Irreversible inhibitors of serine, cysteine, and threonine proteases

JC Powers, JL Asgian, ÖD Ekici, KE James - Chemical reviews, 2002 - ACS Publications
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 …

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 …

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 …

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 …

Three-dimensional quantitative structure− activity relationship analyses using comparative molecular field analysis and comparative molecular similarity indices …

M Böhm, J Stürzebecher, G Klebe - Journal of medicinal chemistry, 1999 - ACS Publications
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 …

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 …

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 …

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 …

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 …

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 …