Irreversible inhibitors of serine, cysteine, and threonine proteases
Proteases or proteolytic enzymes form one of the largest and more important groups of
enzymes. Proteases selectively catalyze the hydrolysis of peptide bonds and can be divided …
enzymes. Proteases selectively catalyze the hydrolysis of peptide bonds and can be divided …
The protein structures that shape caspase activity, specificity, activation and inhibition
P Fuentes-Prior, GS Salvesen - Biochemical Journal, 2004 - portlandpress.com
The death morphology commonly known as apoptosis results from a post-translational
pathway driven largely by specific limited proteolysis. In the last decade the structural basis …
pathway driven largely by specific limited proteolysis. In the last decade the structural basis …
Caspase substrates
JC Timmer, GS Salvesen - Cell Death & Differentiation, 2007 - nature.com
The relatively common occurrence of sequences within proteins that match the consensus
substrate specificity of caspases in intracellular proteins suggests a multitude of substrates …
substrate specificity of caspases in intracellular proteins suggests a multitude of substrates …
Recent developments in structure-based drug design
G Klebe - Journal of molecular medicine, 2000 - Springer
Structure-based design has emerged as a new tool in medicinal chemistry. A prerequisite for
this new approach is an understanding of the principles of molecular recognition in protein …
this new approach is an understanding of the principles of molecular recognition in protein …
Three-dimensional quantitative structure− activity relationship analyses using comparative molecular field analysis and comparative molecular similarity indices …
Three-dimensional quantitative structure− activity relationship (3D QSAR) methods were
applied using a training set of 72 inhibitors of the benzamidine type with respect to their …
applied using a training set of 72 inhibitors of the benzamidine type with respect to their …
A brief historical review of the waterfall/cascade of blood coagulation
EW Davie - Journal of Biological Chemistry, 2003 - ASBMB
Being in the Neurath laboratory gave me an excellent chance to interact with his other
graduate students and postdoctoral fellows. Individuals such as Leon Cunningham gave me …
graduate students and postdoctoral fellows. Individuals such as Leon Cunningham gave me …
Peptide exosite inhibitors of factor VIIa as anticoagulants
MS Dennis, C Eigenbrot, NJ Skelton, MH Ultsch… - Nature, 2000 - nature.com
Potent anticoagulants have been derived by targeting the tissue factor–factor VIIa complex
with naive peptide libraries displayed on M13 phage. The peptides specifically block the …
with naive peptide libraries displayed on M13 phage. The peptides specifically block the …
Surface loops of trypsin-like serine proteases as determinants of function
P Goettig, H Brandstetter, V Magdolen - Biochimie, 2019 - Elsevier
Trypsin and chymotrypsin-like serine proteases from family S1 (clan PA) constitute the
largest protease group in humans and more generally in vertebrates. The prototypes …
largest protease group in humans and more generally in vertebrates. The prototypes …
Gene induction by coagulation factor Xa is mediated by activation of protease-activated receptor 1
M Riewald, VV Kravchenko, RJ Petrovan… - Blood, The Journal …, 2001 - ashpublications.org
Cell signaling by coagulation factor Xa (Xa) contributes to pro-inflammatory responses in
vivo. This study characterizes the signaling mechanism of Xa in a HeLa cell line that …
vivo. This study characterizes the signaling mechanism of Xa in a HeLa cell line that …
Structure and interaction modes of thrombin
W Bode - Blood Cells, Molecules, and Diseases, 2006 - Elsevier
Any vascular injury triggers the burst-like release of the trypsin-like serine proteinase α-
thrombin. Thrombin, the main executioner of the coagulation cascade, exhibits procoagulant …
thrombin. Thrombin, the main executioner of the coagulation cascade, exhibits procoagulant …