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Synonyms: AT-001 | B13/17K H2 relaxin
Compound class: Peptide or derivative
Comment: An analogue of H2 relaxin, B-R13/17K H2 relaxin is a dimer of A and B chains. The arginine residues of the B chain of H2 relaxin (amino acids 13 and 17) are substituted for lysine residues, to form the analogue, whereas the A chain has the amino acid sequence of the natural subunit. The amino acid sequence of this synthetic B chain is shown on the 'structure' tab. For the structure of the A chain, see the ligand page for human relaxin (A chain).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Hossain MA, Samuel CS, Binder C, Hewitson TD, Tregear GW, Wade JD, Bathgate RA. (2010)
The chemically synthesized human relaxin-2 analog, B-R13/17K H2, is an RXFP1 antagonist.
Amino Acids, 39 (2): 409-16. [PMID:20043231]
2. Neschadim A, Pritzker LB, Pritzker KP, Branch DR, Summerlee AJ, Trachtenberg J, Silvertown JD. (2014)
Relaxin receptor antagonist AT-001 synergizes with docetaxel in androgen-independent prostate xenografts.
Endocr Relat Cancer, 21 (3): 459-71. [PMID:24812057]