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Updated: Sep 8, 2025

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通过移除被困水分子来优化丁氨酸减小酶 (PAD) 抑制剂

Mark E Schnute1, Gary M Chinigo2, Kentaro Futatsugi1

  • 1Medicine Design, Pfizer Inc., Cambridge, Massachusetts 02139, United States.

ACS medicinal chemistry letters
|August 20, 2025
PubMed
概括

研究人员优化了一种针对自身免疫性疾病和癌症的新型抑制剂, 这种改进的化合物具有强大的抑制和有利于潜在治疗的药物动力学特性.

关键词:
在 PADI2在 PADI4聚结合点其他类型达尔金因脱酶水分子的移位

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Ligand Binding Sites02:40

Ligand Binding Sites

Proteins are dynamic macromolecules that carry out a wide variety of essential processes; however, the activities of most proteins depend on their interactions with other molecules or ions, known as ligands.
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
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