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重组Ig1 Axl受体结构域的分子特征：药物发现筛选中一个引人关注的诱饵

Molecular Characterization of the Recombinant Ig1 Axl Receptor Domain: An Intriguing Bait for Screening in Drug Discovery.

作者信息

Di Stasi Rossella, De Rosa Lucia, Izzi Guido, D'Andrea Luca Domenico

机构信息

Istituto di Biostrutture e Bioimmagini, CNR-Consiglio Nazionale delle Ricerche, Via Pietro Castellino 111, 80131 Napoli, Italy.

Istituto di Scienze e Tecnologie Chimiche "Giulio Natta", CNR-Consiglio Nazionale delle Ricerche, Via Mario Bianco 9, 20131 Milano, Italy.

出版信息

Molecules. 2024 Jan 20;29(2):521. doi: 10.3390/molecules29020521.

DOI:10.3390/molecules29020521
PMID:38276597
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10818745/
Abstract

Axl receptor tyrosine kinase and its ligand Gas6 regulate several biological processes and are involved in both the onset and progression of tumor malignancies and autoimmune diseases. Based on its key role in these settings, Axl is considered a promising target for the development of molecules with therapeutic and diagnostic purposes. In this paper, we describe the molecular characterization of the recombinant Ig1 domain of Axl (Ig1 Axl) and its biochemical properties. For the first time, an exhaustive spectroscopic characterization of the recombinant protein through circular dichroism and fluorescence studies is also reported, as well as a binding analysis to its natural ligand Gas6, paving the way for the use of recombinant Ig1 Axl as a bait in drug discovery screening procedures aimed at the identification of novel and specific binders targeting the Axl receptor.

摘要

Axl受体酪氨酸激酶及其配体Gas6调节多种生物学过程，参与肿瘤恶性肿瘤和自身免疫性疾病的发生和发展。基于其在这些情况下的关键作用，Axl被认为是开发具有治疗和诊断目的分子的有前景的靶点。在本文中，我们描述了Axl重组Ig1结构域（Ig1 Axl）的分子特征及其生化特性。首次通过圆二色性和荧光研究对重组蛋白进行了详尽的光谱表征，以及对其天然配体Gas6的结合分析，为在旨在鉴定靶向Axl受体的新型特异性结合剂的药物发现筛选程序中使用重组Ig1 Axl作为诱饵铺平了道路。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/536235da57df/molecules-29-00521-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/8ebf6ebc6860/molecules-29-00521-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/e92406a51e50/molecules-29-00521-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/81266a995556/molecules-29-00521-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/49d849bcb339/molecules-29-00521-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/2f4e3ff47e75/molecules-29-00521-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/cbd4508545e9/molecules-29-00521-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/74a841526e43/molecules-29-00521-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/536235da57df/molecules-29-00521-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/8ebf6ebc6860/molecules-29-00521-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/e92406a51e50/molecules-29-00521-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/81266a995556/molecules-29-00521-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/49d849bcb339/molecules-29-00521-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/2f4e3ff47e75/molecules-29-00521-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/cbd4508545e9/molecules-29-00521-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/74a841526e43/molecules-29-00521-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8d2f/10818745/536235da57df/molecules-29-00521-g008.jpg

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Therapeutic peptides: current applications and future directions.治疗性肽：当前的应用及未来方向。
Signal Transduct Target Ther. 2022 Feb 14;7(1):48. doi: 10.1038/s41392-022-00904-4.
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Exploiting Protein N-Terminus for Site-Specific Bioconjugation.利用蛋白质N端进行位点特异性生物共轭
Molecules. 2021 Jun 9;26(12):3521. doi: 10.3390/molecules26123521.
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Therapeutic aspects of the Axl/Gas6 molecular system.Axl/Gas6分子系统的治疗学方面。
Drug Discov Today. 2020 Dec;25(12):2130-2148. doi: 10.1016/j.drudis.2020.09.022. Epub 2020 Sep 28.
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A screening study of high affinity peptide as molecular binder for AXL, tyrosine kinase receptor involving in Zika virus entry.一项关于高亲和力肽作为AXL分子结合剂的筛选研究，AXL是一种参与寨卡病毒进入的酪氨酸激酶受体。
Bioelectrochemistry. 2021 Feb;137:107670. doi: 10.1016/j.bioelechem.2020.107670. Epub 2020 Sep 7.
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Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update.FDA 批准的小分子蛋白激酶抑制剂的特性：2020 年更新。
Pharmacol Res. 2020 Feb;152:104609. doi: 10.1016/j.phrs.2019.104609. Epub 2019 Dec 17.
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AXL receptor tyrosine kinase as a promising anti-cancer approach: functions, molecular mechanisms and clinical applications.AXL 受体酪氨酸激酶作为一种有前途的抗癌方法：功能、分子机制和临床应用。
Mol Cancer. 2019 Nov 4;18(1):153. doi: 10.1186/s12943-019-1090-3.
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Biochemical and Conformational Characterization of Recombinant VEGFR2 Domain 7.重组 VEGFR2 结构域 7 的生化和构象特征。
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Monoclonal antibody therapy of solid tumors: clinical limitations and novel strategies to enhance treatment efficacy.实体瘤的单克隆抗体治疗：临床局限性及提高治疗效果的新策略
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