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TitleProspect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine.
Journal, issue, pagesNat Commun, Vol. 14, Issue 1, Page 962, Year 2023
Publish dateFeb 21, 2023
AuthorsJie Zhao / Hong Fu / Jingjing Yu / Weiqi Hong / Xiaowen Tian / Jieyu Qi / Suyue Sun / Chang Zhao / Chao Wu / Zheng Xu / Lin Cheng / Renjie Chai / Wei Yan / Xiawei Wei / Zhenhua Shao /
PubMed AbstractSomatostatin receptor 2 (SSTR2) is highly expressed in neuroendocrine tumors and represents as a therapeutic target. Several peptide analogs mimicking the endogenous ligand somatostatin are available ...Somatostatin receptor 2 (SSTR2) is highly expressed in neuroendocrine tumors and represents as a therapeutic target. Several peptide analogs mimicking the endogenous ligand somatostatin are available for clinical use, but poor therapeutic effects occur in a subset of patients, which may be correlated with subtype selectivity or cell surface expression. Here, we clarify the signal bias profiles of the first-generation peptide drug octreotide and a new-generation small molecule paltusotine by evaluating their pharmacological characteristics. We then perform cryo-electron microscopy analysis of SSTR2-Gi complexes to determine how the drugs activate SSTR2 in a selective manner. In this work, we decipher the mechanism of ligand recognition, subtype selectivity and signal bias property of SSTR2 sensing octreotide and paltusotine, which may aid in designing therapeutic drugs with specific pharmacological profiles against neuroendocrine tumors.
External linksNat Commun / PubMed:36810324 / PubMed Central
MethodsEM (single particle)
Resolution3.24 - 3.37 Å
Structure data

33708

7yac

EMDB-33708, PDB-7yac:
Paltusotine-bound SSTR2-Gi complex
Method: EM (single particle) / Resolution: 3.24 Å

33710

7yae

EMDB-33710, PDB-7yae:
Octreotide-bound SSTR2-Gi complex
Method: EM (single particle) / Resolution: 3.37 Å

Chemicals

ChemComp-IUD:
Paltusotine

ChemComp-CLR:
CHOLESTEROL

Source
  • homo sapiens (human)
  • mus musculus (house mouse)
  • synthetic construct (others)
KeywordsSIGNALING PROTEIN / agonist / membrane protein / Complex

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