Proteases universally recognize beta strands in their active sites.

PubWeight™: 1.90‹?› | Rank: Top 3%

🔗 View Article (PMID 15755082)

Published in Chem Rev on March 01, 2005

Authors

Joel D A Tyndall1, Tessa Nall, David P Fairlie

Author Affiliations

1: Centre for Drug Design and Development, Institute for Molecular Bioscience, University of Queensland, Brisbane, Qld 4072, Australia. joel.tyndall@otago.ac.nz

Articles citing this

Sequence-specific intramembrane proteolysis: identification of a recognition motif in rhomboid substrates. Mol Cell (2009) 2.45

Contemporary strategies for the stabilization of peptides in the alpha-helical conformation. Curr Opin Chem Biol (2008) 1.99

Enhanced metabolic stability and protein-binding properties of artificial alpha helices derived from a hydrogen-bond surrogate: application to Bcl-xL. Angew Chem Int Ed Engl (2005) 1.59

The structural basis for catalysis and substrate specificity of a rhomboid protease. EMBO J (2010) 1.20

Energetics-based protein profiling on a proteomic scale: identification of proteins resistant to proteolysis. J Mol Biol (2007) 1.15

Interstitial collagen catabolism. J Biol Chem (2013) 1.13

Active-site gating regulates substrate selectivity in a chymotrypsin-like serine protease the structure of haemophilus influenzae immunoglobulin A1 protease. J Mol Biol (2009) 1.12

Structure and reactivity of Trypanosoma brucei pteridine reductase: inhibition by the archetypal antifolate methotrexate. Mol Microbiol (2006) 1.11

The mechanism of inhibition of antibody-based inhibitors of membrane-type serine protease 1 (MT-SP1). J Mol Biol (2007) 1.10

Cleavage entropy as quantitative measure of protease specificity. PLoS Comput Biol (2013) 1.02

A new autocatalytic activation mechanism for cysteine proteases revealed by Prevotella intermedia interpain A. J Biol Chem (2007) 1.01

Coarse-grained description of protein internal dynamics: an optimal strategy for decomposing proteins in rigid subunits. Biophys J (2009) 0.99

Development of small molecules designed to modulate protein-protein interactions. J Comput Aided Mol Des (2006) 0.97

Macromolecular assembly-driven processing of the 2/3 cleavage site in the alphavirus replicase polyprotein. J Virol (2011) 0.97

Protein domain mimetics as in vivo modulators of hypoxia-inducible factor signaling. Proc Natl Acad Sci U S A (2013) 0.96

Pyrrolinone-based peptidomimetics. "Let the enzyme or receptor be the judge". Acc Chem Res (2010) 0.94

Prediction of protein cleavage site with feature selection by random forest. PLoS One (2012) 0.91

Engineering of substrate selectivity for tissue factor.factor VIIa complex signaling through protease-activated receptor 2. J Biol Chem (2010) 0.90

Differential P1 arginine and lysine recognition in the prototypical proprotein convertase Kex2. Proc Natl Acad Sci U S A (2007) 0.90

Anatomy of β-strands at protein-protein interfaces. ACS Chem Biol (2014) 0.89

A lead discovery strategy driven by a comprehensive analysis of proteases in the peptide substrate space. Protein Sci (2010) 0.88

Directed evolution of highly selective proteases by using a novel FACS-based screen that capitalizes on the p53 regulator MDM2. Chembiochem (2012) 0.88

Insights into the functionality of the putative residues involved in enterocin AS-48 maturation. Appl Environ Microbiol (2010) 0.87

Identification and partial characterization of extracellular aspartic protease genes from Metschnikowia pulcherrima IWBT Y1123 and Candida apicola IWBT Y1384. Appl Environ Microbiol (2012) 0.86

ALADYN: a web server for aligning proteins by matching their large-scale motion. Nucleic Acids Res (2010) 0.85

Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus. Bioorg Med Chem Lett (2013) 0.84

Factor Xa active site substrate specificity with substrate phage display and computational molecular modeling. J Biol Chem (2008) 0.84

Structural basis for activity regulation and substrate preference of clostridial collagenases G, H, and T. J Biol Chem (2013) 0.82

Engineering the substrate and inhibitor specificities of human coagulation Factor VIIa. Biochem J (2007) 0.82

