New cathepsin inhibitors to explore the fluorophilic properties of the S~2 pocket of cathepsin B: Design, synthesis, and biological evaluation

Fustero S.; Rodrigo V.; Sánchez-Rosell? M.; Del Pozo C.; Timoneda J.; Frizler M.; Sisay M.T.; Bajorath J.; Calle L.P.; Ca?ada F.J.; Jiménez-Barbero J.; Gütschow M.

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New cathepsin inhibitors to explore the fluorophilic properties of the S~2 pocket of cathepsin B: Design, synthesis, and biological evaluation

机译：探索组织蛋白酶B S〜2口袋的亲氟特性的新型组织蛋白酶抑制剂：设计，合成和生物学评估

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Fluor-in or out? Based on β,β-difluorinated cycloaliphatic amino acids, a library of new dipeptide nitriles was evaluated as human cathepsin inhibitors. The orientation of the fluorinated face relative to the protein structure of cathepsin B was elucidated by molecular modeling and NMR studies (see figure). For (R)-configured eutomers, the fluorine atoms are directed to the S~2 pocket, whereas in (S)-configured distomers, the fluorinated face is solvent-exposed.

机译：氟或氟？基于β，β-二氟环脂族氨基酸，评估了新的二肽腈文库作为人组织蛋白酶抑制剂。通过分子建模和NMR研究阐明了氟化面相对于组织蛋白酶B蛋白质结构的方向（参见图）。对于（R）构造的eu体，氟原子被定向到S_2凹穴，而在（S）构造的dis体中，氟化面暴露于溶剂中。

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《Chemistry: A European journal》 |2011年第19期|共5页
作者
Fustero S.; Rodrigo V.; Sánchez-Rosell? M.; Del Pozo C.; Timoneda J.; Frizler M.; Sisay M.T.; Bajorath J.; Calle L.P.; Ca?ada F.J.; Jiménez-Barbero J.; Gütschow M.;
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正文语种 eng
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fluorinated ligands; hydrolases; inhibitors; peptides; stereoselectivity;

机译：氟化配体;水解酶;抑制剂;肽;立体选择性;

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1. New cathepsin inhibitors to explore the fluorophilic properties of the S~2 pocket of cathepsin B: Design, synthesis, and biological evaluation [J] . Fustero S., Rodrigo V., Sánchez-Rosell? M., Chemistry: A European journal . 2011,第19期

机译：探索组织蛋白酶B S〜2口袋的亲氟特性的新型组织蛋白酶抑制剂：设计，合成和生物学评估
2. Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes [J] . Yuan Xiao-Yu, Ren Zhongyuan, Wu Yuqing, Bioorganic and medicinal chemistry . 2019,第6期

机译：抑制剂抑制剂对消化不良的软骨细胞抑制剂的设计，合成及生物学评价
3. Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors. [J] . Kishore Kumar GD, Chavarria GE, Charlton Sevcik A Bioorganic and Medicinal Chemistry Letters . 2010,第4期

机译：设计，合成和生物学评估基于硫半乳糖苷的组织蛋白酶L抑制剂。
4. Structure-based design and synthesis of cathepsin K inhibitors [C] . Regina Kasprzykowska, Franciszek Kasprzykowski, Xin Wang, European Peptide Symposium . 2002

机译：基于结构的组织蛋白酶K抑制剂的设计和合成
5. Design, Synthesis and Analysis of Potential Photo-Activatable Cathepsin K Inhibitors. [D] . Nisbett, Khalin Evania. 2017

机译：潜在的光活化组织蛋白酶K抑制剂的设计，合成和分析。
6. Design synthesis and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors [O] . G.D. Kishore Kumar, Gustavo E. Chavarria, Amanda K. Charlton-Sevcik, -1

机译：设计合成和生物评估基于硫半乳糖苷的组织蛋白酶L抑制剂
7. Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype [O] . Michael C. Myers, Parag P. Shah, Mary Pat Beavers, 2008

机译：组织蛋白酶抑制剂的设计，合成和评价：利用独特的硫代氨基甲酸盐

New cathepsin inhibitors to explore the fluorophilic properties of the S~2 pocket of cathepsin B: Design, synthesis, and biological evaluation

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