Discovery and SAR Studies of Orally Active Somatostatin Receptor Subtype-2 (SSTR2) Agonists for the Treatment of Acromegaly.

Acromegaly / drug therapy Animals Growth Hormone Rats Receptors, Somatostatin / agonists Somatostatin Structure-Activity Relationship
GPCR SSTR2 Somatostatin acromegaly nonpeptidic orally active

Journal

ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337

Informations de publication

Date de publication:
20 05 2020
Historique:
pubmed: 22 4 2020
medline: 22 6 2021
entrez: 22 4 2020
Statut: ppublish

Résumé

Acromegaly is a disease caused by the oversecretion of growth hormone. It is currently treated by intravenous injection with cyclic peptide drugs that activate somatostatin receptor subtype 2 (SSTR2). Here, novel nonpeptidic, small-molecule, and orally active SSTR2 agonists were identified from a hit compound (

Identifiants

DOI: 10.1021/acschemneuro.0c00124 PMID: 32315148
pubmed: 32315148
doi: 10.1021/acschemneuro.0c00124
doi:

Substances chimiques

Receptors, Somatostatin 0
Sstr2 protein, rat 0
Somatostatin 51110-01-1
Growth Hormone 9002-72-6

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

1482-1494

Auteurs

Akiharu Ishida (A)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.
ORCID: 0000-0001-5096-1377

Yohei Tajima (Y)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Yasuyuki Okabe (Y)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Takeshi Matsushita (T)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Tetsuya Sekiguchi (T)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Satomi Imaide (S)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Yoshinori Nomura (Y)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Motoyuki Tanaka (M)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Shoji Nojima (S)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Atsushi Yoshida (A)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Yoko Iyoda (Y)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Shohei Aoki (S)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Takuya Nishio (T)

Department of Biology & Pharmacology, Ono Pharmaceutical Co., Ltd., 3-1-1 Sakurai, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.

Tatsuya Komagata (T)

Department of Biology & Pharmacology, Ono Pharmaceutical Co., Ltd., 3-1-1 Sakurai, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.

Masanori Iwaki (M)

Department of Biology & Pharmacology, Ono Pharmaceutical Co., Ltd., 3-1-1 Sakurai, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.

Tomoyuki Shono (T)

Pharmacokinetic Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.

Atsushi Naganawa (A)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

Akira Imagawa (A)

Medicinal Chemistry Research Laboratories, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima-gun, Osaka 618-8585, Japan.

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Classifications MeSH

Recherchemedicale.com › Maladies endocriniennes › Maladies de l'hypophyse › Hyperpituitarisme › Acromégalie › Discovery and SAR Studies of Orally Active...
Recherchemedicale.com › Eucaryotes › Animaux › Discovery and SAR Studies of Orally Active...
Recherchemedicale.com › Acides aminés, peptides et protéines › Peptides › Hormones peptidiques › Hormones hypophysaires › Hormones antéhypophysaires › Hormone de croissance › Discovery and SAR Studies of Orally Active...
Recherchemedicale.com › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Discovery and SAR Studies of Orally Active...
Recherchemedicale.com › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs peptidiques › Récepteur hormones hypothalamiques hypophysotropes régulatrices › Récepteur somatostatine › Discovery and SAR Studies of Orally Active...
Recherchemedicale.com › Acides aminés, peptides et protéines › Protéines › Protéines de tissu nerveux › Neuropeptides › Hormones hypothalamiques › Hormones hypothalamiques hypophysotropes inhibitrices › Somatostatine › Discovery and SAR Studies of Orally Active...
Recherchemedicale.com › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Discovery and SAR Studies of Orally Active...