Genome-wide pan-GPCR cell libraries accelerate drug discovery
G protein-coupled receptors (GPCRs) are pivotal in mediating diverse physiological and pathological processes, rendering them promising targets for drug discovery. GPCRs account for about 40% of FDA-approved drugs, representing the most successful drug targets. However, only approximately 15% of the...
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| Published in | Acta pharmaceutica Sinica. B Vol. 14; no. 10; pp. 4296 - 4311 |
|---|---|
| Main Authors | , , , , , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
Netherlands
Elsevier B.V
01.10.2024
Elsevier |
| Subjects | |
| Online Access | Get full text |
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| Abstract | G protein-coupled receptors (GPCRs) are pivotal in mediating diverse physiological and pathological processes, rendering them promising targets for drug discovery. GPCRs account for about 40% of FDA-approved drugs, representing the most successful drug targets. However, only approximately 15% of the 800 human GPCRs are targeted by market drugs, leaving numerous opportunities for drug discovery among the remaining receptors. Cell expression systems play crucial roles in the GPCR drug discovery field, including novel target identification, structural and functional characterization, potential ligand screening, signal pathway elucidation, and drug safety evaluation. Here, we discuss the principles, applications, and limitations of widely used cell expression systems in GPCR-targeted drug discovery, GPCR function investigation, signal pathway characterization, and pharmacological property studies. We also propose three strategies for constructing genome-wide pan-GPCR cell libraries, which will provide a powerful platform for GPCR ligand screening, and facilitate the study of GPCR mechanisms and drug safety evaluation, ultimately accelerating the process of GPCR-targeted drug discovery.
The genome-wide pan-GPCR cell line libraries, which utilize overexpression, PRESTO-Tango, and CRISPRa/i technologies, provide a powerful platform for GPCR-targeted drug discovery, which will facilitate the study of GPCR function, drug safety evaluation, and accelerate GPCR drug discovery. [Display omitted] |
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| AbstractList | G protein-coupled receptors (GPCRs) are pivotal in mediating diverse physiological and pathological processes, rendering them promising targets for drug discovery. GPCRs account for about 40% of FDA-approved drugs, representing the most successful drug targets. However, only approximately 15% of the 800 human GPCRs are targeted by market drugs, leaving numerous opportunities for drug discovery among the remaining receptors. Cell expression systems play crucial roles in the GPCR drug discovery field, including novel target identification, structural and functional characterization, potential ligand screening, signal pathway elucidation, and drug safety evaluation. Here, we discuss the principles, applications, and limitations of widely used cell expression systems in GPCR-targeted drug discovery, GPCR function investigation, signal pathway characterization, and pharmacological property studies. We also propose three strategies for constructing genome-wide pan-GPCR cell libraries, which will provide a powerful platform for GPCR ligand screening, and facilitate the study of GPCR mechanisms and drug safety evaluation, ultimately accelerating the process of GPCR-targeted drug discovery.G protein-coupled receptors (GPCRs) are pivotal in mediating diverse physiological and pathological processes, rendering them promising targets for drug discovery. GPCRs account for about 40% of FDA-approved drugs, representing the most successful drug targets. However, only approximately 15% of the 800 human GPCRs are targeted by market drugs, leaving numerous opportunities for drug discovery among the remaining receptors. Cell expression systems play crucial roles in the GPCR drug discovery field, including novel target identification, structural and functional characterization, potential ligand screening, signal pathway elucidation, and drug safety evaluation. Here, we discuss the principles, applications, and limitations of widely used cell expression systems in GPCR-targeted drug discovery, GPCR function investigation, signal pathway characterization, and pharmacological property studies. We also propose three strategies for constructing genome-wide pan-GPCR cell libraries, which will provide a powerful platform for GPCR ligand screening, and facilitate the study of GPCR mechanisms and drug safety evaluation, ultimately accelerating the process of GPCR-targeted drug discovery. G protein-coupled receptors (GPCRs) are pivotal in mediating diverse physiological and pathological processes, rendering them promising targets for drug discovery. GPCRs account for about 40% of FDA-approved drugs, representing the most successful drug targets. However, only approximately 15% of the 800 human GPCRs are targeted by market drugs, leaving numerous opportunities for drug discovery among the remaining receptors. Cell expression systems play crucial roles in the GPCR drug discovery field, including novel target identification, structural and functional characterization, potential ligand screening, signal pathway elucidation, and drug safety evaluation. Here, we discuss the principles, applications, and limitations of widely used cell expression systems in GPCR-targeted drug discovery, GPCR function investigation, signal pathway characterization, and pharmacological property studies. We also propose three strategies for constructing genome-wide pan-GPCR cell libraries, which will provide a powerful platform for GPCR ligand screening, and facilitate the study of GPCR mechanisms and drug safety evaluation, ultimately accelerating the process of GPCR-targeted drug discovery. The genome-wide pan-GPCR cell line libraries, which utilize overexpression, PRESTO-Tango, and CRISPRa/i technologies, provide a powerful platform for GPCR-targeted drug discovery, which will facilitate the study of GPCR function, drug safety evaluation, and accelerate GPCR drug