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首页> 外文期刊>Drug discovery today >Progress in corticotropin-releasing factor-1 antagonist development.
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Progress in corticotropin-releasing factor-1 antagonist development.

机译：促肾上腺皮质激素释放因子1拮抗剂的开发进展。

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Corticotropin releasing factor (CRF) receptor antagonists have been sought since the stress-secreted peptide was isolated in 1981. Although evidence is mixed concerning the efficacy of CRF(1) antagonists as antidepressants, CRF(1) antagonists might be novel pharmacotherapies for anxiety and addiction. Progress in understanding the two-domain model of ligand-receptor interactions for CRF family receptors might yield chemically novel CRF(1) receptor antagonists, including peptide CRF(1) antagonists, antagonists with signal transduction selectivity and nonpeptide CRF(1) antagonists that act via the extracellular (rather than transmembrane) domains. Novel ligands that conform to the prevalent pharmacophore and exhibit drug-like pharmacokinetic properties have been identified. The therapeutic utility of CRF(1) antagonists should soon be clearer: several small molecules are currently in Phase II/III clinical trials for depression, anxiety and irritable bowel syndrome.
机译：自从1981年分离出应力分泌肽以来，就一直在寻找促肾上腺皮质激素释放因子（CRF）受体拮抗剂。尽管关于CRF（1）拮抗剂作为抗抑郁药的功效的证据不一，但CRF（1）拮抗剂可能是治疗焦虑症和抑郁症的新药。瘾。了解CRF家族受体的配体-受体相互作用的两域模型的进展可能会产生化学上新颖的CRF（1）受体拮抗剂，包括肽CRF（1）拮抗剂，具有信号传导选择性的拮抗剂和起作用的非肽CRF（1）拮抗剂通过细胞外（而非跨膜）结构域。已经鉴定出符合流行药效基团并表现出药物样药代动力学性质的新型配体。 CRF（1）拮抗剂的治疗作用应该很快变得更加清晰：目前一些处于抑郁，焦虑和肠易激综合症的II / III期临床试验的小分子。

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