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Updated: Jun 3, 2025

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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在药物设计中的定位酶和传送器基础的沉性药物相互作用研究

Thomas Schroeter1, Kimberly Lapham1, Manthena V S Varma1

  • 1Department of Pharmacokinetics Dynamics & Metabolism, Pfizer Inc., Groton, Connecticut 06340, United States.

Journal of medicinal chemistry
|January 6, 2025
PubMed
概括

药物开发可以通过专注于关键酶和载体来简化药物相互作用 (DDI) 的早期评估. 这种方法有助于优先考虑候选人解决未满足的医疗需求,而不会影响安全.

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Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers18:57

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers

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Structure-Activity Relationships and Drug Design

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Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
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Drug interactions are a critical aspect of pharmacology and can occur when two or more drugs compete for the same binding site. This competition can result in one drug displacing another, altering the effect of the displaced drug. Drug interactions are complex processes that rely heavily on how much of the displacer drug is present and how strongly it can bind to the same sites as the displaced drug.
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