Development of Orally Bioavailable Peptides Targeting an Intracellular Protein: From a Hit to a Clinical KRAS Inhibitor

Cyclicpeptides as a therapeutic modality are attractinga lotof attention due to their potential for oral absorption and accessibilityto intracellular tough targets. Here, starting with a drug-like hitdiscovered using an mRNA display library, we describe a chemical optimizationthat led to the orally...

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Veröffentlicht in:	Journal of the American Chemical Society Jg. 145; H. 30; S. 16610 - 16620
Hauptverfasser:	Tanada, Mikimasa, Tamiya, Minoru, Matsuo, Atsushi, Chiyoda, Aya, Takano, Koji, Ito, Toshiya, Irie, Machiko, Kotake, Tomoya, Takeyama, Ryuuichi, Kawada, Hatsuo, Hayashi, Ryuji, Ishikawa, Shiho, Nomura, Kenichi, Furuichi, Noriyuki, Morita, Yuya, Kage, Mirai, Hashimoto, Satoshi, Nii, Keiji, Sase, Hitoshi, Ohara, Kazuhiro, Ohta, Atsushi, Kuramoto, Shino, Nishimura, Yoshikazu, Iikura, Hitoshi, Shiraishi, Takuya
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	WASHINGTON Amer Chemical Soc 02.08.2023
Schlagworte:	Chemistry Chemistry, Multidisciplinary Physical Sciences Science & Technology CHAIN PERMEABILITY SMALL-MOLECULE INHIBITORS DRUG DISCOVERY MESSENGER-RNA DISPLAY BINDING CYCLOSPORINE INSIGHTS
ISSN:	0002-7863, 1520-5126, 1520-5126
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