Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMI4FKH)

• Drug Name: lysophosphatidylethanolamine Drug Info
• Synonyms: monoacylglycerophosphoethanolamine

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 73755142
  TTD Drug ID: DMI4FKH

Molecule-Related Drug Atlas

Drug(s) Targeting Glucose-dependent insulinotropic receptor (GPR119)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Guanfacine extended release	DMB1CZ8	Attention deficit hyperactivity disorder	6A05.Z	Approved	[4]
DS-8500	DMUXIRM	Diabetic complication	5A2Y	Phase 2	[5]
SAR-260093	DMBJU2G	Type-2 diabetes	5A11	Phase 2	[6]
GSK1292263	DMDMXKQ	Gastric adenocarcinoma	2B72	Phase 2	[7]
BMS-903452	DM7JW0B	Type-2 diabetes	5A11	Phase 1	[8]
APD-597	DM36FOG	Type-2 diabetes	5A11	Phase 1	[9]
DA-1241	DMPJA64	Type 2 diabetes	5A11	Phase 1	[10]
APD668	DMN8R2U	Type-2 diabetes	5A11	Discontinued in Phase 1	[11]
PSN821	DMGEWUS	Type-2 diabetes	5A11	Terminated	[12]
N-oleoylethanolamide	DMJQ4L7	Discovery agent	N.A.	Investigative	[13]

Drug(s) Affected By CASP8 and FADD-like apoptosis regulator (CFLAR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Beta-carotene	DM0RXBT	Vitamin deficiency	5B55-5B71	Approved	[14]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[15]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[16]
Dactinomycin	DM2YGNW	Adult kidney Wilms tumor		Approved	[17]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[18]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[19]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[20]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[21]
Rifampicin	DM5DSFZ	Non-insulin dependent diabetes	5A11	Approved	[22]
Ethacrynic acid	DM60QMR	Edema	MG29	Approved	[23]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Glucose-dependent insulinotropic receptor (GPR119)	TT7QNVC	GP119_HUMAN	Agonist	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
CASP8 and FADD-like apoptosis regulator (CFLAR)	OTX14BAS	CFLAR_HUMAN	Gene/Protein Processing	[3]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5652).
• [2] Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor. Biochem Biophys Res Commun. 2005 Jan 28;326(4):744-51.
• [3] Ursodeoxycholyl lysophosphatidylethanolamide inhibits cholestasis- and hypoxia-induced apoptosis by upregulating antiapoptosis proteins. Exp Biol Med (Maywood). 2015 Feb;240(2):252-60. doi: 10.1177/1535370214547157. Epub 2014 Aug 14.
• [4] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 126).
• [5] Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31.
• [6] GPR119 agonists for the treatment of type 2 diabetes. Expert Opin Ther Pat. 2009 Oct;19(10):1339-59.
• [7] Gut hormone pharmacology of a novel GPR119 agonist (GSK1292263), metformin, and sitagliptin in type 2 diabetes mellitus: results from two randomized studies.PLoS One.2014 Apr 3;9(4):e92494.
• [8] Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119. J MedChem. 2014 Sep 25;57(18):7499-508.
• [9] Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-5.
• [10] ClinicalTrials.gov (NCT03646721) A Study to Evaluate the Safety, Tolerability, PK and PD of DA-1241 in Healthy Male Subjects and Subjects With T2DM. U.S. National Institutes of Health.
• [11] Announces Initiation of Phase 1 Clinical Trial of Arena Type 2 Diabetes Drug Candidate in Collaboration With Ortho-McNeil. Arena Pharmaceuticals, Inc. FEBRUARY 07, 2006.
• [12] Clinical pipeline report, company report or official report of Astellas Pharma (2011).
• [13] Screening beta-arrestin recruitment for the identification of natural ligands for orphan G-protein-coupled receptors. J Biomol Screen. 2013 Jun;18(5):599-609.
• [14] Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
• [15] PGK1 induction by a hydrogen peroxide treatment is suppressed by antioxidants in human colon carcinoma cells. Biosci Biotechnol Biochem. 2008 Jul;72(7):1799-808. doi: 10.1271/bbb.80079. Epub 2008 Jul 7.
• [16] Peripheral blood expression of nuclear factor-kappab-regulated genes is associated with rheumatoid arthritis disease activity and responds differentially to anti-tumor necrosis factor-alpha versus methotrexate. J Rheumatol. 2007 Sep;34(9):1817-22. Epub 2007 Aug 1.
• [17] Combination of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) and actinomycin D induces apoptosis even in TRAIL-resistant human pancreatic cancer cells. Clin Cancer Res. 2001 Feb;7(2):407-14.
• [18] Simvastatin induces apoptosis in human colon cancer cells and in tumor xenografts, and attenuates colitis-associated colon cancer in mice. Int J Cancer. 2008 Aug 15;123(4):951-7. doi: 10.1002/ijc.23593.
• [19] Quercetin potentiates apoptosis by inhibiting nuclear factor-kappaB signaling in H460 lung cancer cells. Biol Pharm Bull. 2013;36(6):944-51. doi: 10.1248/bpb.b12-01004.
• [20] Troglitazone sensitizes tumor cells to TRAIL-induced apoptosis via down-regulation of FLIP and Survivin. Apoptosis. 2006 Sep;11(9):1503-12. doi: 10.1007/s10495-006-8896-3.
• [21] Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
• [22] Rifampicin inhibits CD95-mediated apoptosis of Jurkat T cells via glucocorticoid receptors by modifying the expression of molecules regulating apoptosis. J Clin Immunol. 2002 Jan;22(1):37-47. doi: 10.1023/a:1014256603539.
• [23] Ethacrynic acid and a derivative enhance apoptosis in arsenic trioxide-treated myeloid leukemia and lymphoma cells: the role of glutathione S-transferase p1-1. Clin Cancer Res. 2012 Dec 15;18(24):6690-701. doi: 10.1158/1078-0432.CCR-12-0770. Epub 2012 Oct 18.