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Literature DB >> 25754495

The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.

Yingzhi Bi¹, Carolyn D Dzierba², Cynthia Fink¹, Yudith Garcia¹, Michael Green¹, Jianxin Han¹, Soojin Kwon¹, Godwin Kumi¹, Zhi Liang¹, Ying Liu¹, Ying Qiao¹, Yulian Zhang¹, Greg Zipp¹, Neil Burford², Meredith Ferrante², Robert Bertekap², Martin Lewis², Angela Cacace², Ryan S Westphal², David Kimball¹, Joanne J Bronson², John E Macor².

Abstract

Modulating GPR88 activity is suggested to have therapeutic utility in the treatment of CNS disorders, such as schizophrenia. This Letter will describe the discovery and SAR development of a class of potent GPR88 agonists.

Entities: Disease Gene

Keywords: Agonists; CNS; GPC; GPR88; Schizophrenia

Mesh：

Substances：

Year: 2015 PMID： 25754495 DOI： 10.1016/j.bmcl.2015.02.038

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

11 in total

Review 1. Ins and outs of GPCR signaling in primary cilia.

Authors: Kenneth Bødtker Schou; Lotte Bang Pedersen; Søren Tvorup Christensen
Journal: EMBO Rep Date: 2015-08-21 Impact factor: 8.807

2. Effect of Substitution on the Aniline Moiety of the GPR88 Agonist 2-PCCA: Synthesis, Structure-Activity Relationships, and Molecular Modeling Studies.

Authors: Chunyang Jin; Ann M Decker; Danni L Harris; Bruce E Blough
Journal: ACS Chem Neurosci Date: 2016-08-16 Impact factor: 4.418

Review 3. Orphan Receptor GPR88 as an Emerging Neurotherapeutic Target.

Authors: Na Ye; Bang Li; Qi Mao; Eric A Wold; Sheng Tian; John A Allen; Jia Zhou
Journal: ACS Chem Neurosci Date: 2018-12-20 Impact factor: 4.418

4. Design, Synthesis, and Structure-Activity Relationship Studies of (4-Alkoxyphenyl)glycinamides and Bioisosteric 1,3,4-Oxadiazoles as GPR88 Agonists.

Authors: Md Toufiqur Rahman; Ann M Decker; Tiffany L Langston; Kelly M Mathews; Lucas Laudermilk; Rangan Maitra; Weiya Ma; Emmanuel Darcq; Brigitte L Kieffer; Chunyang Jin
Journal: J Med Chem Date: 2020-11-18 Impact factor: 7.446

5. Discovery of a Potent, Selective, and Brain-Penetrant Small Molecule that Activates the Orphan Receptor GPR88 and Reduces Alcohol Intake.

Authors: Chunyang Jin; Ann M Decker; Viren H Makhijani; Joyce Besheer; Emmanuel Darcq; Brigitte L Kieffer; Rangan Maitra
Journal: J Med Chem Date: 2018-07-30 Impact factor: 7.446

6. Design, synthesis and pharmacological evaluation of 4-hydroxyphenylglycine and 4-hydroxyphenylglycinol derivatives as GPR88 agonists.

Authors: Chunyang Jin; Ann M Decker; Tiffany L Langston
Journal: Bioorg Med Chem Date: 2016-12-01 Impact factor: 3.641

The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.

Review 1. Ins and outs of GPCR signaling in primary cilia.

2. Effect of Substitution on the Aniline Moiety of the GPR88 Agonist 2-PCCA: Synthesis, Structure-Activity Relationships, and Molecular Modeling Studies.

Review 3. Orphan Receptor GPR88 as an Emerging Neurotherapeutic Target.

4. Design, Synthesis, and Structure-Activity Relationship Studies of (4-Alkoxyphenyl)glycinamides and Bioisosteric 1,3,4-Oxadiazoles as GPR88 Agonists.

5. Discovery of a Potent, Selective, and Brain-Penetrant Small Molecule that Activates the Orphan Receptor GPR88 and Reduces Alcohol Intake.

6. Design, synthesis and pharmacological evaluation of 4-hydroxyphenylglycine and 4-hydroxyphenylglycinol derivatives as GPR88 agonists.

7. Activation and allosteric regulation of the orphan GPR88-Gi1 signaling complex.

8. Development and validation of a high-throughput calcium mobilization assay for the orphan receptor GPR88.

Review 9. Orphan G Protein Coupled Receptors in Affective Disorders.

10. Neuron-specific cilia loss differentially alters locomotor responses to amphetamine in mice.