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用于鉴定子宫收缩新调节因子的药物发现策略。

Drug discovery strategies for the identification of novel regulators of uterine contractility.

作者信息

Siricilla Shajila, Iwueke Chisom C, Herington Jennifer L

机构信息

Division of Neonatology, Department of Pediatrics, Vanderbilt University Medical Center, Nashville, TN, USA.

Division of Maternal-Fetal Medicine, Department of Obstetrics and Gynecology, Vanderbilt University Medical Center, Nashville, TN, USA.

出版信息

Curr Opin Physiol. 2020 Feb;13:71-86. doi: 10.1016/j.cophys.2019.10.012. Epub 2019 Oct 23.

DOI:10.1016/j.cophys.2019.10.012
PMID:32864532
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7451233/
Abstract

Preterm birth and postpartum hemorrhage are the leading causes of neonatal and maternal morbidities worldwide, respectively. Current clinically utilized tocolytics and uterotonics to manage these obstetric conditions are limited due to their off-target effects and/or lack of efficacy. Thus, an ideal tocolytic or uterotonic would be uterine-selective with rapid onset and long-duration efficacy. Here, we discuss strategies for the discovery of new therapeutic targets and compounds that regulate uterine contractility with the aforementioned properties.

摘要

早产和产后出血分别是全球新生儿和孕产妇发病的主要原因。目前临床上用于治疗这些产科疾病的宫缩抑制剂和宫缩剂由于其脱靶效应和/或疗效不足而受到限制。因此，理想的宫缩抑制剂或宫缩剂应具有子宫选择性，起效迅速且疗效持久。在此，我们讨论发现具有上述特性的调节子宫收缩力的新治疗靶点和化合物的策略。

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Pharmacol Res. 2019 Aug;146:104268. doi: 10.1016/j.phrs.2019.104268. Epub 2019 May 9.
2
Myometrial Transcriptional Signatures of Human Parturition.人类分娩的子宫肌层转录特征
Front Genet. 2019 Apr 1;10:185. doi: 10.3389/fgene.2019.00185. eCollection 2019.
3
In vitro comparison of liposomal drug delivery systems targeting the oxytocin receptor: a potential novel treatment for obstetric complications.
靶向催产素受体的脂质体药物递送系统的体外比较：一种潜在的产科并发症新疗法。
Int J Nanomedicine. 2019 Mar 27;14:2191-2206. doi: 10.2147/IJN.S198116. eCollection 2019.
4
Paired Utility of Aza-Amino Acyl Proline and Indolizidinone Amino Acid Residues for Peptide Mimicry: Conception of Prostaglandin F2α Receptor Allosteric Modulators That Delay Preterm Birth.氮杂-氨基酸酰脯氨酸和吲哚里西啶酮氨基酸残基对肽模拟物的配对效用：前列腺素 F2α 受体变构调节剂延迟早产的构想。
J Med Chem. 2019 May 9;62(9):4500-4525. doi: 10.1021/acs.jmedchem.9b00056. Epub 2019 Apr 23.
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J Mol Graph Model. 2019 Jun;89:178-191. doi: 10.1016/j.jmgm.2019.03.003. Epub 2019 Mar 16.
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