Target Information

Target General Infomation
Target ID
T58589
Former ID
TTDR00405
Target Name
B1 bradykinin receptor
Gene Name
BDKRB1
Synonyms
B1R; BK-1 receptor; Bradykinin subtype 1receptor; BDKRB1
Target Type
Clinical Trial
Disease Diabetic macular edema [ICD9: 250, 362.01, 362.07, 362.53, 782.3; ICD10: E08-E13, E08.3, E09.3, E10.3, E11.3, E13.3, H35.8, R60.9]
Osteoarthritis [ICD9: 715; ICD10: M15-M19, M47]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Function
This is a receptor for bradykinin. Could be a factor in chronic pain and inflammation.
BioChemical Class
GPCR rhodopsin
Target Validation
T58589
UniProt ID
P46663
Sequence
MASSWPPLELQSSNQSQLFPQNATACDNAPEAWDLLHRVLPTFIISICFFGLLGNLFVLL
VFLLPRRQLNVAEIYLANLAASDLVFVLGLPFWAENIWNQFNWPFGALLCRVINGVIKAN
LFISIFLVVAISQDRYRVLVHPMASRRQQRRRQARVTCVLIWVVGGLLSIPTFLLRSIQA
VPDLNITACILLLPHEAWHFARIVELNILGFLLPLAAIVFFNYHILASLRTREEVSRTRC
GGRKDSKTTALILTLVVAFLVCWAPYHFFAFLEFLFQVQAVRGCFWEDFIDLGLQLANFF
AFTNSSLNPVIYVFVGRLFRTKVWELYKQCTPKSLAPISSSHRKEIFQLFWRN
Drugs and Mode of Action
Drug(s) Safotibant Drug Info Phase 2 Diabetic macular edema [523403]
SSR-240612 Drug Info Phase 2 Rheumatoid arthritis [541730], [547525]
BI 113823 Drug Info Phase 1 Osteoarthritis [523181]
Modulator BI 113823 Drug Info [532906]
Safotibant Drug Info [551643]
Antagonist Des-Arg(9)-[Leu(8)]-BK Drug Info [535320]
NVP-SAA164 Drug Info [541709]
SSR-240612 Drug Info [531635], [544033]
Inhibitor Des-Arg10-Kallidin Drug Info [527294]
Des-Arg10-Leu9-Kallidin Drug Info [527294]
H-DArg-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH(JMV1638) Drug Info [525817]
H-DArg-Arg-Pro-Hyp-Gly-Thi-Ser-D-BT-OH(JMV1431) Drug Info [525817]
H-Lys-Arg-Pro-Hyp-Gly-Igl-Ser-D-BT-OH(JMV1645) Drug Info [525817]
H-Lys-Arg-Pro-Hyp-Gly-Thi-Ser-D-BT-OH(JMV1669) Drug Info [525817]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Complement and coagulation cascades
Inflammatory mediator regulation of TRP channels
Regulation of actin cytoskeleton
Pathways in cancer
NetPath Pathway Leptin Signaling Pathway
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
G alpha (i) signalling events
WikiPathways Complement and Coagulation Cascades
ACE Inhibitor Pathway
Regulation of Actin Cytoskeleton
GPCRs, Class A Rhodopsin-like
Vitamin D Receptor Pathway
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 523181ClinicalTrials.gov (NCT01207973) Safety, Tolerability, Pharmacokinetics and -Dynamics of Multiple Rising Oral Doses of BI 113823 in Patients Patients With Osteoarthritis of the Knee. U.S. National Institutes of Health.
Ref 523403ClinicalTrials.gov (NCT01319487) Safety and Efficacy Study of Topical Administration of FOV2304 (High Dose or Low Dose) for the Treatment of Center-involving Clinically Significant Macular Edema Associated With Diabetic Retinopathy. U.S. National Institutes of Health.
Ref 541730(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: 662).
Ref 547525Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017078)
Ref 525817J Med Chem. 2000 Jun 15;43(12):2382-6.Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists.
Ref 527294Bioorg Med Chem Lett. 2004 Dec 20;14(24):6045-8.Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.
Ref 531635Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
Ref 532906The bradykinin B1 receptor antagonist BI113823 reverses inflammatory hyperalgesia by desensitization of peripheral and spinal neurons. Eur J Pain. 2015 Jan;19(1):132-42.
Ref 535320Evidence for the participation of kinins in Freund's adjuvant-induced inflammatory and nociceptive responses in kinin B1 and B2 receptor knockout mice. Neuropharmacology. 2001 Dec;41(8):1006-12.
Ref 541709(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: 659).
Ref 544033The kinin B1 receptor antagonist SSR240612 reverses tactile and cold allodynia in an experimental rat model of insulin resistance. Br J Pharmacol. 2007 September; 152(2): 280-287.
Ref 551643The role of kinin receptors in cancer and therapeutic opportunities. Cancer Letters Volume 345, Issue 1, 1 April 2014, Pages 27-38.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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