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

General Information of Drug (ID: DM0MO8I)

Drug Name
BQ-123 Drug Info
Synonyms
BQ-123; 136553-81-6; BQ123; BQ 123; Cyclo(D-trp-D-asp-pro-D-val-leu); UNII-S2A8YZM151; CHEBI:2965; S2A8YZM151; CHEMBL314691; cyclo[D-Trp-D-Asp-Pro-D-Val-Leu]; cyclo(D-Asp-Pro-D-Val-Leu-D-Trp); cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu); cyclo-[D-Asp-Pro-d-Val-Leu-d-Trp]; cyclo-(D-Asp-Pro-D-Val-Leu-D-Trp); Cyclo(D-trp-D-asp-L-pro-D-val-L-leu); Cyclo[D-trp-D-asp-L-pro-D-val-L-leu]; cyclo[(D)Trp-(D)Asp-Pro-(D)Val-Leu]; cyclo[D-Asp-L-Pro-D-Val-L-Leu-D-Trp]; cyclo(D-Asp-L-Pro-D-Val-L-Leu-D-Trp)
Indication
Disease Entry ICD 11 Status REF
Pulmonary arterial hypertension BB01.0 Phase 2 [1]
Cross-matching ID
PubChem CID
443289
ChEBI ID
CHEBI:2965
CAS Number
CAS 136553-81-6
TTD Drug ID
DM0MO8I
VARIDT Drug ID
DR01381

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Endothelin A receptor (EDNRA)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [7]
Ambrisentan DMD1QXW Pulmonary arterial hypertension BB01.0 Approved [8]
Macitentan DMP79A1 Cardiovascular disease BA00-BE2Z Approved [9]
Sparsentan DMMP51W IgA nephropathy MF8Y Approved [10]
LU302146 DMMJVXZ Pulmonary hypertension BB01 Approved [11]
Atrasentan DMM74PK Diabetic nephropathy GB61.Z Phase 3 [12]
Clazosentan DMQSBX4 Cerebral vasospasm BA85.Z Phase 3 [13]
PF-1228305 DMS1EQ7 Pulmonary hypertension BB01 Phase 3 [14]
Darusentan DMN8DQH Hypotension BA20-BA21 Phase 3 [15]
FR139317 DMEL5SV Hypertension BA00-BA04 Phase 2 [16]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Multidrug resistance-associated protein 2 (ABCC2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [17]
Methotrexate DM2TEOL Anterior urethra cancer Approved [18]
Folic Acid DMEMBJC Colorectal carcinoma Approved [19]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [20]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [21]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [22]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [23]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [24]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [25]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [26]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Organic anion transporting polypeptide 1B1 (SLCO1B1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [27]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [5]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [28]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [29]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [28]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [30]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [31]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [32]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [33]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [30]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Organic anion transporting polypeptide 1A2 (SLCO1A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [34]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [35]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [36]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [37]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [38]
Rosuvastatin DMMIQ7G Arteriosclerosis BD40 Approved [39]
Saquinavir DMG814N Human immunodeficiency virus infection 1C62 Approved [40]
Enalapril DMNFUZR Congestive heart failure BD10 Approved [41]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [42]
Liothyronine DM6IR3P Congenital hypothyroidism Approved [43]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Organic anion transporting polypeptide 1B3 (SLCO1B3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [44]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [28]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [45]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [46]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [28]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [47]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [31]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [33]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [48]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [33]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Endothelin-1 (EDN1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [49]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [50]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [51]
Methotrexate DM2TEOL Anterior urethra cancer Approved [52]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [53]
Quercetin DM3NC4M Obesity 5B81 Approved [54]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [55]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [56]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [57]
Lisinopril DMUOK4C Chronic heart failure BD1Z Approved [58]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Endothelin A receptor (EDNRA) TTKRD0G EDNRA_HUMAN Antagonist [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [3]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [4]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [5]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Endothelin-1 (EDN1) OTZCACEG EDN1_HUMAN Gene/Protein Processing [6]

