Apoptosis-based therapies and drug targets
U Fischer, K Schulze-Osthoff - Cell Death & Differentiation, 2005 - nature.com
The pathogenesis of many diseases is most closely connected with aberrantly regulated
apoptotic cell death. The past 15 years have witnessed an explosion in the basic knowledge …
apoptotic cell death. The past 15 years have witnessed an explosion in the basic knowledge …
Small molecule active site directed tools for studying human caspases
Caspases are proteases of clan CD and were described for the first time more than two
decades ago. They play critical roles in the control of regulated cell death pathways …
decades ago. They play critical roles in the control of regulated cell death pathways …
First-in-class pan caspase inhibitor developed for the treatment of liver disease
SD Linton, T Aja, RA Armstrong, X Bai… - Journal of medicinal …, 2005 - ACS Publications
A series of oxamyl dipeptides were optimized for pan caspase inhibition, anti-apoptotic
cellular activity and in vivo efficacy. This structure− activity relationship study focused on the …
cellular activity and in vivo efficacy. This structure− activity relationship study focused on the …
Caspase inhibitors: a pharmaceutical industry perspective
SD Linton - Current topics in medicinal chemistry, 2005 - ingentaconnect.com
Caspase inhibition has been demonstrated to be therapeutically effective in moderating
excessive programmed cell death, or apoptosis. Publications detailing programs in the …
excessive programmed cell death, or apoptosis. Publications detailing programs in the …
Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis
JW Becker, J Rotonda, SM Soisson… - Journal of medicinal …, 2004 - ACS Publications
Caspases are cysteine proteases that specifically cleave Asp− Xxx bonds. They are key
agents in inflammation and apoptosis and are attractive targets for therapy against …
agents in inflammation and apoptosis and are attractive targets for therapy against …
Pyrrolo [3, 4-c] quinoline-1, 3-diones as potent caspase-3 inhibitors. Synthesis and SAR of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-pyrrolo [3, 4-c] quinoline-1 …
DV Kravchenko, VM Kysil, SE Tkachenko… - European journal of …, 2005 - Elsevier
Synthesis, biological evaluation and structure–activity relationships for a series of 2-
substituted 4-methyl-8-(morpholine-4-sulfonyl)-1, 3-dioxo-2, 3-dihydro-1H-pyrrolo [3, 4-c] …
substituted 4-methyl-8-(morpholine-4-sulfonyl)-1, 3-dioxo-2, 3-dihydro-1H-pyrrolo [3, 4-c] …
Efficient one-step synthesis of pyrrolo [3, 4-c] quinoline-1, 3-dione derivatives by organocatalytic cascade reactions of isatins and β-ketoamides
We describe an efficient one-step synthesis of pyrrolo [3, 4-c] quinolinedione derivatives
using ethylenediamine diacetate (EDDA)-catalyzed cascade reactions of isatins and β …
using ethylenediamine diacetate (EDDA)-catalyzed cascade reactions of isatins and β …
Exploiting differences in caspase-2 and-3 S2 subsites for selectivity: Structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based …
MC Maillard, FA Brookfield, SM Courtney… - Bioorganic & medicinal …, 2011 - Elsevier
Several caspases have been implicated in the pathogenesis of Huntington's disease (HD);
however, existing caspase inhibitors lack the selectivity required to investigate the specific …
however, existing caspase inhibitors lack the selectivity required to investigate the specific …
Cell death targets and potential modulators in Alzheimer's disease
RE Castro, M MM Santos, P MC Gloria… - Current …, 2010 - ingentaconnect.com
Apoptosis is now recognized as a normal feature in the development of the nervous system
and may also play a role in neurodegenerative disorders, such as Alzheimer's disease. Cell …
and may also play a role in neurodegenerative disorders, such as Alzheimer's disease. Cell …
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: Highly Potent and Selective Inhibitors of the Type 5 17-β-Hydroxysteroid Dehydrogenase AKR1C3
SMF Jamieson, DG Brooke, D Heinrich… - Journal of medicinal …, 2012 - ACS Publications
A high-throughput screen identified 3-(3, 4-dihydroisoquinolin-2 (1H)-ylsulfonyl) benzoic
acid as a novel, highly potent (low nM), and isoform-selective (1500-fold) inhibitor of aldo …
acid as a novel, highly potent (low nM), and isoform-selective (1500-fold) inhibitor of aldo …