A Novel Redox Mechanism for the Glutathione-dependent Reversible Uptake of a Fungal Toxin in Cells*
- P. Bernardo, N. Brasch, C. Chai, P. Waring
- BiologyJournal of Biological Chemistry
- 21 November 2003
It is shown that only the natural (oxidized) form of gliotoxin is actively concentrated in a cell line in a glutathione-dependent manner and this mechanism allows for minimal production of the toxin while enabling maximal intracellular concentration and thus maximal efficacy of killing in a competitor organism initially present at low cell density.
Synthesis, electrochemistry, and bioactivity of the cyanobacterial calothrixins and related quinones.
- P. Bernardo, C. Chai, Bronwyn A. Wilkes
- Chemistry, BiologyJournal of Medicinal Chemistry
- 27 August 2004
The studies indicate that while there is no direct correlation between the reduction potentials and biological activities of the studied compounds, in all cases quinones with EC(50) values <1.6 microM undergo reduction to their respective semiquinones readily, with their E(1/2) values being more positive than -0.5 V versus the standard hydrogen electrode (SHE).
Inactivation of Rabbit Muscle Creatine Kinase by Reversible Formation of an Internal Disulfide Bond Induced by the Fungal Toxin Gliotoxin*
The authors' data are consistent with gliotoxin inducing the formation of an internal disulfide bond in creatine kinase by initially binding and possibly activating a cysteine residue on the protein, followed by reaction with a second neighboring thiol.
Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1.
- P. Bernardo, T. Sivaraman, C. Chai
- Chemistry, BiologyJournal of Medicinal Chemistry
- 11 March 2010
Subsequent NMR studies with mutant proteins and in silico docking studies provide a possible rationale for the observed specificity of rhodanine derivatives as inhibitors of Bcl-2 proteins.
A Class of Pantothenic Acid Analogs Inhibits Plasmodium falciparum Pantothenate Kinase and Represses the Proliferation of Malaria Parasites
It was demonstrated that compounds in this series inhibited the phosphorylation of pantothenic acid by Pantothenate kinase, the first step in the parasite's biosynthesis of the essential enzyme cofactor coenzyme A, doing so competitively, with Ki values in the nanomolar range.
Structure-activity delineation of quinones related to the biologically active Calothrixin B.
- P. Bernardo, C. Chai, M. Le Guen, Geoffrey D. Smith, P. Waring
- Chemistry, BiologyBioorganic & Medicinal Chemistry Letters
- 2007
The identification of naturally occurring labdane diterpenoid calcaratarin D as a potential anti-inflammatory agent.
- Quy T N Tran, W. Wong, C. Chai
- Biology, ChemistryEuropean journal of medicinal chemistry
- 15 July 2019
Structure revision and cytotoxic activity of the scabrosin esters, epidithiopiperazinediones from the lichen Xanthoparmelia scabrosa
- M. Ernst-Russell, C. Chai, A. Hurne, P. Waring, D. Hockless, J. Elix
- Chemistry
- 1999
The scabrosin esters (1){(4), isolated from the lichen Xanthoparmelia scabrosa, were reanalysed by modern one- and two-dimensional n.m.r. spectroscopic methods, including 15N n.m.r. spectroscopy, and…
Hybocarpone, a novel cytotoxic naphthazarin derivative from mycobiont cultures of the lichen Lecanora hybocarpa
- M. Ernst-Russell, J. Elix, C. Chai, A. Willis, N. Hamada, T. H. Nash
- Chemistry
- 20 August 1999
A compendium of small molecule direct-acting and host-targeting inhibitors as therapies against alphaviruses
- K. Ching, Lisa F P Ng, C. Chai
- BiologyJournal of Antimicrobial Chemotherapy
- 21 July 2017
A mini-review discusses some of the major features in the replication cycle of alphaviruses, highlighting the key viral targets and host components that participate in alphvirus replication and the molecular functions that were used in drug design.
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