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: 997).
2 Endothelin in heart failure: a promising therapeutic target Heart. 1997 Feb;77(2):93-4.
3 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
4 Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33.
5 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
6 Actions of endothelin and corticotropin releasing factor in the guinea-pig ileum: no evidence for an interaction with capsaicin-sensitive neurons. Neuropeptides. 2003 Aug;37(4):220-32. doi: 10.1016/s0143-4179(03)00048-9.
7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
8 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
9 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
10 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
11 Influence of endothelin receptor antagonists on myocardial protein kinase C isoforms in uraemic cardiomyopathy. Clin Sci (Lond). 2002 Aug;103 Suppl 48:276S-279S.
12 Effects of a selective ET(A)-receptor antagonist, atrasentan (ABT-627), in murine models of allergic asthma: demonstration of mouse strain specificity. Clin Sci (Lond). 2002 Aug;103 Suppl 48:367S-370S.
13 Effects of the selective endothelin A (ET(A)) receptor antagonist Clazosentan on cerebral perfusion and cerebral oxygenation following severe subar... Acta Neurochir (Wien). 2007;149(9):911-8; discussion 918.
14 Pfizer. Product Development Pipeline. March 31 2009.
15 Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats. J Cardiovasc Pharmacol. 2006 Mar;47(3):456-62.
16 Reduction of bFGF-induced smooth muscle cell proliferation and endothelin receptor mRNA expression by mevastatin and atorvastatin. Biochem Pharmacol. 2002 Aug 1;64(3):497-505.
17 Involvement of the drug transporters p glycoprotein and multidrug resistance-associated protein Mrp2 in telithromycin transport. Antimicrob Agents Chemother. 2006 Jan;50(1):80-7.
18 Dose-dependent disposition of methotrexate in Abcc2 and Abcc3 gene knockout murine models. Drug Metab Dispos. 2011 Nov;39(11):2155-61.
19 Mammalian multidrug-resistance proteins (MRPs). Essays Biochem. 2011 Sep 7;50(1):179-207.
20 Enhancing chemosensitivity in oral squamous cell carcinoma by lentivirus vector-mediated RNA interference targeting EGFR and MRP2. Oncol Lett. 2016 Sep;12(3):2107-2114.
21 Multidrug resistance associated protein 2 mediates transport of prostaglandin E2. Liver Int. 2006 Apr;26(3):362-8.
22 Lentivirus-mediated RNAi silencing targeting ABCC2 increasing the sensitivity of a human nasopharyngeal carcinoma cell line against cisplatin. J Transl Med. 2008 Oct 4;6:55.
23 Effect of acetaminophen on expression and activity of rat liver multidrug resistance-associated protein 2 and P-glycoprotein. Biochem Pharmacol. 2004 Aug 15;68(4):791-8.
24 Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7.
25 Delineating the contribution of secretory transporters in the efflux of etoposide using Madin-Darby canine kidney (MDCK) cells overexpressing P-glycoprotein (Pgp), multidrug resistance-associated protein (MRP1), and canalicular multispecific organic anion transporter (cMOAT). Drug Metab Dispos. 2002 Apr;30(4):457-63.
26 Multidrug Resistance-Associated Protein 2 (MRP2) Mediated Transport of Oxaliplatin-Derived Platinum in Membrane Vesicles. PLoS One. 2015 Jul 1;10(7):e0130727.
27 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
28 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
29 Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
30 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
31 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
32 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
33 FDA Drug Development and Drug Interactions
34 Interaction of methotrexate with organic-anion transporting polypeptide 1A2 and its genetic variants. J Pharmacol Exp Ther. 2006 Aug;318(2):521-9.
35 Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3. Pflugers Arch. 2001 Nov;443(2):188-95.
36 Environmental and genetic factors affecting transport of imatinib by OATP1A2. Clin Pharmacol Ther. 2011 Jun;89(6):816-20.
37 Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1. Biochem Pharmacol. 2010 Dec 1;80(11):1746-53.
38 Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
39 Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806.
40 Human organic anion-transporting polypeptide OATP-A (SLC21A3) acts in concert with P-glycoprotein and multidrug resistance protein 2 in the vectorial transport of Saquinavir in Hep G2 cells. Mol Pharm. 2004 Jan 12;1(1):49-56.
41 Uptake of enalapril and expression of organic anion transporting polypeptide 1 in zonal, isolated rat hepatocytes. Drug Metab Dispos. 2000 Jul;28(7):801-6.
42 Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver. Gastroenterology. 1995 Oct;109(4):1274-82.
43 Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Endocrinology. 2001 May;142(5):2005-12.
44 LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001 Jun;120(7):1689-99.
45 Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008 Apr 14;584(1):57-65.
46 Influence of non-steroidal anti-inflammatory drugs on organic anion transporting polypeptide (OATP) 1B1- and OATP1B3-mediated drug transport. Drug Metab Dispos. 2011 Jun;39(6):1047-53.
47 Relevance of conserved lysine and arginine residues in transmembrane helices for the transport activity of organic anion transporting polypeptide 1B3. Br J Pharmacol. 2010 Feb 1;159(3):698-708.
48 Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
49 ?-adrenoceptors and muscarinic receptors mediate opposing effects on endothelin-1 expression in human lung fibroblasts. Eur J Pharmacol. 2012 Sep 15;691(1-3):218-24. doi: 10.1016/j.ejphar.2012.07.002. Epub 2012 Jul 13.
50 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
51 Induction of endothelin-1 expression by oxidative stress in vascular smooth muscle cells. Cardiovasc Pathol. 2001 Nov-Dec;10(6):311-5. doi: 10.1016/s1054-8807(01)00095-3.
52 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
53 [Effect of simvastatin on endothelin-1 expression in endothelial cell cultured hypoxically]. Sichuan Da Xue Xue Bao Yi Xue Ban. 2008 Jan;39(1):72-5.
54 Effects of dietary polyphenols on gene expression in human vascular endothelial cells. Proc Nutr Soc. 2008 Feb;67(1):42-7.
55 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
56 Nucleoside reverse transcriptase inhibitors induce a mitophagy-associated endothelial cytotoxicity that is reversed by coenzyme Q10 cotreatment. Toxicol Sci. 2013 Aug;134(2):323-34. doi: 10.1093/toxsci/kft105. Epub 2013 May 2.
57 Cardiac toxicity of high-dose cyclophosphamide in patients with multiple myeloma undergoing autologous hematopoietic stem cell transplantation. Int J Hematol. 2007 Jun;85(5):408-14. doi: 10.1532/IJH97.E0620.
58 Different effects of angiotensin converting enzyme inhibitors on endothelin-1 and nitric oxide balance in human vascular endothelial cells: evidence of an oxidant-sensitive pathway. Mediators Inflamm. 2008;2008:305087. doi: 10.1155/2008/305087. Epub 2008 Dec 1.