生物学千禧年难题
The Millennium Problems for Biology

原始链接: https://millenniumproblems.bio/

这项挑战要求开发出零样本(zero-shot)蛋白质结合剂,使其在细胞外给药后能够结合预先注册的细胞内靶标。参赛方案必须在没有任何湿实验优化、筛选或定向进化的前提下生成。在靶标公布后,方案必须在24小时内完成设计,并需在20个不同的靶标上实现80%的成功率。 递送机制必须具有临床治疗可行性,禁止使用电穿孔、转染或膜破坏等技术。由于小分子药物存在合成瓶颈,本次挑战仅限于蛋白质结合剂,且优先考虑模拟人源化单克隆抗体的设计。鉴于标准抗体通常难以有效穿透细胞,鼓励参赛者根据需要对蛋白质支架进行修饰,以确保其进入细胞内部。本挑战的最终目标是建立一个可靠、快速的计算框架,用于设计能够穿过细胞膜并中和高难度细胞内靶标的治疗性蛋白质。

抱歉。
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原文

Demonstrate the ability to produce protein binders against intracellular targets.

Specifically, demonstrate the ability to design zero-shot protein binders that, without further evolution or optimization, will reliably engage preregistered intracellular protein targets in living cells when administered extracellularly to those cells at pharmacologically supported concentrations. The cell entry mechanism must be plausible in a therapeutic context, i.e., transfection, intrabody expression, electroporation, membrane disruption, or similar methods are not permitted. The challenge will be considered complete when the design can be demonstrated against 20 preregistered targets with an 80% success rate. Once the targets are preregistered, the designs of the resulting proteins must be produced within 24 hours, and no wet lab work is allowed prior to evaluation except for the purpose of producing the designed proteins for assay. (Hence, for example, screening and target-specific evolution are not permitted once the targets are provided.)

The original intention of this problem was specifically to design antibodies against intracellular targets. However, it is anticipated that modifications to the antibody scaffold will be required in order for the problem to be solvable. Since we cannot put an upper bound on the magnitude of the modifications required, we have broadened the problem to encompass any protein binders. However, solutions that involve binders resembling humanized monoclonal antibodies will be greatly preferred. The problem would likely be even more impactful if solved in general for small molecule binders, rather than protein binders or antibodies. However, with small molecule binders, synthesis is a major bottleneck that would limit validation, and thus we have chosen to restrict the scope to protein binders.

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