Epidemiology of Scabies in Palestine

Hamarsheh, Omar

doi:10.1007/978-3-030-36811-1_149

Cited by 1 publication

(1 citation statement)

References 26 publications

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“…This process can be corrupted to become an oncogenic driver of cancer when KRAS is mutated and overactivated. 35 Besides direct KRAS inhibitors, tremendous effort has been focused on indirect approaches to inhibit KRAS signaling. Upstream inhibition, including receptor tyrosine kinase inhibitors such as sorafenib (NCT01715441) and regorafenib (NCT03520842), GEF (SOS) inhibitors such as BI 1701963 (NCT04111458), and SHP2 inhibitors such as TNO155 (NCT03114319) and JAB-3312 (NCT04045496), provides promising treatment for KRAS-mutated cancer patients, and their recent developments have been reviewed elsewhere.…”

Section: Kras Mutations and Signaling Pathwaysmentioning

confidence: 99%

Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics

et al. 2020

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KRAS, the most frequently mutated oncogene, plays a predominant role in driving initiation and progression of cancers. Decades of effort to target KRAS using small molecules has been unsuccessful, causing KRAS to be considered an “undruggable” cancer target. However, this view began to change recently, as drug discovery techniques have developed several KRAS G12C allosteric inhibitors that are currently being evaluated in clinical trials. Herein we provide an in-depth analysis of the structure and binding pockets of KRAS, medicinal chemistry optimization processes, and the biological characterization of small-molecule inhibitors that directly target KRAS, including covalent allosteric inhibitors specific for the G12C mutant, GTP-competitive inhibitors targeting the nucleotide-binding site, and protein–protein interaction inhibitors that bind in the switch I/II pocket or the A59 site. Additionally, we propose potential challenges faced by these new classes of KRAS inhibitors under clinical evaluation.

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Section: Kras Mutations and Signaling Pathwaysmentioning

confidence: 99%