KIFC1 ATPase activity...
Includes: Supplementary data
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Biochem J (2016) 473 (5): 537.
Published: 24 February 2016
...) isoforms to antagonize TGF-β signalling and TGF-β-induced responses. These findings suggest that sCD109 may play an important role in regulating TGF-β action. binding CD109 glycoprotein inhibitor TGF-β isoforms trap Transforming growth factor-β (TGF-β) is a multifunctional growth factor...
Includes: Supplementary data
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Biochem J (2014) 462 (3): 425–432.
Published: 22 August 2014
... for drug discovery, and inhibitors that target this activity may increase the efficacy of nucleoside/nucleotide analogues, and may help to delay the onset of drug resistance. In the present study, we have developed a FRET (Förster resonance energy transfer)-based high-throughput screening assay for the AZT...
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Biochem J (2014) 459 (3): 505–512.
Published: 11 April 2014
... in characterizing functions of methyllysine-recognizing epigenetic readers. Calixarenes disrupt the association of the PHD finger of CHD4 with a trimethylated, but not an unmodified, histone tail. calixarene chromodomain helicase DNA-binding protein 4 (CHD4) histone inhibitor methylation plant...
Includes: Supplementary data
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Biochem J (2013) 456 (1): 1–12.
Published: 24 October 2013
... of these enzymes have resulted in the development of potent and selective inhibitors. The present review gives an overview of these inhibitors and how they have been used on cell lines, primary cells and animals to modulate O -GlcNAc levels and study the effects on signal transduction. 1 To whom...
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Biochem J (2013) 451 (2): 313–328.
Published: 28 March 2013
...Yinghong Gao; Stephen P. Davies; Martin Augustin; Anna Woodward; Umesh A. Patel; Robert Kovelman; Kevin J. Harvey Despite the development of a number of efficacious kinase inhibitors, the strategies for rational design of these compounds have been limited by target promiscuity. In an effort...
Includes: Supplementary data
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Biochem J (2013) 450 (2): 375–386.
Published: 15 February 2013
... in each well with 100 μl lysis buffer containing protease inhibitors. Protein concentrations were measured using a Bio-Rad Laboratories protein assay kit. Lysates containing 30–80 μg protein were subjected to SDS/PAGE (10 or 12% gels). The separated proteins were transferred on to a nitrocellulose...
Includes: Supplementary data
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Biochem J (2012) 448 (3): 417–423.
Published: 21 November 2012
...Jin H. Park; Yingting Liu; Mark A. Lemmon; Ravi Radhakrishnan Erlotinib and gefitinib, tyrosine kinase inhibitors used to block EGFR (epidermal growth factor receptor) signalling in cancer, are thought to bind only the active conformation of the EGFR-TKD (tyrosine kinase domain). Through parallel...
Includes: Supplementary data
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Biochem J (2011) 438 (3): 467–474.
Published: 26 August 2011
... for the action of insecticides. PUGNAc [ O -(2-acetamido-2-deoxy- D -glucopyransylidene)-amino- N -phenylcarbamate] was initially identified as an inhibitor against GH20 β- N -acetyl- D -hexosaminidases. So far no crystal structure of PUGNAc in complex with any GH20 β- N -acetyl- D -hexosaminidase has been...
Includes: Supplementary data
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Biochem J (2006) 393 (2): e1.
Published: 23 December 2005
... of basic residues, a specificity that resembles that of the furin-like PCs (proprotein convertases). This led to the demonstration that furin/PC inhibitors containing poly( D -arginine) are also potent inhibitors of NS3, and that anthrax toxin protective antigen and myelin basic protein are potential NS3...
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Biochem J (2005) 389 (2): 365–371.
Published: 05 July 2005
... analogue inhibitors. The true transition state, however, has not been structurally characterized. The crystal structure of the C95M/C1095A HIV-1 protease tethered dimer shows a distinctive feature in which the two flaps of the enzyme are in a ‘closed conformation’ even in the unliganded state. This unique...
