Target Information

Target General Infomation
Target ID
T91894
Former ID
TTDI02313
Target Name
Proto-oncogene Mas
Gene Name
MAS1
Synonyms
MAS1
Target Type
Clinical Trial
Disease Diabetic foot ulcer [ICD9: 707; ICD10: L88-L89]
Sarcoma [ICD9: 202.8; ICD10: C81-C86]
Function
Receptor for angiotensin 1-7 (By similarity). Acts specifically as a functional antagonist of AGTR1 (angiotensin-2 type 1 receptor), although it up-regulates AGTR1 receptor levels. Positive regulation of AGTR1 levels occurs through activationof the G-proteins GNA11 and GNAQ, and stimulation of the protein kinase C signaling cascade. The antagonist effect on AGTR1 function is probably due to AGTR1 being physically altered by MAS1.
BioChemical Class
GPCR rhodopsin
UniProt ID
P04201
Sequence
MDGSNVTSFVVEEPTNISTGRNASVGNAHRQIPIVHWVIMSISPVGFVENGILLWFLCFR
MRRNPFTVYITHLSIADISLLFCIFILSIDYALDYELSSGHYYTIVTLSVTFLFGYNTGL
YLLTAISVERCLSVLYPIWYRCHRPKYQSALVCALLWALSCLVTTMEYVMCIDREEESHS
RNDCRAVIIFIAILSFLVFTPLMLVSSTILVVKIRKNTWASHSSKLYIVIMVTIIIFLIF
AMPMRLLYLLYYEYWSTFGNLHHISLLFSTINSSANPFIYFFVGSSKKKRFKESLKVVLT
RAFKDEMQPRRQKDNCNTVTVETVV
Drugs and Mode of Action
Drug(s) Angiotensin-(1-7) Drug Info Phase 3 Sarcoma [532124], [541138]
DSC-127 Drug Info Phase 3 Diabetic foot ulcer [532124], [543052]
Agonist Angiotensin-(1-7) Drug Info [532124]
AR234960 Drug Info [531662]
AVE 0991 Drug Info [527181]
DSC-127 Drug Info [532124]
Antagonist AR244555 Drug Info [531662]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Renin-angiotensin system
WikiPathways ACE Inhibitor Pathway
GPCRs, Class A Rhodopsin-like
References
Ref 532124New therapeutic pathways in the RAS. J Renin Angiotensin Aldosterone Syst. 2012 Dec;13(4):505-8.
Ref 541138(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: 582).
Ref 543052(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: 8300).
Ref 527181Nonpeptide AVE 0991 is an angiotensin-(1-7) receptor Mas agonist in the mouse kidney. Hypertension. 2004 Oct;44(4):490-6. Epub 2004 Aug 23.
Ref 531662Inhibition of Mas G-protein signaling improves coronary blood flow, reduces myocardial infarct size, and provides long-term cardioprotection. Am J Physiol Heart Circ Physiol. 2012 Jan 1;302(1):H299-311.
Ref 532124New therapeutic pathways in the RAS. J Renin Angiotensin Aldosterone Syst. 2012 Dec;13(4):505-8.

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