Targets for Combating the Evolution of Acquired Antibiotic Resistance. Biochemistry (2015) 0.82

Truncated and helix-constrained peptides with high affinity and specificity for the cFos coiled-coil of AP-1. PLoS One (2013) 0.81

Engineering next generation proteases. Curr Opin Biotechnol (2009) 0.81

Evolutionary origins of a bioactive peptide buried within Preproalbumin. Plant Cell (2014) 0.81

Synthesis of peptide macrocycles using unprotected amino aldehydes. Nat Protoc (2010) 0.81

Lysine biosynthesis in bacteria: a metallodesuccinylase as a potential antimicrobial target. J Biol Inorg Chem (2012) 0.81

Prediction and Analysis of Post-Translational Pyruvoyl Residue Modification Sites from Internal Serines in Proteins. PLoS One (2013) 0.80

Identification of folding preferences of cleavage junctions of HIV-1 precursor proteins for regulation of cleavability. J Mol Model (2010) 0.79

Specificity determinants for autoproteolysis of LexA, a key regulator of bacterial SOS mutagenesis. Biochemistry (2014) 0.78

A computational approach for detecting peptidases and their specific inhibitors at the genome level. BMC Bioinformatics (2007) 0.78

Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 3CL Protease. J Med Chem (2016) 0.78

Recent Advances in the Discovery of Norovirus Therapeutics. J Med Chem (2015) 0.78

A Helix-Stabilizing Linker Improves Subcutaneous Bioavailability of a Helical Peptide Independent of Linker Lipophilicity. Bioconjug Chem (2016) 0.77

Allosteric inhibition of the neuropeptidase neurolysin. J Biol Chem (2014) 0.77

Structure-based design and synthesis of triazole-based macrocyclic inhibitors of norovirus protease: Structural, biochemical, spectroscopic, and antiviral studies. Eur J Med Chem (2016) 0.77

Comparison of the Internal Dynamics of Metalloproteases Provides New Insights on Their Function and Evolution. PLoS One (2015) 0.76

Heterocycles in peptidomimetics and pseudopeptides: design and synthesis. Pharmaceuticals (Basel) (2012) 0.75

Effects of FlAsH/tetracysteine (TC) Tag on PrP proteolysis and PrPres formation by TC-scanning. Chembiochem (2013) 0.75

Cysteine protease inhibition by nitrile-based inhibitors: a computational study. Front Chem (2013) 0.75

Design, synthesis, and evaluation of a novel series of macrocyclic inhibitors of norovirus 3CL protease. Eur J Med Chem (2016) 0.75

Protease Inhibitors in View of Peptide Substrate Databases. J Chem Inf Model (2016) 0.75

Characterizing Protease Specificity: How Many Substrates Do We Need? PLoS One (2015) 0.75

Peptide binding to a bacterial signal peptidase visualized by peptide tethering and carrier-driven crystallization. IUCrJ (2016) 0.75

Modulation of Backbone Flexibility for Effective Dissociation of Antibacterial and Hemolytic Activity in Cyclic Peptides. ACS Med Chem Lett (2016) 0.75

Salt bridge as a gatekeeper against partial unfolding. Protein Sci (2016) 0.75

A DFT study on the role of long range correlation interaction and solvent effects in homochiral and heterochiral cyclic trimerization of imidazole based heterocyclic amino acids. J Mol Model (2016) 0.75

Backbone hydrogen bond strengths can vary widely in transmembrane helices. J Am Chem Soc (2017) 0.75

Quantitative measurement of protease ligand conformation. J Comput Aided Mol Des (2008) 0.75

Protein Domain Mimics as Modulators of Protein-Protein Interactions. Acc Chem Res (2017) 0.75

Articles by these authors

MR1 presents microbial vitamin B metabolites to MAIT cells. Nature (2012) 3.71

The future of peptide-based drugs. Chem Biol Drug Des (2013) 3.41

Histone deacetylases as regulators of inflammation and immunity. Trends Immunol (2011) 2.18

Differential effects of selective HDAC inhibitors on macrophage inflammatory responses to the Toll-like receptor 4 agonist LPS. J Leukoc Biol (2010) 2.07

