<i>De Novo</i> Discovery of α,α-Disubstituted α‑amino Acid-Containing α‑helical Peptides as Competitive PPARγ PPI Inhibitors

α,α-Disubstituted α-amino acids (dαAAs) are important building blocks for peptidomimetics as they are strong inducers of helicity and protect against proteolytic degradation. However, <i>de novo</i> discovery of dαAA-containing peptides with genetically encoded libraries is limited due t...

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التفاصيل البيبلوغرافية
المؤلف الرئيسي:	Maxwell Sigal (22561153) (author)
مؤلفون آخرون:	Markus Egner (17049285) (author), Chikako Okada (11632265) (author), Daniel Merk (1373682) (author), Toru Sengoku (132922) (author), Takayuki Katoh (25496) (author), Hiroaki Suga (295809) (author)
منشور في:	2025
الموضوعات:	Biophysics Biochemistry Cell Biology Pharmacology Biotechnology Cancer Inorganic Chemistry Plant Biology Environmental Sciences not elsewhere classified Chemical Sciences not elsewhere classified throughput (> 10 ray crystallography revealed poor incorporation efficiency optimized ribosomal incorporation important building blocks de novo </ genetically encoded libraries multiple achiral dαaas identify novel α containing peptides bound 12 </ sup helical discovery platform containing peptides cellulo </ peptide libraries helical peptides hit peptides helical conformation work validates strong inducers providing access proteolytically stable proteolytic degradation new chemical macrocyclic α limited due interface via disubstituted α conformational space cell permeable amino acids affinity selection activated receptor
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<i>De Novo</i> Discovery of α,α-Disubstituted α‑amino Acid-Containing α‑helical Peptides as Competitive PPARγ PPI Inhibitors

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