Published in Chem Rev on April 12, 2010
Extension of the CHARMM General Force Field to sulfonyl-containing compounds and its utility in biomolecular simulations. J Comput Chem (2012) 1.20
Structure-Based Design of Inhibitors of Protein-Protein Interactions: Mimicking Peptide Binding Epitopes. Angew Chem Int Ed Engl (2015) 1.17
Small molecules, big targets: drug discovery faces the protein-protein interaction challenge. Nat Rev Drug Discov (2016) 0.93
Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions. J Am Chem Soc (2011) 0.93
Ste24p Mediates Proteolysis of Both Isoprenylated and Non-prenylated Oligopeptides. J Biol Chem (2016) 0.84
Substituted imidazo[1,2-a]pyridines as β-strand peptidomimetics. Org Lett (2012) 0.79
Systematic Targeting of Protein-Protein Interactions. Trends Pharmacol Sci (2016) 0.79
Structural modifications of (Z)-3-(2-aminoethyl)-5-(4-ethoxybenzylidene)thiazolidine-2,4-dione that improve selectivity for inhibiting the proliferation of melanoma cells containing active ERK signaling. Org Biomol Chem (2013) 0.76
The membrane anchor of the transcriptional activator SREBP is characterized by intrinsic conformational flexibility. Proc Natl Acad Sci U S A (2015) 0.75
Protein Domain Mimics as Modulators of Protein-Protein Interactions. Acc Chem Res (2017) 0.75
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
The toxicogenomic multiverse: convergent recruitment of proteins into animal venoms. Annu Rev Genomics Hum Genet (2009) 2.30
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
Proteases universally recognize beta strands in their active sites. Chem Rev (2005) 1.90
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
Isolation and characterization of a cone snail protease with homology to CRISP proteins of the pathogenesis-related protein superfamily. J Biol Chem (2003) 1.44
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
Architecture of a single membrane spanning cytochrome P450 suggests constraints that orient the catalytic domain relative to a bilayer. Proc Natl Acad Sci U S A (2014) 1.23
Enzymatic characterization and homology model of a catalytically active recombinant West Nile virus NS3 protease. J Biol Chem (2004) 1.22
Targeting protein-protein interactions: suppression of Stat3 dimerization with rationally designed small-molecule, nonpeptidic SH2 domain binders. Chembiochem (2008) 1.21
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
Direct modification of the proinflammatory cytokine macrophage migration inhibitory factor by dietary isothiocyanates. J Biol Chem (2009) 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
Cannabinoid CB1 and CB2 receptor ligand specificity and the development of CB2-selective agonists. Curr Med Chem (2008) 1.05
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
Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics. Bioorg Med Chem Lett (2007) 1.01
Abc1p is a multidrug efflux transporter that tips the balance in favor of innate azole resistance in Candida krusei. Antimicrob Agents Chemother (2008) 1.01
Antagonism of protease-activated receptor 2 protects against experimental colitis. J Pharmacol Exp Ther (2011) 1.01
Protective effect of a human C5a receptor antagonist against hepatic ischaemia-reperfusion injury in rats. J Hepatol (2004) 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
D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. Chembiochem (2003) 0.99
Over one hundred peptide-activated G protein-coupled receptors recognize ligands with turn structure. Chem Rev (2005) 0.99
A novel class of anticancer compounds targets the actin cytoskeleton in tumor cells. Cancer Res (2013) 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
Honey bee dopamine and octopamine receptors linked to intracellular calcium signaling have a close phylogenetic and pharmacological relationship. PLoS One (2011) 0.94
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
Nonpeptidic ligands for peptide-activated G protein-coupled receptors. Chem Rev (2007) 0.92
Mimetics of the peptide beta-strand. Mini Rev Med Chem (2002) 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
Variable Expression of GLIPR1 Correlates with Invasive Potential in Melanoma Cells. Front Oncol (2013) 0.91
A cyclic beta-strand tripeptide with an alpha-helix like CD spectrum. Org Lett (2009) 0.91
Specific interactions between the Candida albicans ABC transporter Cdr1p ectodomain and a D-octapeptide derivative inhibitor. Mol Microbiol (2012) 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
Identification of a serine protease inhibitor which causes inclusion vacuole reduction and is lethal to Chlamydia trachomatis. Mol Microbiol (2013) 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
Mode of binding of methyl acceptor substrates to the adrenaline-synthesizing enzyme phenylethanolamine N-methyltransferase: implications for catalysis. Biochemistry (2005) 0.89
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
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
Inhibition of inflammation and fibrosis by a complement C5a receptor antagonist in DOCA-salt hypertensive rats. J Cardiovasc Pharmacol (2011) 0.88
A potent and selective inhibitor of group IIa secretory phospholipase A2 protects rats from TNBS-induced colitis. Int Immunopharmacol (2005) 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