discovery. [Display omitted] G protein-coupled receptors (GPCRs) are pivotal in mediating diverse physiological and pathological processes, rendering them promising targets for drug discovery. GPCRs account for about 40% of FDA-approved drugs, representing the most successful drug targets. However, only approximately 15% of the 800 human GPCRs are targeted by market drugs, leaving numerous opportunities for drug discovery among the remaining receptors. Cell expression systems play crucial roles in the GPCR drug discovery field, including novel target identification, structural and functional characterization, potential ligand screening, signal pathway elucidation, and drug safety evaluation. Here, we discuss the principles, applications, and limitations of widely used cell expression systems in GPCR-targeted drug discovery, GPCR function investigation, signal pathway characterization, and pharmacological property studies. We also propose three strategies for constructing genome-wide pan-GPCR cell libraries, which will provide a powerful platform for GPCR ligand screening, and facilitate the study of GPCR mechanisms and drug safety evaluation, ultimately accelerating the process of GPCR-targeted drug discovery. The genome-wide pan-GPCR cell line libraries, which utilize overexpression, PRESTO-Tango, and CRISPRa/i technologies, provide a powerful platform for GPCR-targeted drug discovery, which will facilitate the study of GPCR function, drug safety evaluation, and accelerate GPCR drug discovery. Image 1 G protein-coupled receptors (GPCRs) are pivotal in mediating diverse physiological and pathological processes, rendering them promising targets for drug discovery. GPCRs account for about 40% of FDA-approved drugs, representing the most successful drug targets. However, only approximately 15% of the 800 human GPCRs are targeted by market drugs, leaving numerous opportunities for drug discovery among the remaining receptors. Cell expression systems play crucial roles in the GPCR drug discovery field, including novel target identification, structural and functional characterization, potential ligand screening, signal pathway elucidation, and drug safety evaluation. Here, we discuss the principles, applications, and limitations of widely used cell expression systems in GPCR-targeted drug discovery, GPCR function investigation, signal pathway characterization, and pharmacological property studies. We also propose three strategies for constructing genome-wide pan-GPCR cell libraries, which will provide a powerful platform for GPCR ligand screening, and facilitate the study of GPCR mechanisms and drug safety evaluation, ultimately accelerating the process of GPCR-targeted drug discovery. |
| Author | Liu, Wei Cong, Zhaotong Wang, Can Zhu, Lingping Yang, Hanting Chen, Shilin Zhao, Jinghao Liao, Jiayu Sun, Dan Liu, Zhixiang Qian, Zhongzhi Wang, Yongfu He, Taiping |
| Author_xml | – sequence: 1 givenname: Hanting orcidid: 0000-0003-0891-8257 surname: Yang fullname: Yang, Hanting organization: School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China – sequence: 2 givenname: Yongfu surname: Wang fullname: Wang, Yongfu organization: School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China – sequence: 3 givenname: Wei surname: Liu fullname: Liu, Wei organization: Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China – sequence: 4 givenname: Taiping orcidid: 0009-0000-7372-9466 surname: He fullname: He, Taiping organization: Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China – sequence: 5 givenname: Jiayu surname: Liao fullname: Liao, Jiayu organization: Department of Bioengineering, University of California, Riverside, CA 92521, USA – sequence: 6 givenname: Zhongzhi surname: Qian fullname: Qian, Zhongzhi organization: Chinese Pharmacopoeia Commission, Beijing 100061, China – sequence: 7 givenname: Jinghao orcidid: 0000-0002-1347-3056 surname: Zhao fullname: Zhao, Jinghao organization: Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China – sequence: 8 givenname: Zhaotong surname: Cong fullname: Cong, Zhaotong organization: Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China – sequence: 9 givenname: Dan orcidid: 0000-0003-1637-6902 surname: Sun fullname: Sun, Dan organization: Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China – sequence: 10 givenname: Zhixiang orcidid: 0000-0003-2586-5273 surname: Liu fullname: Liu, Zhixiang organization: Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China – sequence: 11 givenname: Can surname: Wang fullname: Wang, Can organization: Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China – sequence: 12 givenname: Lingping orcidid: 0000-0001-6959-7755 surname: Zhu fullname: Zhu, Lingping email: zhulingping@cdutcm.edu.cn organization: Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China – sequence: 13 givenname: Shilin surname: Chen fullname: Chen, Shilin email: slchen@cdutcm.edu.cn organization: Institute of Herbgenomics, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/39525595$$D View this record in MEDLINE/PubMed |
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| CitedBy_id | crossref_primary_10_1016_j_xinn_2024_100774 crossref_primary_10_3389_fpls_2024_1433015 crossref_primary_10_3389_fpls_2024_1445365 crossref_primary_10_3390_ijms26072973 crossref_primary_10_1016_j_apsb_2025_03_025 crossref_primary_10_1186_s12864_025_11359_6 |
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| Keywords | High-throughput screening Transgenic cell library Genome-wide pan-GPCR Drug discovery G-protein coupled receptors |
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| SubjectTerms | Drug discovery G-protein coupled receptors Genome-wide pan-GPCR High-throughput screening Review Transgenic cell library |
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| Title | Genome-wide pan-GPCR cell libraries accelerate drug discovery |
| URI | https://dx.doi.org/10.1016/j.apsb.2024.06.023 https://www.ncbi.nlm.nih.gov/pubmed/39525595 https://www.proquest.com/docview/3128751860 https://pubmed.ncbi.nlm.nih.gov/PMC11544303 https://doaj.org/article/e860f0f034d94446ae35e2edb5bdc19c |
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