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1.
Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies.
Bioorg Med Chem Lett
; 29(3): 503-508, 2019 02 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-30594433
2.
A Selective Novel Peroxisome Proliferator-Activated Receptor (PPAR)-α Antagonist Induces Apoptosis and Inhibits Proliferation of CLL Cells In Vitro and In Vivo.
Mol Med
; 21: 410-9, 2015 Jun 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-26070013
3.
Identification of the first potent, selective and bioavailable PPARα antagonist.
Bioorg Med Chem Lett
; 24(10): 2267-72, 2014 May 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-24745969
4.
First-in-human Phase I Trial of TPST-1120, an Inhibitor of PPARα, as Monotherapy or in Combination with Nivolumab, in Patients with Advanced Solid Tumors.
Cancer Res Commun
; 4(4): 1100-1110, 2024 Apr 18.
Artículo
en Inglés
| MEDLINE | ID: mdl-38551394
5.
Dual Blockade of EP2 and EP4 Signaling is Required for Optimal Immune Activation and Antitumor Activity Against Prostaglandin-Expressing Tumors.
Cancer Res Commun
; 3(8): 1486-1500, 2023 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-37559947
6.
DP2 (CRTh2) antagonism reduces ocular inflammation induced by allergen challenge and respiratory syncytial virus.
Int Arch Allergy Immunol
; 157(3): 259-68, 2012.
Artículo
en Inglés
| MEDLINE | ID: mdl-22042170
7.
Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation.
J Pharmacol Exp Ther
; 338(1): 290-301, 2011 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-21487069
8.
Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.
Bioorg Med Chem Lett
; 21(21): 6608-12, 2011 Nov 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-21958540
9.
Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.
Bioorg Med Chem Lett
; 21(3): 1036-40, 2011 Feb 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-21211969
10.
Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung.
J Pharmacol Exp Ther
; 332(3): 764-75, 2010 Mar.
Artículo
en Inglés
| MEDLINE | ID: mdl-19996299
11.
5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.
Bioorg Med Chem Lett
; 20(15): 4598-601, 2010 Aug 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-20566292
12.
5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.
Bioorg Med Chem Lett
; 20(1): 213-7, 2010 Jan 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-19914828
13.
Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.
Bioorg Med Chem Lett
; 19(3): 834-6, 2009 Feb 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-19097777
14.
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
Bioorg Med Chem Lett
; 19(16): 4647-51, 2009 Aug 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-19608418
15.
In vitro and in vivo pharmacology of NXT629, a novel and selective PPARα antagonist.
Eur J Pharmacol
; 809: 130-140, 2017 Aug 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-28483457
16.
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
J Med Chem
; 48(24): 7520-34, 2005 Dec 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-16302794
17.
A novel class of nonpeptidic biaryl inhibitors of human cathepsin K.
J Med Chem
; 46(17): 3709-27, 2003 Aug 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-12904076
18.
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.
J Med Chem
; 54(23): 8013-29, 2011 Dec 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-22059882
19.
Therapeutic efficacy of AM156, a novel prostanoid DP2 receptor antagonist, in murine models of allergic rhinitis and house dust mite-induced pulmonary inflammation.
Eur J Pharmacol
; 638(1-3): 142-9, 2010 Jul 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-20447387
20.
Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation.
Eur J Pharmacol
; 640(1-3): 211-8, 2010 Aug 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-20519143