Recent advances of RAF (rapidly accelerated fibrosarcoma) inhibitors as anti-cancer agents

Eur J Med Chem. 2018 Oct 5:158:144-166. doi: 10.1016/j.ejmech.2018.09.005.

Usama M Ammar ¹, Mohammed S Abdel-Maksoud ², Chang-Hyun Oh ³

Affiliations

1 Center for Biomaterials, Korea Institute of Science & Technology (KIST), Seoul, Seongbuk-gu, 02792, Republic of Korea; Department of Biomolecular Science, University of Science & Technology (UST), Daejeon, Yuseong-gu, 34113, Republic of Korea; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ahram Canadian University, Giza, 12566, Egypt.
2 Medicinal & Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre (NRC), Dokki, Giza, 12622, Egypt.
3 Center for Biomaterials, Korea Institute of Science & Technology (KIST), Seoul, Seongbuk-gu, 02792, Republic of Korea; Department of Biomolecular Science, University of Science & Technology (UST), Daejeon, Yuseong-gu, 34113, Republic of Korea. Electronic address: [email protected].

PMID: 30216849 DOI: 10.1016/j.ejmech.2018.09.005

Abstract

Frequent oncogenic mutations have been identified in MAPK (mitogen-activated protein kinase) signaling pathway components. As a result, MAPK pathway is associated with human Cancer initiation, in particular Raf (rapidly accelerated fibrosarcoma) component. The mutation in Raf component leads to auto-activation of MAPK signaling pathway, stimulating the uncontrolled cell growth and proliferation. In last few years, diverse chemical scaffolds have been identified as Raf inhibitors. Most of these scaffolds show potent anti-cancer activity. The present review highlights the recent investigations of Raf inhibitors during the last five years.

Keywords

Anti-cancer agents; MAPK; RAF inhibitors.

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