Translational PK–PD for targeted protein degradation
Abstract
This tutorial review provides practical insights and a proposed roadmap for building the translational PK–PD understanding for protein degrader therapeutics.
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PK and PD liabilities are likely to emerge for small-molecule degraders, especially for relatively large PROTAC compounds.
“Pharmacokinetics (PK) and pharmacodynamics (PD) liabilities are likely to emerge for small-molecule degraders, especially in the case of the relatively large PROTAC compounds.73”
From Advancing Targeted Protein Degradation via Multiomics Profiling and Artificial Intelligence (2023) · cites this paper as [73]
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- Authors
- Bartlett, D. W., & Gilbert, A. M.
- Affiliations
- Pfizer (United States) (US)
- Corresponding author
- Bartlett, Derek W.
- Venue
- Chemical Society Reviews
- Publisher
- Royal Society of Chemistry (RSC)
- Published
- 2022
- Volume
- 51
- Issue
- 9
- Pages
- 3477-3486
- ISSN
- 0306-0012 (ISSN-L)
- 1460-4744
- OpenAlex
- W4224302152
- Cited by
- 55
- References
- 29
- Citations by year
- 2026: 12 · 2025: 12 · 2024: 16 · 2023: 13 · 2022: 2
- FWCI
- 1.12
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Chemical Society Reviews (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Pfizer
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
- Keywords
- targeted protein degradation, protein degraders, pharmacokinetics, pharmacodynamics, pharmacokinetic-pharmacodynamic modeling, translational pharmacology, drug development, mathematical modeling, rational drug design
- MeSH terms
- Models, Biological, Proteolysis
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