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![[Figure 4]](raj5002fig4mag.jpg)
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Figure 4
Structural biology across the pharmaceutical R&D continuum, from discovery to development. The schematic illustrates how structural biology supports drug discovery and development activities from target identification through post-approval. The teal arrow traces the discovery-to-development trajectory, including target validation, construct design, screening, hit-to-lead and lead optimization, preclinical testing, clinical development, regulatory approval and post-market safety surveillance. Across this continuum, structural biology enables mechanistic understanding and modality selection, informs construct and assay design and, once tractable chemical matter is identified, guides structure–activity relationships (SAR) and informs structure-based drug design. In late discovery and preclinical development, structural approaches mitigate off-target liabilities (e.g. PXR, CYPs, HERG), enable structural studies for biocatalysis engineering and support the generation of crystalline suspensions of biologics. It also allows the structure determination of engineered cyclic peptides and small molecules by X-ray and microED analysis. Downstream applications include antibody epitope mapping and potency assessment, formulation design, optimization of manufacturing processes (e.g. quality control of virus-like particles), protecting intellectual property through determination of absolute configuration and in situ structural analysis of drug action within tissues. Structural biology continues to inform quality control and product characterization throughout life-cycle management. Created in BioRender. Gabelli, S. (2026), https://BioRender.com/ovp1tyq. |
![[Figure 4]](raj5002fig4.jpg)
 | STRUCTURAL BIOLOGY |
ISSN: 2059-7983
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