What's all the FLAP about?: 5-lipoxygenase-activating protein inhibitors for inflammatory diseases
JF Evans, AD Ferguson, RT Mosley… - Trends in …, 2008 - cell.com
Leukotrienes have physiological roles in innate immune responses and pathological roles in
inflammatory diseases, such as asthma, allergic rhinitis and atherosclerosis. Anti-leukotriene …
inflammatory diseases, such as asthma, allergic rhinitis and atherosclerosis. Anti-leukotriene …
A novel, orally active LPA1 receptor antagonist inhibits lung fibrosis in the mouse bleomycin model
JS Swaney, C Chapman, LD Correa… - British journal of …, 2010 - Wiley Online Library
Background and purpose: The aim of this study was to assess the potential of an antagonist
selective for the lysophosphatidic acid receptor, LPA1, in treating lung fibrosis We evaluated …
selective for the lysophosphatidic acid receptor, LPA1, in treating lung fibrosis We evaluated …
Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung
KJ Stebbins, AR Broadhead, CS Baccei, JM Scott… - … of Pharmacology and …, 2010 - ASPET
Prostaglandin D2 (PGD2) is one of a family of biologically active lipids derived from
arachidonic acid via the action of COX-1 and COX-2. PGD2 is released from mast cells and …
arachidonic acid via the action of COX-1 and COX-2. PGD2 is released from mast cells and …
Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist
JS Swaney, C Chapman, LD Correa, KJ Stebbins… - … of Pharmacology and …, 2011 - ASPET
Lysophosphatidic acid (LPA) is a bioactive phospholipid that signals through a family of at
least six G protein-coupled receptors designated LPA1–6. LPA type 1 receptor (LPA1) …
least six G protein-coupled receptors designated LPA1–6. LPA type 1 receptor (LPA1) …
Nonpeptide αvβ3 Antagonists. Part 11: Discovery and Preclinical Evaluation of Potent αvβ3 Antagonists for the Prevention and Treatment of Osteoporosis
PJ Coleman, KM Brashear, BC Askew… - Journal of medicinal …, 2004 - ACS Publications
3-(S)-Pyrimidin-5-yl-9-(5, 6, 7, 8-tetrahydro-[1, 8] naphthyridin-2-yl)-nonanoic acid (5e) and 3-
(S)-(methylpyrimidin-5-yl)-9-(5, 6, 7, 8-tetrahydro-[1, 8] naphthyridin-2-yl)-nonanoic acid (5f) …
(S)-(methylpyrimidin-5-yl)-9-(5, 6, 7, 8-tetrahydro-[1, 8] naphthyridin-2-yl)-nonanoic acid (5f) …
Structural basis for inhibition of human autotaxin by four potent compounds with distinct modes of binding
AJ Stein, G Bain, P Prodanovich, AM Santini… - Molecular …, 2015 - ASPET
Autotaxin (ATX) is a secreted enzyme that hydrolyzes lysophosphatidylcholine to
lysophosphatidic acid (LPA). LPA is a bioactive phospholipid that regulates diverse …
lysophosphatidic acid (LPA). LPA is a bioactive phospholipid that regulates diverse …
Identification of 4-(aminomethyl)-6-(trifluoromethyl)-2-(phenoxy) pyridine derivatives as potent, selective, and orally efficacious inhibitors of the copper-dependent …
MW Rowbottom, G Bain, I Calderon… - Journal of medicinal …, 2017 - ACS Publications
LOXL2 catalyzes the oxidative deamination of ε-amines of lysine and hydroxylysine residues
within collagen and elastin, generating reactive aldehydes (allysine). Condensation with …
within collagen and elastin, generating reactive aldehydes (allysine). Condensation with …
Small molecule lysyl oxidase-like 2 (LOXL2) inhibitors: the identification of an inhibitor selective for LOXL2 over LOX
JH Hutchinson, MW Rowbottom… - ACS medicinal …, 2017 - ACS Publications
Two series of novel LOXL2 enzyme inhibitors are described: benzylamines substituted with
electron withdrawing groups at the para-position and 2-substituted pyridine-4 …
electron withdrawing groups at the para-position and 2-substituted pyridine-4 …
Selective inhibition of autotaxin is efficacious in mouse models of liver fibrosis
G Bain, KE Shannon, F Huang, J Darlington… - … of Pharmacology and …, 2017 - ASPET
Autotaxin (ATX) is a secreted glycoprotein that converts lysophosphatidylcholine (LPC) to
the bioactive phospholipid lysophosphatidic acid (LPA) and is the major enzyme generating …
the bioactive phospholipid lysophosphatidic acid (LPA) and is the major enzyme generating …
Nonpeptide αvβ3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent αvβ3 Antagonist for the Prevention and Treatment of Osteoporosis
JH Hutchinson, W Halczenko… - Journal of medicinal …, 2003 - ACS Publications
3 (S)-(6-Methoxypyridin-3-yl)-3-{2-oxo-3-[3-(5, 6, 7, 8-tetrahydro-[1, 8]-naphthyridin-2-yl)
propyl] imidazolidin-1-yl} propionic acid 6 was identified as a potent and selective antagonist …
propyl] imidazolidin-1-yl} propionic acid 6 was identified as a potent and selective antagonist …