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Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers

Pituitary, 2022-04, Vol.25 (2), p.328-339

2022

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Discovery of nonpeptide 3,4-dihydroquinazoline-4-carboxamides as potent and selective sst2 agonists

Bioorganic & medicinal chemistry letters, 2020-09, Vol.30 (17), p.127391-127391, Article 127391

2020

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Discovery of 4-(3-aminopyrrolidinyl)-3-aryl-5-(benzimidazol-2-yl)-pyridines as potent and selective SST5 agonists for the treatment of congenital hyperinsulinism

Bioorganic & medicinal chemistry letters, 2022-09, Vol.71, p.128807-128807, Article 128807

2022

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Reproductive physiology of a humanized GnRH receptor mouse model: application in evaluation of human-specific analogs

American journal of physiology: endocrinology and metabolism, 2013-07, Vol.305 (1), p.E67-E77

2013

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ACROBAT Edge: Safety and Efficacy of Switching Injected SRLs to Oral Paltusotine in Patients With Acromegaly

The journal of clinical endocrinology and metabolism, 2023-05, Vol.108 (5), p.e148-e159

2023

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Acromegaly Disease Control Maintained After Switching From Injected Somatostatin Receptor Ligands to Oral Paltusotine

The journal of clinical endocrinology and metabolism, 2024-06

2024

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Discovery of substituted 3H-pyrido[2,3-d]pyrimidin-4-ones as potent, biased, and orally bioavailable sst2 agonist

Bioorganic & medicinal chemistry letters, 2020-11, Vol.30 (21), p.127496-127496, Article 127496

2020

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Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist

ACS medicinal chemistry letters, 2023-01, Vol.14 (1), p.66-74

2023

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Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist

ACS medicinal chemistry letters, 2024-04, Vol.15 (4), p.478-485

2024

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Distinct Conformations of the Corticotropin Releasing Factor Type 1 Receptor Adopted following Agonist and Antagonist Binding Are Differentially Regulated

The Journal of biological chemistry, 2005-03, Vol.280 (12), p.11560-11568

2005

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Differential Desensitization, Receptor Phosphorylation, β-Arrestin Recruitment, and ERK1/2 Activation by the Two Endogenous Ligands for the CC Chemokine Receptor 7

The Journal of biological chemistry, 2004-05, Vol.279 (22), p.23214-23222

2004

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Synthesis of aryl-1,2,4-triazine-3,5-diones as antagonists of the gonadotropin-releasing hormone receptor

Bioorganic & medicinal chemistry letters, 2005-10, Vol.15 (19), p.4363-4366

2005

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Identification of CC Chemokine Receptor 7 Residues Important for Receptor Activation

The Journal of biological chemistry, 2004-10, Vol.279 (41), p.42383-42392

2004

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Trapping of a Nonpeptide Ligand by the Extracellular Domains of the Gonadotropin-Releasing Hormone Receptor Results in Insurmountable Antagonism

Molecular pharmacology, 2007-08, Vol.72 (2), p.238-247

2007

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Discovery of Sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor

Journal of medicinal chemistry, 2008-12, Vol.51 (23), p.7478-7485

2008

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Non-Peptide Gonadotropin-Releasing Hormone Receptor Antagonists

Journal of medicinal chemistry, 2008-06, Vol.51 (12), p.3331-3348

2008

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Somatotroph hypoplasia and dwarfism in transgenic mice expressing a non-phosphorylatable CREB mutant

Nature (London), 1991-04, Vol.350 (6319), p.622-624

1991

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A Novel Synthesis of 2-Arylpyrrolo[1,2- a]pyrimid-7-ones and Their Structure–Activity Relationships as Potent GnRH Receptor Antagonists

Bioorganic & medicinal chemistry letters, 2002-02, Vol.12 (3), p.403-406

2002

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Suppression of Serum Luteinizing Hormone in Postmenopausal Women by an Orally Administered Nonpeptide Antagonist of the Gonadotropin-Releasing Hormone Receptor (NBI-42902)

