Project Background
A biotechnology company sought to optimize its existing AR small molecule and develop a PROTAC candidate to expand beyond the therapeutic strategy of traditional inhibitors. The project was at an early R&D stage, and the client needed support in clarifying target degradability, defining an E3 ligase selection strategy, and improving the efficiency of assay setup and validation.
Our Support
To address the client’s needs, we first conducted degradability analysis around the AR target and designed multiple PROTAC candidate series based on the existing active molecule. During the project, we evaluated both CRBN- and VHL-based E3 ligase strategies and systematically optimized the warhead, linker length, flexibility, and conjugation sites. We then assessed degradation efficiency and activity performance through Western blot, cell-based degradation assays, and dose–response analysis. In total, we designed and synthesized more than 20 PROTAC molecules and identified 2 candidates with nanomolar AR degradation activity, clear dose dependency, and favorable cellular activity.
Client Testimonial
The BOC Sciences team provided efficient and professional support throughout the design and advancement of our PROTAC project. Their expertise in molecular design, experimental execution, and result interpretation helped us define the optimization direction more quickly and accelerate overall project progress.
Project Background
An innovative drug discovery company aimed to build a new PROTAC pipeline for the treatment of Tau-related neurodegenerative diseases and required candidates with good brain penetration potential to explore therapeutic strategies beyond traditional small-molecule inhibitors. The client had not yet identified the optimal target entry point or a clear molecular development plan and therefore sought external professional support to advance the project systematically, from target screening and degradability assessment to molecular design and candidate delivery.
Our Support
We first worked closely with the client to clarify the project’s application direction, expected degradation outcomes, and candidate advancement goals. We then screened 8 potential targets across Tau-related pathways and protein functions, taking into account druggability, PROTAC development feasibility, patent clearance potential, competitive landscape, and research novelty, and identified the most suitable targets for project progression. After target selection, we combined literature research, molecular modeling, and screening strategies to systematically evaluate different warhead, E3 ligase, and linker combinations, and through multiple rounds of molecular design and optimization, delivered more than 30 PROTAC design proposals to the client. We then carried out activity screening and degradation validation and identified several candidate molecules that met the client’s expectations, showing good brain penetration potential in the PAMPA-BBB assay and clear Tau protein degradation activity.
Client Testimonial
From initial requirement discussions and target screening to molecular design and activity validation, BOC Sciences provided systematic and efficient support for our PROTAC project. The team demonstrated strong professionalism in both technical execution and project advancement, helping us obtain promising candidates more quickly.
Expands Access to Difficult Targets
