eneboparatide   Click here for help

GtoPdb Ligand ID: 13815

Synonyms: AZP-3601 | AZP3601 | LA-PTH [2]
Compound class: Peptide
Comment: Eneboparatide (AZP-3601) is a synthetic long-acting PTH receptor 1 agonist [1-2]. It is a fusion of modified PTH(1-14) with amino acid substitutions and PTHrP(15-36). Compared to native human PTH, amino acid substitution in the PTH region of eneboparatide are S3>A, H5>I, L8>M, D10>Q, K11>R, G12>A, S14>W,L18>A, F22>A, H26>K Eneboparatide associates more potently with the R0 conformation of PTH1R (in the presence of 125I-PTH(1-34) and GTPγS to block receptor-G protein-coupling, compared to PTH(1-34) or PTH(1-84) [2]. All three peptides interact with the RG (G protein-coupled) conformation of PTH1R with similar potencies.
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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.

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View interactive charts of activity data across species
References
1. Rejnmark L. (2024)
Treatment of Hypoparathyroidism by Re-Establishing the Effects of Parathyroid Hormone.
Endocrinol Metab (Seoul), 39 (2): 262-266. [PMID:38572533]
2. Shimizu M, Joyashiki E, Noda H, Watanabe T, Okazaki M, Nagayasu M, Adachi K, Tamura T, Potts Jr JT, Gardella TJ et al.. (2016)
Pharmacodynamic Actions of a Long-Acting PTH Analog (LA-PTH) in Thyroparathyroidectomized (TPTX) Rats and Normal Monkeys.
J Bone Miner Res, 31 (7): 1405-12. [PMID:26865415]
3. Takacs I, Mezosi E, Soto A, Kamenický P, Figueres L, Galvez Moreno MA, Lemoine S, Borson-Chazot F, Capel I, Ouldrouis T et al.. (2024)
An Open-label Phase 2 Study of Eneboparatide, a Novel PTH Receptor 1 Agonist, in Hypoparathyroidism.
J Clin Endocrinol Metab, 109 (9): 2199-2209. [PMID:38449442]