GPCRs Revisited: New Insights Lead to Novel Drugs
GPCRs play a critical role in human physiology and are a prime target for drug discovery globally. Novel insights into the functions of GPCRs are providing unique approaches to modulate these proteins to generate unique drug candidates. Next generation ligands include those with novel pharmacologies...
| Main Authors: | , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2011-01-01
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| Series: | Pharmaceuticals |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1424-8247/4/2/244/ |
| _version_ | 1811265776530751488 |
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| author | Terry Reisine Richard M. Eglen |
| author_facet | Terry Reisine Richard M. Eglen |
| author_sort | Terry Reisine |
| collection | DOAJ |
| description | GPCRs play a critical role in human physiology and are a prime target for drug discovery globally. Novel insights into the functions of GPCRs are providing unique approaches to modulate these proteins to generate unique drug candidates. Next generation ligands include those with novel pharmacologies such as allosteric regulators as well pepducins, that affect the interaction of GPCRs with G proteins, to either block selective receptor signaling pathways or mimic the actions of intracellular domains of receptors, thereby activating GPCRs to signal selectively to intracellular pathways. We will review these new concepts and then discuss how they may be exploited using modern discovery technologies to provide novel drug candidates for the future. |
| first_indexed | 2024-04-12T20:30:01Z |
| format | Article |
| id | doaj.art-fd35d00774344c989d8a6cc84bb349e8 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-04-12T20:30:01Z |
| publishDate | 2011-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-fd35d00774344c989d8a6cc84bb349e82022-12-22T03:17:46ZengMDPI AGPharmaceuticals1424-82472011-01-014224427210.3390/ph4020244GPCRs Revisited: New Insights Lead to Novel DrugsTerry ReisineRichard M. EglenGPCRs play a critical role in human physiology and are a prime target for drug discovery globally. Novel insights into the functions of GPCRs are providing unique approaches to modulate these proteins to generate unique drug candidates. Next generation ligands include those with novel pharmacologies such as allosteric regulators as well pepducins, that affect the interaction of GPCRs with G proteins, to either block selective receptor signaling pathways or mimic the actions of intracellular domains of receptors, thereby activating GPCRs to signal selectively to intracellular pathways. We will review these new concepts and then discuss how they may be exploited using modern discovery technologies to provide novel drug candidates for the future.http://www.mdpi.com/1424-8247/4/2/244/GPCRG proteinallosterismdualstericoligomerizationpharmacophorecrystal structureNMRDMRpepducin |
| spellingShingle | Terry Reisine Richard M. Eglen GPCRs Revisited: New Insights Lead to Novel Drugs Pharmaceuticals GPCR G protein allosterism dualsteric oligomerization pharmacophore crystal structure NMR DMR pepducin |
| title | GPCRs Revisited: New Insights Lead to Novel Drugs |
| title_full | GPCRs Revisited: New Insights Lead to Novel Drugs |
| title_fullStr | GPCRs Revisited: New Insights Lead to Novel Drugs |
| title_full_unstemmed | GPCRs Revisited: New Insights Lead to Novel Drugs |
| title_short | GPCRs Revisited: New Insights Lead to Novel Drugs |
| title_sort | gpcrs revisited new insights lead to novel drugs |
| topic | GPCR G protein allosterism dualsteric oligomerization pharmacophore crystal structure NMR DMR pepducin |
| url | http://www.mdpi.com/1424-8247/4/2/244/ |
| work_keys_str_mv | AT terryreisine gpcrsrevisitednewinsightsleadtonoveldrugs AT richardmeglen gpcrsrevisitednewinsightsleadtonoveldrugs |