SURVIVAL SIGNALING INHIBITORS AS CANCER DRUGS

生存信号抑制剂作为抗癌药物

• 批准号: 6287886
• 负责人: ELIZABETH SHARLOW
• 金额: $ 25.14万
• 依托单位: PROLX PHARMACEUTICALS, LP
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-02-08 至 2002-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6287886
• 关键词: antineoplastics; biological signal transduction; drug design /synthesis /production; drug discovery /isolation; drug screening /evaluation; enzyme inhibitors; laboratory mouse; phosphatidylinositols; protein kinase; tumor suppressor genes

ProlX Pharmaceuticals has demonstrated that there is strong evidence for the following: 1) PtdIns-3-kinase and Akt are two novel validated molecular targets for anti-cancer drug discovery; 2) The targets are relevant to a variety for human cancers; and 3) Inhibiting the targets with a small molecule drug should in principle overcome the effects of the human tumor suppressor gene PTEN. The objective of the Phase I study, to be conducted by ProlX Pharmaceuticals, is to identify, form a group of 4 analogues with different in vitro properties, the most active in vivo anti- tumor compound. ProlX Pharmaceuticals will establish the activity of the lead compounds against tumor xenografts and obtain preliminary information whether the compounds are orally active. PROPOSED COMMERCIAL APPLICATIONS: One in early four deaths in the US is due to cancer. The overall cancer drug market exceeds $2 billion in the USA. There is significant need to identify novel and selective small molecule-based cancer therapies. The proposal seeks to undertake preclinical evaluation of a novel group of clinical candidates and initiate a Phase 1 Clinical Trial for its eventual use as a therapy against ovarian, pancreatic prostate and breast cancer.

ProlX Pharmaceuticals已经证明，有强有力的证据表明：1）PtdIns-3-激酶和Akt是抗癌药物发现的两种新的经验证的分子靶标; 2）靶标与多种人类癌症相关;以及3）用小分子药物抑制靶标原则上应克服人类肿瘤抑制基因PTEN的作用。将由ProIX Pharmaceuticals进行的I期研究的目的是鉴定最具体内活性的抗肿瘤化合物，形成具有不同体外性质的4种类似物的组。ProlX Pharmaceuticals将确定先导化合物对肿瘤异种移植物的活性，并获得化合物是否具有口服活性的初步信息。 拟议的商业应用：在美国，四分之一的早期死亡是由于癌症。在美国，整个癌症药物市场超过20亿美元。非常需要鉴定新的和选择性的基于小分子的癌症疗法。该提案旨在对一组新的临床候选药物进行临床前评估，并启动1期临床试验，以最终用于治疗卵巢癌、胰腺癌、前列腺癌和乳腺癌。