Antigen-loaded MR1 tetramers define T cell receptor heterogeneity in mucosal-associated invariant T cells. J Exp Med (2013) 2.04

Inflammatory lipid mediators in adipocyte function and obesity. Nat Rev Endocrinol (2010) 1.87

Structure, function and pathophysiology of protease activated receptors. Pharmacol Ther (2011) 1.81

Potencies of human immunodeficiency virus protease inhibitors in vitro against Plasmodium falciparum and in vivo against murine malaria. Antimicrob Agents Chemother (2006) 1.72

Recognition of vitamin B metabolites by mucosal-associated invariant T cells. Nat Commun (2013) 1.61

Beta-strand mimetics. Chem Rev (2004) 1.52

Intravenous immunoglobulin (IVIG) protects the brain against experimental stroke by preventing complement-mediated neuronal cell death. Proc Natl Acad Sci U S A (2007) 1.46

Histone deacetylase inhibitors in inflammatory disease. Curr Top Med Chem (2009) 1.46

Single turn peptide alpha helices with exceptional stability in water. J Am Chem Soc (2005) 1.42

A small molecule C5a receptor antagonist protects kidneys from ischemia/reperfusion injury in rats. Kidney Int (2003) 1.41

A potent human C5a receptor antagonist protects against disease pathology in a rat model of inflammatory bowel disease. J Immunol (2003) 1.40

Downsizing human, bacterial, and viral proteins to short water-stable alpha helices that maintain biological potency. Proc Natl Acad Sci U S A (2010) 1.38

Protease inhibitors in the clinic. Med Chem (2005) 1.33

Enzymatic characterization and homology model of a catalytically active recombinant West Nile virus NS3 protease. J Biol Chem (2004) 1.22

Cleavage of hemoglobin by hookworm cathepsin D aspartic proteases and its potential contribution to host specificity. FASEB J (2002) 1.20

A new paradigm for protein kinase inhibition: blocking phosphorylation without directly targeting ATP binding. Drug Discov Today (2007) 1.19

Antifibrotic activity of an inhibitor of histone deacetylases in DOCA-salt hypertensive rats. Br J Pharmacol (2010) 1.16

Toward drugs for protease-activated receptor 2 (PAR2). J Med Chem (2013) 1.12

Comparative anti-inflammatory activities of antagonists to C3a and C5a receptors in a rat model of intestinal ischaemia/reperfusion injury. Br J Pharmacol (2004) 1.11

An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats. FASEB J (2012) 1.11

Potent cationic inhibitors of West Nile virus NS2B/NS3 protease with serum stability, cell permeability and antiviral activity. J Med Chem (2008) 1.10

Structure of West Nile virus NS3 protease: ligand stabilization of the catalytic conformation. J Mol Biol (2008) 1.10

Protective effects of a potent C5a receptor antagonist on experimental acute limb ischemia-reperfusion in rats. J Surg Res (2004) 1.09

Insights to substrate binding and processing by West Nile Virus NS3 protease through combined modeling, protease mutagenesis, and kinetic studies. J Biol Chem (2006) 1.09

Protective effect of a new C5a receptor antagonist against ischemia-reperfusion injury in the rat small intestine. J Surg Res (2002) 1.08

Site-directed mutagenesis and kinetic studies of the West Nile Virus NS3 protease identify key enzyme-substrate interactions. J Biol Chem (2004) 1.06

Targeting histone deacetylase inhibitors for anti-malarial therapy. Curr Top Med Chem (2009) 1.06

Comparative protection against rat intestinal reperfusion injury by a new inhibitor of sPLA2, COX-1 and COX-2 selective inhibitors, and an LTC4 receptor antagonist. Br J Pharmacol (2003) 1.05

Antiarthritic activity of an orally active C5a receptor antagonist against antigen-induced monarticular arthritis in the rat. Arthritis Rheum (2002) 1.03

Modular alpha-helical mimetics with antiviral activity against respiratory syncitial virus. J Am Chem Soc (2006) 1.02

Protective effect of a human C5a receptor antagonist against hepatic ischaemia-reperfusion injury in rats. J Hepatol (2004) 1.01

Antagonism of protease-activated receptor 2 protects against experimental colitis. J Pharmacol Exp Ther (2011) 1.01

Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity. Mol Pharmacol (2004) 1.00

Novel agonists and antagonists for human protease activated receptor 2. J Med Chem (2010) 1.00

Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax. Antimicrob Agents Chemother (2010) 0.99

Over one hundred peptide-activated G protein-coupled receptors recognize ligands with turn structure. Chem Rev (2005) 0.99

D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. Chembiochem (2003) 0.99

Lysine acetylation in obesity, diabetes and metabolic disease. Immunol Cell Biol (2011) 0.98

Update 1 of: Proteases universally recognize beta strands in their active sites. Chem Rev (2010) 0.98

C5aR and C3aR antagonists each inhibit diet-induced obesity, metabolic dysfunction, and adipocyte and macrophage signaling. FASEB J (2012) 0.97

HDAC inhibitors: modulating leukocyte differentiation, survival, proliferation and inflammation. Immunol Cell Biol (2011) 0.96

Comparative agonist/antagonist responses in mutant human C5a receptors define the ligand binding site. J Biol Chem (2005) 0.95

The role of the N-terminal domain of the complement fragment receptor C5L2 in ligand binding. J Biol Chem (2006) 0.95

Antifibrotic activity of an inhibitor of group IIA secretory phospholipase A2 in young spontaneously hypertensive rats. J Immunol (2006) 0.95

In silico screening of small molecule libraries using the dengue virus envelope E protein has identified compounds with antiviral activity against multiple flaviviruses. Antiviral Res (2009) 0.94

Inflammatory responses induced by lipopolysaccharide are amplified in primary human monocytes but suppressed in macrophages by complement protein C5a. J Immunol (2013) 0.94

Antimalarial activity of the anticancer histone deacetylase inhibitor SB939. Antimicrob Agents Chemother (2012) 0.94

Hookworm aspartic protease, Na-APR-2, cleaves human hemoglobin and serum proteins in a host-specific fashion. J Infect Dis (2003) 0.94

Agonists and antagonists of protease activated receptors (PARs). Curr Med Chem (2006) 0.93

Mutagenesis of the West Nile virus NS2B cofactor domain reveals two regions essential for protease activity. J Gen Virol (2008) 0.92

Comparative gene expression profiling of P. falciparum malaria parasites exposed to three different histone deacetylase inhibitors. PLoS One (2012) 0.92

Mimetics of the peptide beta-strand. Mini Rev Med Chem (2002) 0.92

Nonpeptidic ligands for peptide-activated G protein-coupled receptors. Chem Rev (2007) 0.92

Diet-induced obesity, adipose inflammation, and metabolic dysfunction correlating with PAR2 expression are attenuated by PAR2 antagonism. FASEB J (2013) 0.92

Alpha-turn mimetics: short peptide alpha-helices composed of cyclic metallopentapeptide modules. J Am Chem Soc (2004) 0.92

Profiling gene expression induced by protease-activated receptor 2 (PAR2) activation in human kidney cells. PLoS One (2010) 0.92

Design, synthesis, potency, and cytoselectivity of anticancer agents derived by parallel synthesis from alpha-aminosuberic acid. J Med Chem (2006) 0.92

A cyclic beta-strand tripeptide with an alpha-helix like CD spectrum. Org Lett (2009) 0.91

Towards histone deacetylase inhibitors as new antimalarial drugs. Curr Pharm Des (2012) 0.91

Consecutive cyclic pentapeptide modules form short alpha-helices that are very stable to water and denaturants. Angew Chem Int Ed Engl (2004) 0.90

Countering cooperative effects in protease inhibitors using constrained beta-strand-mimicking templates in focused combinatorial libraries. J Med Chem (2004) 0.90

A convergent solution-phase synthesis of the macrocycle Ac-Phe-[Orn-Pro-D-Cha-Trp-Arg], a potent new antiinflammatory drug. J Org Chem (2003) 0.90

An inhibitor of phospholipase A2 group IIA modulates adipocyte signaling and protects against diet-induced metabolic syndrome in rats. Diabetes (2012) 0.90

Histone deacetylase 7 promotes Toll-like receptor 4-dependent proinflammatory gene expression in macrophages. J Biol Chem (2013) 0.89

Synthesis and structural properties of patellamide A derivatives and their copper(II) compounds. Chemistry (2002) 0.89

