New concepts in drug discovery: collateral efficacy and permissive antagonism.
about
Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000Translocation of arrestin induced by human A(3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathwaysWhat systems can and can't doEvolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligandNew Frontier in Glycoprotein Hormones and Their Receptors Structure-FunctionTargeting G protein coupled receptor-related pathways as emerging molecular therapiesPositive allosteric modulators of metabotropic glutamate 2 receptors in schizophrenia treatmentDREADDs: novel tools for drug discovery and developmentProtein C anticoagulant and cytoprotective pathwaysGaddum Memorial Lecture 2014: receptors as an evolving concept: from switches to biased microprocessorsNovel Allosteric Modulators of G Protein-coupled ReceptorsCharacterization of an mGluR2/3 negative allosteric modulator in rodent models of depressionA linear framework for time-scale separation in nonlinear biochemical systemsAntibodies raised against different extracellular loops of the melanocortin-3 receptor affect energy balance and autonomic function in rats{Beta}-blocker drugs mediate calcium signaling in native central nervous system neurons by {beta}-arrestin-biased agonismLabel-free integrative pharmacology on-target of opioid ligands at the opioid receptor familyAllosteric modulation of metabotropic glutamate receptors.Both ligand- and cell-specific parameters control ligand agonism in a kinetic model of g protein-coupled receptor signaling.Duplexed label-free G protein--coupled receptor assays for high-throughput screening.Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7An innovative method to classify SERMs based on the dynamics of estrogen receptor transcriptional activity in living animals.Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery.Quantitative phosphoproteomics dissection of seven-transmembrane receptor signaling using full and biased agonists.The hinge region of human thyroid-stimulating hormone (TSH) receptor operates as a tunable switch between hormone binding and receptor activation.Functional selectivity in adrenergic and angiotensin signaling systems.Development of allosteric modulators of GPCRs for treatment of CNS disordersLabel-Free Receptor Assays.Allosteric modulation of protease-activated receptor signaling.Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor.Orthosteric binding of ρ-Da1a, a natural peptide of snake venom interacting selectively with the α1A-adrenoceptorG protein-coupled receptors--recent advancesAllosteric regulation of pathologic angiogenesis: potential application for angiogenesis-related blindness.S-nitrosylation-regulated GPCR signaling.Probing the binding site of the A1 adenosine receptor reengineered for orthogonal recognition by tailored nucleosides.Functional selectivity at the μ-opioid receptor: implications for understanding opioid analgesia and tolerance.The therapeutic potential of orphan GPCRs, GPR35 and GPR55.Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptorAllosteric interactions between δ and κ opioid receptors in peripheral sensory neuronsA negative allosteric modulator demonstrates biased antagonism of the follicle stimulating hormone receptor.The atypical antipsychotics clozapine and olanzapine promote down-regulation and display functional selectivity at human 5-HT7 receptors.
P2860
Q21262008-74919CD9-462F-4D0A-B2D1-269E9A4EAD08Q24646643-F5F1D997-5DA9-4D2F-B965-66DADE214AD1Q24654880-846C9254-C6FE-4A2C-A4E2-6749C7FDB795Q24676976-84D4554F-3BEA-412F-9ED7-6116F48B07BFQ26779481-1C3CF13E-22A5-45EA-AA7A-72DA60DF16FAQ26829964-D2C7CB01-50FC-44C2-90D2-FC56919AB35DQ26852047-0661105A-49F1-42C8-B036-29C4B75D1425Q26995396-69212E02-21B8-49B3-8DD8-1D30531F80A4Q26999113-9936778C-7672-4C5E-AE8B-10C7CD473DB1Q27005640-7FEAE828-6186-4A5C-9D59-351E0591A370Q28081112-0509DB80-F072-4F03-A600-9E7837C5E9FEQ28253233-0CE3798D-E126-467F-94B3-5BF0F86D6C65Q28483677-17436889-CC00-4B0B-91AE-65BCD9749511Q28565823-EC594F5C-0E23-41D9-82E9-C5AEAAAA4FA5Q28582523-E4B91D66-12CA-4832-AFD6-2D4B346DC4DFQ28709650-D8B7A33E-2085-4A1D-B824-AF84F668B62FQ30448534-92AA777F-17FD-4E3F-A602-58574F289612Q33269156-5E96765F-324B-4D86-A478-B4A846C24733Q33386660-BDE6D556-4FE3-452C-96D9-5F536E7B6E36Q33520184-0258E17B-0C78-4C55-954F-8A40C1E592BCQ33780223-4E34304C-2EC0-465B-92D4-7412169885F8Q33890786-685C282D-6C40-4657-BDF5-A33B208FCC7BQ34122067-B35C64BB-B12B-47BC-ABFD-73808DCC5620Q34336103-A484C8DC-C327-4707-80FF-C624DC759AE4Q34359586-9693E34B-A26B-411A-8ABE-C1026631C0E7Q34373958-C10164A1-E0B1-47D6-B4C5-7873A710ECF7Q34473007-87E580C0-56C8-4023-8B0B-15A5CBDF7FE2Q34543233-49D7B1FB-CD38-42CC-B2E1-08B040507063Q34672123-F3A1A0FA-6B25-4A90-AAED-8405A607F283Q34918713-3D7B8713-B676-440D-8680-229DF7BF53DDQ35065927-F78DE600-7712-4303-B9B4-9BC32C170A1FQ35084192-4B7243BF-B35E-4BA4-9E42-9F823B738C09Q35091511-3014C9FD-29B2-4112-9381-F981431460D3Q35119322-CA249BFF-2F7D-4B0B-A628-C8BCD05A4FE1Q35264421-8E90CAF3-11A0-4872-8586-351C71DED31BQ35425244-B4C3856E-5016-417A-BE49-2D242CF9BC5EQ35574655-9B5F8ED4-3DBB-45F9-B29F-C7B1274B16E7Q35688476-8BC720F3-C1EC-4A0D-8197-110D83C0F9ADQ35817527-F19A2F9D-42C7-4EBB-A28A-BD2BB8682DE3Q35911754-7CCA8D1C-46AB-43BC-A450-1B34075B7866
P2860
New concepts in drug discovery: collateral efficacy and permissive antagonism.
description
2005 nî lūn-bûn
@nan
2005年の論文
@ja
2005年学术文章
@wuu
2005年学术文章
@zh-cn
2005年学术文章
@zh-hans
2005年学术文章
@zh-my
2005年学术文章
@zh-sg
2005年學術文章
@yue
2005年學術文章
@zh
2005年學術文章
@zh-hant
name
New concepts in drug discovery: collateral efficacy and permissive antagonism.
@ast
New concepts in drug discovery: collateral efficacy and permissive antagonism.
@en
type
label
New concepts in drug discovery: collateral efficacy and permissive antagonism.
@ast
New concepts in drug discovery: collateral efficacy and permissive antagonism.
@en
prefLabel
New concepts in drug discovery: collateral efficacy and permissive antagonism.
@ast
New concepts in drug discovery: collateral efficacy and permissive antagonism.
@en
P2860
P356
P1476
New concepts in drug discovery: collateral efficacy and permissive antagonism.
@en
P2093
Terry Kenakin
P2860
P2888
P304
P356
10.1038/NRD1875
P577
2005-11-01T00:00:00Z