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Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR.
Zheng, Mengmeng; Li, Chunpu; Zhou, Mi; Jia, Ru; Cai, Gang; She, Fengyu; Wei, Lulu; Wang, Shaohui; Yu, Jie; Wang, Dingyan; Calcul, Laurent; Sun, Xingmin; Luo, Xiaomin; Cheng, Feng; Li, Qi; Wang, Yan; Cai, Jianfeng.
Afiliação
  • Zheng M; Department of Chemistry, University of South Florida, 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
  • Li C; Department of Chemistry, University of South Florida, 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
  • Zhou M; Department of Medical Oncology & Cancer Institute of Medicine, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
  • Jia R; Department of Chemistry, University of South Florida, 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
  • Cai G; Department of Medical Oncology & Cancer Institute of Medicine, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
  • She F; Department of Medical Oncology & Cancer Institute of Medicine, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
  • Wei L; Department of Chemistry, University of South Florida, 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
  • Wang S; Department of Chemistry, University of South Florida, 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
  • Yu J; Department of Molecular Medicine, Morsani College of Medicine, University of South Florida, Tampa, Florida 33612, United States.
  • Wang D; Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
  • Calcul L; Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
  • Sun X; Department of Chemistry, University of South Florida, 4202 E. Fowler Avenue, Tampa, Florida 33620, United States.
  • Luo X; Department of Molecular Medicine, Morsani College of Medicine, University of South Florida, Tampa, Florida 33612, United States.
  • Cheng F; Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
  • Li Q; Department of Pharmaceutical Sciences, College of Pharmacy, University of South Florida, Tampa, Florida 33612, United States.
  • Wang Y; Department of Medical Oncology & Cancer Institute of Medicine, Shuguang Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
  • Cai J; Academy of Integrative Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
J Med Chem ; 64(15): 11219-11228, 2021 08 12.
Article em En | MEDLINE | ID: mdl-34297567
ABSTRACT
It is very promising to target the extracellular domain of epidermal growth factor receptor (EGFR) for developing novel and selective anticancer therapies. Herein, we report the discovery of a novel small molecule, M-2-5, from a one-bead-two-compound (OBTC) cyclic γ-AApeptide library. The molecule was found to bind tightly to the extracellular domain of EGFR. Intriguingly, this molecule could also effectively antagonize EGF-stimulated EGFR phosphorylation and downstream signal transduction. Furthermore, together with its remarkable resistance to proteolytic degradation, M-2-5 was shown to effectively inhibit cell proliferation and migration in vitro and suppresses the growth of tumor in the A549 xenograft model in vivo, highlighting its potential therapeutic application for cancer treatment.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Descoberta de Drogas / Peptidomiméticos Idioma: En Ano de publicação: 2021 Tipo de documento: Article
Texto completo
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PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Descoberta de Drogas / Peptidomiméticos Idioma: En Ano de publicação: 2021 Tipo de documento: Article