Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTOISYB)

DTT Name Proto-oncogene Mas (MAS)
Synonyms MGRA; MAS1 proto-oncogene, G protein-coupled receptor
Gene Name MAS1
DTT Type
Clinical trial target
 [1]
BioChemical Class
GPCR rhodopsin
UniProt ID
MAS_HUMAN
TTD ID
T91894
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDGSNVTSFVVEEPTNISTGRNASVGNAHRQIPIVHWVIMSISPVGFVENGILLWFLCFR
MRRNPFTVYITHLSIADISLLFCIFILSIDYALDYELSSGHYYTIVTLSVTFLFGYNTGL
YLLTAISVERCLSVLYPIWYRCHRPKYQSALVCALLWALSCLVTTMEYVMCIDREEESHS
RNDCRAVIIFIAILSFLVFTPLMLVSSTILVVKIRKNTWASHSSKLYIVIMVTIIIFLIF
AMPMRLLYLLYYEYWSTFGNLHHISLLFSTINSSANPFIYFFVGSSKKKRFKESLKVVLT
RAFKDEMQPRRQKDNCNTVTVETVV
Function
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 activation of 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. Receptor for angiotensin 1-7.
KEGG Pathway
Neuroactive ligand-receptor interaction (hsa04080 )
Renin-angiotensin system (hsa04614 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
2 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Angiotensin-(1-7) DM76GZ0 Sarcoma 2A60-2C35 Phase 3 [1]
DSC-127 DMM0HAE Diabetic foot ulcer BD54 Phase 3 [1]
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3 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
AR234960 DMTN10D Discovery agent N.A. Investigative [2]
AR244555 DM68QY0 Discovery agent N.A. Investigative [2]
AVE 0991 DM9R3WT Discovery agent N.A. Investigative [3]
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Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Sarcoma 2C82 Muscle tissue 2.91E-75 -0.43 -1.38
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References

1 New therapeutic pathways in the RAS. J Renin Angiotensin Aldosterone Syst. 2012 Dec;13(4):505-8.
2 Inhibition 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.
3 Nonpeptide AVE 0991 is an angiotensin-(1-7) receptor Mas agonist in the mouse kidney. Hypertension. 2004 Oct;44(4):490-6.