Published in Bioorg Med Chem Lett on January 11, 2008
Reduction of nitrite to nitric oxide during ischemia protects against myocardial ischemia-reperfusion damage. Proc Natl Acad Sci U S A (2004) 3.23
ADAMs 10 and 17 represent differentially regulated components of a general shedding machinery for membrane proteins such as transforming growth factor alpha, L-selectin, and tumor necrosis factor alpha. Mol Biol Cell (2009) 2.46
Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1. Antimicrob Agents Chemother (2005) 2.07
Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther (2010) 1.93
Murine CXCR1 is a functional receptor for GCP-2/CXCL6 and interleukin-8/CXCL8. J Biol Chem (2006) 1.79
Prostate cancer-associated mutations in speckle-type POZ protein (SPOP) regulate steroid receptor coactivator 3 protein turnover. Proc Natl Acad Sci U S A (2013) 1.66
Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening. Mol Cancer Ther (2011) 1.51
ADAM17 is regulated by a rapid and reversible mechanism that controls access to its catalytic site. J Cell Sci (2010) 1.49
A new class of potent matrix metalloproteinase 13 inhibitors for potential treatment of osteoarthritis: Evidence of histologic and clinical efficacy without musculoskeletal toxicity in rat models. Arthritis Rheum (2009) 1.38
Subtype-specific beta-adrenoceptor signaling pathways in the heart and their potential clinical implications. Trends Pharmacol Sci (2004) 1.38
Small-molecule antagonists for CXCR2 and CXCR1 inhibit human melanoma growth by decreasing tumor cell proliferation, survival, and angiogenesis. Clin Cancer Res (2009) 1.34
A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation. J Pharmacol Exp Ther (2007) 1.30
P2Y(13): identification and characterization of a novel Galphai-coupled ADP receptor from human and mouse. J Pharmacol Exp Ther (2002) 1.22
A novel cannabinoid peripheral cannabinoid receptor-selective inverse agonist blocks leukocyte recruitment in vivo. J Pharmacol Exp Ther (2005) 1.20
The pyrimidinergic P2Y6 receptor mediates a novel release of proinflammatory cytokines and chemokines in monocytic cells stimulated with UDP. Biochem Biophys Res Commun (2005) 1.19
Small molecule antagonists for CXCR2 and CXCR1 inhibit human colon cancer liver metastases. Cancer Lett (2010) 1.18
Short-chain fatty acids act as antiinflammatory mediators by regulating prostaglandin E(2) and cytokines. World J Gastroenterol (2009) 1.10
Disruption of CCL21-induced chemotaxis in vitro and in vivo by M3, a chemokine-binding protein encoded by murine gammaherpesvirus 68. J Virol (2003) 1.10
Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism. Bioorg Med Chem (2013) 1.07
Pharmacological characterization of Sch527123, a potent allosteric CXCR1/CXCR2 antagonist. J Pharmacol Exp Ther (2007) 1.05
Pharmacological analysis of calcium responses mediated by the human A3 adenosine receptor in monocyte-derived dendritic cells and recombinant cells. Mol Pharmacol (2003) 1.05
A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection. BMC Immunol (2012) 1.02
CCR2 and CXCR4 regulate peripheral blood monocyte pharmacodynamics and link to efficacy in experimental autoimmune encephalomyelitis. J Inflamm (Lond) (2009) 1.02
Small molecule chemokine mimetics suggest a molecular basis for the observation that CXCL10 and CXCL11 are allosteric ligands of CXCR3. Br J Pharmacol (2012) 0.99
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist. J Med Chem (2006) 0.99
Activation and functional significance of the renin-angiotensin system in mice with cardiac restricted overexpression of tumor necrosis factor. Circulation (2003) 0.96
Stereoselective synthesis of L-oliose trisaccharide via iterative alkynol cycloisomerization and acid-catalyzed glycosylation. Org Lett (2002) 0.93
Structure-guided discovery of cyclin-dependent kinase inhibitors. Biopolymers (2008) 0.91
Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis. Biochem Biophys Res Commun (2009) 0.91
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket. Bioorg Med Chem Lett (2008) 0.90
Homologous and heterologous regulation of somatostatin receptor 2. Mol Endocrinol (2002) 0.90
Thymic stromal lymphopoietin receptor blockade reduces allergic inflammation in a cynomolgus monkey model of asthma. J Allergy Clin Immunol (2013) 0.89
Synthesis and structure-activity relationships of 3,4-diaminocyclobut-3-ene-1,2-dione CXCR2 antagonists. Bioorg Med Chem Lett (2006) 0.87
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists. Bioorg Med Chem Lett (2007) 0.86
Induction of lysosomal and plasma membrane-bound sialidases in human T-cells via T-cell receptor. Biochem J (2004) 0.86
A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors. Bioorg Med Chem Lett (2011) 0.85
IK682, a tight binding inhibitor of TACE. Arch Biochem Biophys (2006) 0.85
Effect of Chinese drugs for supplementing Qi, nourishing Yin and activating blood circulation on myocardial perfusion in patients with acute myocardial infarction after revascularization. Chin J Integr Med (2009) 0.84
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1. Bioorg Med Chem Lett (2011) 0.84
Identification of CXCR3 receptor agonists in combinatorial small-molecule libraries. Biochem Biophys Res Commun (2006) 0.84
CXCR2 receptor antagonists: a medicinal chemistry perspective. Curr Top Med Chem (2014) 0.84
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors. Bioorg Med Chem Lett (2013) 0.84
Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors. Bioorg Med Chem Lett (2011) 0.84
Activation of glibenclamide-sensitive ATP-sensitive K+ channels during β-adrenergically induced metabolic stress produces a substrate for atrial tachyarrhythmia. Circ Arrhythm Electrophysiol (2012) 0.82
Pharmacological characterization of the chemokine receptor, hCCR1 in a stable transfectant and differentiated HL-60 cells: antagonism of hCCR1 activation by MIP-1beta. Br J Pharmacol (2002) 0.82
Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2. Bioorg Med Chem Lett (2007) 0.82
Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach. Bioorg Med Chem Lett (2013) 0.82
The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists. Bioorg Med Chem Lett (2005) 0.82
Mutation spectrum in a large cohort of unrelated Chinese patients with hypertrophic cardiomyopathy. Am J Cardiol (2013) 0.82
Identification of full, partial and inverse CC chemokine receptor 3 agonists using [35S]GTPgammaS binding. Eur J Pharmacol (2002) 0.82
A role for histamine in cytokine modulation by the adenosine A(3) receptor agonist, 2-Cl-IB-MECA. Eur J Pharmacol (2002) 0.82
Pharmacological characterization of human S1P4 using a novel radioligand, [4,5-3H]-dihydrosphingosine-1-phosphate. Br J Pharmacol (2004) 0.81
Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors. Bioorg Med Chem Lett (2012) 0.81
EC144 is a potent inhibitor of the heat shock protein 90. J Med Chem (2012) 0.81