Design and synthesis of (S)- and (R)-α-(phenyl)ethylamine-derived NH-type ligands and their application for the chemical resolution of α-amino acids

2014 ◽  
Vol 12 (32) ◽  
pp. 6239 ◽  
Author(s):  
Ryosuke Takeda ◽  
Akie Kawamura ◽  
Aki Kawashima ◽  
Hiroki Moriwaki ◽  
Tatsunori Sato ◽  
...  
Keyword(s):  
Amino Acids ◽  
Design And Synthesis ◽  
Chemical Resolution

Chemical Resolution of C,N-Unprotected α-Substituted β-Amino Acids Using Stable and Recyclable Proline-Derived Chiral Ligands

2018 ◽  
Vol 83 (17) ◽  
pp. 9870-9878 ◽  
Author(s):  
Shuni Wang ◽  
Yong Nian ◽  
Shengbin Zhou ◽  
Jiang Wang ◽  
Hong Liu
Keyword(s):  
Amino Acids ◽  
Chiral Ligands ◽  
Chemical Resolution

Molecular Design and Synthesis of Artificial Ion Channels Based on Cyclic Peptides Containing Unnatural Amino Acids

2001 ◽  
Vol 66 (9) ◽  
pp. 2978-2989 ◽  
Author(s):  
Hitoshi Ishida ◽  
Zhi Qi ◽  
Masahiro Sokabe ◽  
Kiyoshi Donowaki ◽  
Yoshihisa Inoue
Keyword(s):  
Amino Acids ◽  
Ion Channels ◽  
Unnatural Amino Acids ◽  
Cyclic Peptides ◽  
Molecular Design ◽  
Design And Synthesis

scholarly journals Rational Design and Synthesis of Novel Dual Protacs for Simultaneous Degradation of EGFR and PARP

2021 ◽  
Author(s):  
Mengzhu Zheng ◽  
Junfeng Huo ◽  
Xiaoxia Gu ◽  
Canrong Wu ◽  
Qingzhe Zhang ◽  
...  
Keyword(s):  
Amino Acids ◽  
Drug Discovery ◽  
Rational Design ◽  
Bispecific Antibodies ◽  
Design And Synthesis ◽  
Synthetic Strategy ◽  
Dual Targeting ◽  
Different Types ◽  
Natural Amino Acids ◽  
Simultaneous Degradation

Inspired by the success of dual targeting drugs, especially bispecific antibodies, we propose to combine the concept of protac and dual targeting to design and synthesize dual protac molecules with the function of degrading two completely different types of targets simultaneously. A library of novel dual targeting protac molecules have been rationally designed and prepared. A convergent synthetic strategy has been utilized to achieve high synthetic efficiency. These dual protac structures are characterized by using trifunctional natural amino acids as star-type core linkers to connect two independent inhibitors and E3 ligands together. In this study, gefitinib, olaparib, and CRBN or VHL E3 ligand were used as substrates to synthesize novel dual protacs. They successfully degraded both EGFR and PARP simultaneously in cancer cells. Being the first successful example of dual protacs, this technique will greatly widen the range of application of the protac method and open up a new field for drug discovery.

scholarly journals Recent advances in the synthesis and application of fluorescent α-amino acids

2016 ◽  
Vol 14 (38) ◽  
pp. 8911-8921 ◽  
Author(s):  
Alexander H. Harkiss ◽  
Andrew Sutherland
Keyword(s):  
Amino Acids ◽  
Biological Systems ◽  
Design And Synthesis ◽  
Recent Advances

The design and synthesis of new fluorescent α-amino acids as well as their application in imaging of biological systems has been reviewed.

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