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Title: Allosteric Tuning of Caspase-7: A Fragment-Based Drug Discovery Approach

Journal Article · · Angewandte Chemie (International Edition)
ORCiD logo [1]; ORCiD logo [2]; ORCiD logo [3]
  1. Division of Medicinal and Natural Products Chemistry, College of Pharmacy, University of Iowa, 115 S Grand Ave Iowa City IA 52242 USA
  2. Department of Biochemistry, College of Medicine, University of Iowa, 51 Newton Road Iowa City IA 52242 USA; Protein Crystallography Facility, Roy J. and Lucille A. Carver College of Medicine, University of Iowa, 51 Newton Road Iowa City IA 52242 USA
  3. Division of Medicinal and Natural Products Chemistry, College of Pharmacy, University of Iowa, 115 S Grand Ave Iowa City IA 52242 USA; Department of Biochemistry, College of Medicine, University of Iowa, 51 Newton Road Iowa City IA 52242 USA

Not provided.

Research Organization:
Lawrence Berkeley National Laboratory (LBNL), Berkeley, CA (United States)
Sponsoring Organization:
USDOE Office of Science (SC)
Grant/Contract Number:
AC02-05CH11231
OSTI ID:
1623486
Journal Information:
Angewandte Chemie (International Edition), Vol. 56, Issue 46; ISSN 1433-7851
Publisher:
WileyCopyright Statement
Country of Publication:
United States
Language:
English
Citation Metrics:
Cited by: 8 works
Citation information provided by
Web of Science

References (20)

Human Caspases: Activation, Specificity, and Regulation journal May 2009
Caspase Substrates and Cellular Remodeling journal July 2011
Caspase Functions in Cell Death and Disease: Figure 1. journal April 2015
Discovery of an allosteric site in the caspases journal August 2004
Twenty years on: the impact of fragments on drug discovery journal July 2016
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings 1PII of original article: S0169-409X(96)00423-1. The article was originally published in Advanced Drug Delivery Reviews 23 (1997) 3–25. 1 journal March 2001
The rise of fragment-based drug discovery journal June 2009
A three-stage biophysical screening cascade for fragment-based drug discovery journal October 2013
A Class of Allosteric Caspase Inhibitors Identified by High-Throughput Screening journal August 2012
L2′ loop is critical for caspase-7 active site formation: Essentiality of L2′ Loop in Caspase-7 journal April 2009
Caspase Allostery and Conformational Selection journal January 2016
Structural snapshots reveal distinct mechanisms of procaspase-3 and -7 activation journal May 2013
Fibrils Colocalize Caspase-3 with Procaspase-3 to Foster Maturation journal August 2012
Small-Molecule Activators of a Proenzyme journal November 2009
An Uncleavable Procaspase-3 Mutant Has a Lower Catalytic Efficiency but an Active Site Similar to That of Mature Caspase-3 journal October 2003
Kinetic comparison of procaspase-3 and caspase-3 journal October 2005
Mutations in the Procaspase-3 Dimer Interface Affect the Activity of the Zymogen journal October 2003
On the Mode of Activation of the Catalytically Essential Sulfhydryl Group of Papain journal February 1973
Chemical Mechanism of a Cysteine Protease, Cathepsin C, As Revealed by Integration of both Steady-State and Pre-Steady-State Solvent Kinetic Isotope Effects journal August 2008
Dissecting an Allosteric Switch in Caspase-7 Using Chemical and Mutational Probes journal July 2009

Cited By (3)

Identification of FDA-approved drugs as novel allosteric inhibitors of human executioner caspases journal October 2018
Proteases: Pivot Points in Functional Proteomics book October 2018
Determination of the binding mechanism of histone deacetylase inhibitors journal December 2018