Btk Inhibitors: A Medicinal Chemistry and Drug Delivery Perspective.
Btk Inhibitors: A Medicinal Chemistry and Drug Delivery Perspective.
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DOI：
10.3390/ijms22147641
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发表时间：
2021-07-16
影响因子：
5.6
通讯作者：
Spallarossa A
中科院分区：
文献类型：
--
作者：
Brullo C;Villa C;Tasso B;Russo E;Spallarossa A
近年来，布鲁顿酪氨酸激酶（Btk）已成为药物化学研究的新靶点。自2013年批准伊曲替尼用于治疗不同的血液癌症（如白血病和淋巴瘤）以来，其他两种不可逆的Btk抑制剂已上市。为了克服不可逆Btk抑制剂的局限性，已经开发了可逆化合物，目前正在评估中。近年来，许多Btk抑制剂已获得专利并在文献中报道。本文综述了近年来开发的可逆Btk抑制剂及其在恶性肿瘤、慢性炎症和SARS-CoV-2感染等方面的临床试验和临床前研究进展。此外，报道了研究以增加伊鲁替尼生物利用度的纳米制剂。
In the past few years, Bruton’s tyrosine Kinase (Btk) has emerged as new target in medicinal chemistry. Since approval of ibrutinib in 2013 for treatment of different hematological cancers (as leukemias and lymphomas), two other irreversible Btk inhibitors have been launched on the market. In the attempt to overcome irreversible Btk inhibitor limitations, reversible compounds have been developed and are currently under evaluation. In recent years, many Btk inhibitors have been patented and reported in the literature. In this review, we summarized the (ir)reversible Btk inhibitors recently developed and studied clinical trials and preclinical investigations for malignancies, chronic inflammation conditions and SARS-CoV-2 infection, covering advances in the field of medicinal chemistry. Furthermore, the nanoformulations studied to increase ibrutinib bioavailability are reported.
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影响因子：
2.2
作者：
Goess, Christian;Harris, Christopher M.;Long, Andrew J.
通讯作者：
Long, Andrew J.
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14.8
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Bradshaw JM;McFarland JM;Paavilainen VO;Bisconte A;Tam D;Phan VT;Romanov S;Finkle D;Shu J;Patel V;Ton T;Li X;Loughhead DG;Nunn PA;Karr DE;Gerritsen ME;Funk JO;Owens TD;Verner E;Brameld KA;Hill RJ;Goldstein DM;Taunton J
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Burger, Jan A.