The journal of clinical endocrinology and metabolism, 2006-10, Vol.91 (10), p.3903-3907

2006

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Overlapping, Nonidentical Binding Sites of Different Classes of Nonpeptide Antagonists for the Human Gonadotropin-Releasing Hormone Receptor

Journal of medicinal chemistry, 2006-01, Vol.49 (2), p.637-647

2006

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Pharmacological Characterization of a Novel Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor, NBI-42902

Endocrinology (Philadelphia), 2007-02, Vol.148 (2), p.857-867

2007

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Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties

Bioorganic & medicinal chemistry, 2008-08, Vol.18 (16), p.4503-4507

2008

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3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a Potent and Orally Active Antagonist of the Human Gonadotropin-Releasing Hormone Receptor. Design, Synthesis, and in Vitro and in Vivo Characterization

Journal of medicinal chemistry, 2005-02, Vol.48 (4), p.1169-1178

2005

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Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure–activity relationships and insurmountable antagonism

Biochemical pharmacology, 2006-09, Vol.72 (7), p.838-849

2006

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The N-terminal domain of CCL21 reconstitutes high affinity binding, G protein activation, and chemotactic activity, to the C-terminal domain of CCL19

Biochemical and biophysical research communications, 2006-09, Vol.348 (3), p.1089-1093

2006

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Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers

Discovery of nonpeptide 3,4-dihydroquinazoline-4-carboxamides as potent and selective sst2 agonists

Discovery of 4-(3-aminopyrrolidinyl)-3-aryl-5-(benzimidazol-2-yl)-pyridines as potent and selective SST5 agonists for the treatment of congenital hyperinsulinism

Reproductive physiology of a humanized GnRH receptor mouse model: application in evaluation of human-specific analogs

ACROBAT Edge: Safety and Efficacy of Switching Injected SRLs to Oral Paltusotine in Patients With Acromegaly

Acromegaly Disease Control Maintained After Switching From Injected Somatostatin Receptor Ligands to Oral Paltusotine

Discovery of substituted 3H-pyrido[2,3-d]pyrimidin-4-ones as potent, biased, and orally bioavailable sst2 agonist

Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist

Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist

Distinct Conformations of the Corticotropin Releasing Factor Type 1 Receptor Adopted following Agonist and Antagonist Binding Are Differentially Regulated

Differential Desensitization, Receptor Phosphorylation, β-Arrestin Recruitment, and ERK1/2 Activation by the Two Endogenous Ligands for the CC Chemokine Receptor 7

Synthesis of aryl-1,2,4-triazine-3,5-diones as antagonists of the gonadotropin-releasing hormone receptor

Identification of CC Chemokine Receptor 7 Residues Important for Receptor Activation

Trapping of a Nonpeptide Ligand by the Extracellular Domains of the Gonadotropin-Releasing Hormone Receptor Results in Insurmountable Antagonism

Discovery of Sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor

Non-Peptide Gonadotropin-Releasing Hormone Receptor Antagonists

Somatotroph hypoplasia and dwarfism in transgenic mice expressing a non-phosphorylatable CREB mutant

A Novel Synthesis of 2-Arylpyrrolo[1,2- a]pyrimid-7-ones and Their Structure–Activity Relationships as Potent GnRH Receptor Antagonists

Suppression of Serum Luteinizing Hormone in Postmenopausal Women by an Orally Administered Nonpeptide Antagonist of the Gonadotropin-Releasing Hormone Receptor (NBI-42902)

Overlapping, Nonidentical Binding Sites of Different Classes of Nonpeptide Antagonists for the Human Gonadotropin-Releasing Hormone Receptor

Pharmacological Characterization of a Novel Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor, NBI-42902

Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties

3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a Potent and Orally Active Antagonist of the Human Gonadotropin-Releasing Hormone Receptor. Design, Synthesis, and in Vitro and in Vivo Characterization

Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure–activity relationships and insurmountable antagonism

The N-terminal domain of CCL21 reconstitutes high affinity binding, G protein activation, and chemotactic activity, to the C-terminal domain of CCL19

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