C5a, but not C5a-des Arg, induces upregulation of heteromer formation between complement C5a receptors C5aR and C5L2. Immunol Cell Biol (2013) 0.88

Generation and characterization of proteolytically active and highly stable truncated and full-length recombinant West Nile virus NS3. Protein Expr Purif (2006) 0.88

A potent and selective inhibitor of group IIa secretory phospholipase A2 protects rats from TNBS-induced colitis. Int Immunopharmacol (2005) 0.88

Inhibition of inflammation and fibrosis by a complement C5a receptor antagonist in DOCA-salt hypertensive rats. J Cardiovasc Pharmacol (2011) 0.88

Rv2969c, essential for optimal growth in Mycobacterium tuberculosis, is a DsbA-like enzyme that interacts with VKOR-derived peptides and has atypical features of DsbA-like disulfide oxidases. Acta Crystallogr D Biol Crystallogr (2013) 0.88

Comparative α-helicity of cyclic pentapeptides in water. Angew Chem Int Ed Engl (2014) 0.88

Inhibitors of cyclo-oxygenase-2 and secretory phospholipase A2 preserve bone architecture following ovariectomy in adult rats. Bone (2006) 0.87

Improving on nature: making a cyclic heptapeptide orally bioavailable. Angew Chem Int Ed Engl (2014) 0.87

An interaction between the methyltransferase and RNA dependent RNA polymerase domains of the West Nile virus NS5 protein. J Gen Virol (2013) 0.87

Antimalarial histone deacetylase inhibitors containing cinnamate or NSAID components. Bioorg Med Chem Lett (2010) 0.87

Update 1 of: Beta-strand mimetics. Chem Rev (2010) 0.87

C5a receptor (CD88) inhibition improves hypothermia-induced neuroprotection in an in vitro ischemic model. Neuromolecular Med (2012) 0.86

A refined agonist pharmacophore for protease activated receptor 2. Bioorg Med Chem Lett (2007) 0.86

Current status of short synthetic peptides as vaccines. Med Chem (2006) 0.86

Constraining cyclic peptides to mimic protein structure motifs. Angew Chem Int Ed Engl (2014) 0.85

Metal clips that induce unstructured pentapeptides to be alpha-helical in water. J Am Chem Soc (2009) 0.85

Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. J Med Chem (2004) 0.84

Crystal structures of highly constrained substrate and hydrolysis products bound to HIV-1 protease. Implications for the catalytic mechanism. Biochemistry (2008) 0.84

Total synthesis, structure, and oral absorption of a thiazole cyclic peptide, sanguinamide A. Org Lett (2012) 0.84

Beta-strand mimicking macrocyclic amino acids: templates for protease inhibitors with antiviral activity. J Med Chem (2002) 0.84

An mRNA atlas of G protein-coupled receptor expression during primary human monocyte/macrophage differentiation and lipopolysaccharide-mediated activation identifies targetable candidate regulators of inflammation. Immunobiology (2013) 0.84

Left- and right-handed alpha-helical turns in homo- and hetero-chiral helical scaffolds. J Am Chem Soc (2009) 0.83

Profiling the enzymatic properties and inhibition of human complement factor B. J Biol Chem (2007) 0.83

Conformationally homogeneous cyclic tetrapeptides: useful new three-dimensional scaffolds. J Am Chem Soc (2003) 0.82

Selective hexapeptide agonists and antagonists for human complement C3a receptor. J Med Chem (2010) 0.82

Formation of mononuclear and chloro-bridged binuclear copper(II) complexes of patellamide D, a naturally occurring cyclic peptide: influence of anion and solvent. J Inorg Biochem (2004) 0.82

Stereoelectronic effects dictate molecular conformation and biological function of heterocyclic amides. J Am Chem Soc (2014) 0.81

Rational design and synthesis of an orally bioavailable peptide guided by NMR amide temperature coefficients. Proc Natl Acad Sci U S A (2014) 0.81

A dual-purpose synthetic colloidal platform for protease mapping: substrate profiling for Dengue and West Nile virus proteases. Anal Biochem (2008) 0.81

Peptide inhibitors of the Escherichia coli DsbA oxidative machinery essential for bacterial virulence. J Med Chem (2014) 0.81