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Biochem J (2005) 387 (3): 585–590.
Published: 26 April 2005
...Alan M. SIMM; E. Joel LOVERIDGE; John CROSBY; Matthew B. AVISON; Timothy R. WALSH; Peter M. BENNETT Bulgecin A, a sulphonated N -acetyl- D -glucosamine unit linked to a 4-hydroxy-5-hydroxymethylproline ring by a β-glycosidic linkage, is a novel type of inhibitor for binuclear metallo-β-lactamases...
Includes: Supplementary data
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Biochem J (2005) 385 (1): 181–187.
Published: 14 December 2004
...Benedykt WLADYKA; Katarzyna PUZIA; Adam DUBIN Staphopain A is a staphylococcal cysteine protease. Genes encoding staphopain A and its specific inhibitor, staphostatin A, are localized in an operon. Staphopain A is an important staphylococcal virulence factor. It is difficult to perform studies...
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Biochem J (2004) 384 (2): 201–232.
Published: 23 November 2004
... the fundamental structures of examples from the initiator phase, the pre-mitochondrial regulator phase, the executioner phase, inhibitors and their antagonists, and even the structures of some substrates. The field is as well advanced as the best known of proteolytic pathways, the coagulation cascade...
Includes: Supplementary data
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Biochem J (2004) 377 (1): 171–181.
Published: 01 January 2004
...Qing-Rong LIU; Ping-Wu ZHANG; Zhicheng LIN; Qi-Fu LI; Amina S. WOODS; Juan TRONCOSO; George R. UHL The activities of PP1 (protein phosphatase 1), a principal cellular phosphatase that reverses serine/threonine protein phosphorylation, can be altered by inhibitors whose activities are themselves...
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Biochem J (2003) 370 (3): 737–749.
Published: 15 March 2003
... was observed within tissue types. HDAC inhibitors have been shown to induce specific changes in gene expression and to influence a variety of other processes, including growth arrest, differentiation, cytotoxicity and induction of apoptosis. This challenging field has generated many fascinating results which...
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Biochem J (2002) 366 (2): 653–661.
Published: 01 September 2002
... of topoisomerase I by luteolin is due to the stabilization of topoisomerase-I DNA-cleavable complexes. Hence, luteolin is similar to camptothecin, a class I inhibitor, with respect to its ability to form the topoisomerase I-mediated ‘cleavable complex'. But, unlike camptothecin, luteolin interacts with both free...
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Biochem J (2002) 361 (2): 347–354.
Published: 08 January 2002
... RNA polymerase. One of these mAbs turned out to be the first antibody inhibitor of the binding of NusA and σ70; it did not affect GreB and HepA interactions. Its epitope was located on the β′ subunit at the C-terminus of region G. The properties of this mAb reinforce the idea that the mutually...
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Biochem J (2001) 357 (3): 593–615.
Published: 25 July 2001
... in the context of this important part of the enzyme, with its binding sites for iron protoporphyrin IX (haem), biopterin, l -arginine, and the many inhibitors which interact with them. The exact nature of the NOS reaction, its mechanism and its products continue to be sources of controversy. The role...
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Biochem J (2000) 350 (3): 671–676.
Published: 08 September 2000
... propeptide did not show evidence of forming an active enzyme, of correctly folding in vitro or of inhibiting the active region. folding inhibitor metalloprotease processing pro-enzyme 1 To whom correspondence should be addressed (e-mail [email protected] ). 2 5 2000 28 6...
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Biochem J (1999) 343 (1): 29–37.
Published: 24 September 1999
... μ M) and Arg-Ser-Lys-Arg-SC ( K i 11.4 μ M). 1 To whom correspondence should be addressed, at the Ottawa Hospital Medical School (e-mail [email protected] ). 10 5 1999 22 7 1999 The Biochemical Society, London © 1999 1999 inhibitor protease activity protein substrate...