Abstract：
UNASSIGNED: The Hippo pathway represents a new opportunity for the treatment of cancer. Overexpression of Yes-associated protein (YAP) or transcriptional coactivator with PDZ-binding motif (TAZ) or TEAD has been demonstrated in cancers and YAP mediates resistance to cancer drugs. Since 2018, the potential of this pathway has been illustrated by numerous articles and patents and the first drugs entering in clinical trial phase 1.
UNASSIGNED: This review is limited to published patent applications that have disclosed direct small-molecule inhibitors of the YAP/TAZ-TEAD interaction.
UNASSIGNED: The YAP/TAZ-TEAD transcriptional complex is a promising target for the treatment of cancer. Approximately 30 international patents (used database: Sci-finder, query: TEAD; documents: patents; period: from 2017-January 2022) that disclose TEAD transcriptional inhibitors have been filled since 2018. The mechanism of action is not always described in the patents, we can divide the drugs into three different categories: (i) external TEAD ligands; (ii) non-covalent TEAD ligands of the palmitate pocket; (iii) covalent TEAD ligands, which bind into the palmitate pocket. The first molecules in clinical trial phase 1 are non-covalent TEAD ligands. The selective TEAD ligand have also been patented, published and selectivity could be of great interest for personalized medicine.
UNASSIGNED: This review is limited to published patent applications that have disclosed direct small-molecule inhibitors of the YAP/TAZ-TEAD interaction.
UNASSIGNED: The YAP/TAZ-TEAD transcriptional complex is a promising target for the treatment of cancer. Approximately 30 international patents (used database: Sci-finder, query: TEAD; documents: patents; period: from 2017-January 2022) that disclose TEAD transcriptional inhibitors have been filled since 2018. The mechanism of action is not always described in the patents, we can divide the drugs into three different categories: (i) external TEAD ligands; (ii) non-covalent TEAD ligands of the palmitate pocket; (iii) covalent TEAD ligands, which bind into the palmitate pocket. The first molecules in clinical trial phase 1 are non-covalent TEAD ligands. The selective TEAD ligand have also been patented, published and selectivity could be of great interest for personalized medicine.
摘要：
■Hippo途径代表了治疗癌症的新机会。Yes相关蛋白（YAP）或具有PDZ结合基序（TAZ）或TEAD的转录共激活因子的过表达已在癌症中得到证实，YAP介导对癌症药物的抗性。自2018年以来，该途径的潜力已被许多文章和专利以及第一批进入临床试验阶段的药物所证明。
■本综述限于公开了YAP/TAZ-TEAD相互作用的直接小分子抑制剂的公开专利申请。
■YAP/TAZ-TEAD转录复合物是治疗癌症的有希望的靶标。大约30项国际专利(使用数据库：Sci-finder，查询：TEAD；文件：专利；期间：从2017年1月至2022年1月），公开TEAD转录抑制剂自2018年以来一直在填充。作用机制并不总是在专利中描述，我们可以将药物分为三个不同的类别:(i)外部TEAD配体;(ii)棕榈酸酯口袋的非共价TEAD配体;(iii)共价TEAD配体,结合到棕榈酸盐口袋里。临床试验阶段1中的第一个分子是非共价TEAD配体。选择性TEAD配体也已获得专利，出版和选择性可能对个性化医疗非常感兴趣。
■本综述限于公开了YAP/TAZ-TEAD相互作用的直接小分子抑制剂的公开专利申请。
■YAP/TAZ-TEAD转录复合物是治疗癌症的有希望的靶标。大约30项国际专利(使用数据库：Sci-finder，查询：TEAD；文件：专利；期间：从2017年1月至2022年1月），公开TEAD转录抑制剂自2018年以来一直在填充。作用机制并不总是在专利中描述，我们可以将药物分为三个不同的类别:(i)外部TEAD配体;(ii)棕榈酸酯口袋的非共价TEAD配体;(iii)共价TEAD配体,结合到棕榈酸盐口袋里。临床试验阶段1中的第一个分子是非共价TEAD配体。选择性TEAD配体也已获得专利，出版和选择性可能对个性化医疗非常感兴趣。
