Gastric mucosal defense and cytoprotection: bench to bedside.
- L. Laine, K. Takeuchi, A. Tarnawski
- Medicine, BiologyGastroenterology
- 1 July 2008
Conditions in which mucosal injury is directly related to impairment in mucosal defense are discussed, focusing on disorders with important clinical sequelae: nonsteroidal anti-inflammatory drug (NSAID)-associated injury, which is primarily related to inhibition of cyclooxygenase-mediated PG synthesis, and stress-related mucosal disease (SRMD), which occurs with local ischemia.
Pathogenesis of NSAID-induced gastric damage: importance of cyclooxygenase inhibition and gastric hypermotility.
- K. Takeuchi
- MedicineWorld Journal of Gastroenterology
- 14 May 2012
Gastric hypermotility plays a primary role in the pathogenesis of NSAID-induced gastric damage, and the response, causally related with PG deficiency due to COX-1 inhibition, occurs prior to other pathogenic events such as increased mucosal permeability.
Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.
- N. Negoro, Shinobu Sasaki, Y. Momose
- Chemistry, BiologyACS Medicinal Chemistry Letters
- 18 June 2010
Dihydrobenzofuran derivative 9a showed potent plasma glucose-lowering action and insulinotropic action during an oral glucose tolerance test in female Wistar fatty rats with impaired glucose tolerance, and is currently in clinical trials for the treatment of type 2 diabetes mellitus.
Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.
- Jun Feng, Zhiyuan Zhang, S. L. Gwaltney
- Biology, ChemistryJournal of Medicinal Chemistry
- 19 April 2007
Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) and related quinazolinone-based DPP-4 inhibitors provide sustained reduction of plasma D PP-4 activity and a lowering of blood glucose in animal models of diabetes.
Probiotic Lactobacillus casei strain Shirota prevents indomethacin-induced small intestinal injury: involvement of lactic acid.
- Toshio Watanabe, H. Nishio, T. Arakawa
- Biology, MedicineAmerican Journal of Physiology - Gastrointestinal…
- 1 September 2009
LcS exhibits a prophylactic effect on indomethacin-induced enteropathy by suppressing the LPS/TLR4 signaling pathway and that this probiotic effect of LcS may be mediated by L-lactic acid.
TAK-875, an Orally Available G Protein-Coupled Receptor 40/Free Fatty Acid Receptor 1 Agonist, Enhances Glucose-Dependent Insulin Secretion and Improves Both Postprandial and Fasting Hyperglycemia in…
- Y. Tsujihata, R. Ito, K. Takeuchi
- Medicine, BiologyJournal of Pharmacology and Experimental…
- 1 October 2011
TAK-875 enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia with a low risk of hypoglycemia and no evidence of β cell toxicity.
Inhibition of both COX-1 and COX-2 is required for development of gastric damage in response to nonsteroidal antiinflammatory drugs
- A. Tanaka, H. Araki, Y. Komoike, S. Hase, K. Takeuchi
- MedicineJournal of Physiology - Paris
- 31 December 2001
Role of Cyclooxygenase (COX)-1 and COX-2 Inhibition in Nonsteroidal Anti-Inflammatory Drug-Induced Intestinal Damage in Rats: Relation to Various Pathogenic Events
- A. Tanaka, S. Hase, T. Miyazawa, R. Ohno, K. Takeuchi
- MedicineJournal of Pharmacology and Experimental…
- 1 December 2002
Indomethacin decreased mucosal prostaglandin (PG)E2 content and caused damage in the intestine within 24 h, accompanied by an increase in intestinal contractility, bacterial numbers, myeloperoxidase (MPO) and inducible nitric-oxide synthase (iNOS) activity, and intestinal motility, which explains why intestinal damage occurs only when bothCOX-1 and COX-2 are inhibited.
A Novel Antidiabetic Drug, Fasiglifam/TAK-875, Acts as an Ago-Allosteric Modulator of FFAR1
- Chiori Yabuki, H. Komatsu, M. Mori
- Biology, MedicinePLoS ONE
- 10 October 2013
It is demonstrated that fasiglifam acts as an ago-allosteric modulator of FFAR1 that exerts its effects by acting cooperatively with endogenous plasma FFAs in human patients as well as diabetic animals.
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