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

Usama M Ammar1, Mohammed S Abdel-Maksoud2, Chang-Hyun Oh3

  • 1Center 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.

Insights

RAF pathway mutations drive cancer by promoting uncontrolled cell growth. Recent research focuses on diverse RAF inhibitors, showing potent anti-cancer activity, with this review highlighting investigations over the past five years.

Area of Science:

  • Oncology
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • The mitogen-activated protein kinase (MAPK) signaling pathway is frequently altered in cancer.
  • Mutations in RAF components of the MAPK pathway lead to its auto-activation, driving uncontrolled cell proliferation.
  • RAF signaling is a critical target for anti-cancer drug development.

Purpose of the Study:

  • To review recent investigations of RAF inhibitors over the last five years.
  • To highlight the development of diverse chemical scaffolds targeting the RAF component.
  • To summarize the anti-cancer activity of identified RAF inhibitors.

Main Methods:

  • Literature review of scientific publications from the last five years.
  • Analysis of studies reporting on RAF inhibitors and their chemical scaffolds.
  • Evaluation of reported anti-cancer activities and mechanisms of action.

Main Results:

  • Numerous chemical scaffolds targeting RAF have been identified.
  • Many of these RAF inhibitors demonstrate significant anti-cancer potency.
  • Recent research has expanded the landscape of RAF-targeted therapies.

Conclusions:

  • RAF inhibitors represent a promising therapeutic strategy for cancers driven by MAPK pathway mutations.
  • Continued investigation into novel chemical scaffolds is crucial for advancing RAF-targeted cancer treatments.
  • The development of effective RAF inhibitors holds potential for controlling tumor growth and proliferation.

Related Concept Videos

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
579
Drugs for Treatment of Crohn's Disease in IBD Using Biologic Agents: Anti-TNF01:24

Drugs for Treatment of Crohn's Disease in IBD Using Biologic Agents: Anti-TNF

Tumor Necrosis Factor (TNF), a proinflammatory cytokine, contributes significantly to the inflammation seen in Crohn's disease. It exists as soluble TNF and membrane-bound TNF, with actions mediated through TNF receptors (TNFR). TNFR activation leads to the release of proinflammatory cytokines, T-cell activation, collagen production, and leukocyte migration, all contributing to inflammation in Crohn's disease. Anti-TNF monoclonal antibodies, namely infliximab (Remicade), adalimumab...
558
Accelerators01:17

Accelerators

Accelerators in concrete serve as admixtures to speed up the hardening process, enabling the concrete to achieve early strength faster. Although accelerators do not necessarily impact the time it takes concrete to set, they reduce this time in practice. A common accelerator is calcium chloride, which is particularly useful for hastening early strength development in cold weather or for rapid repair jobs that require quick heat generation after mixing.
The effectiveness of calcium chloride can...
290
Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
11.0K
Average Acceleration01:30

Average Acceleration

The importance of understanding acceleration spans our day-to-day experiences, as well as the vast reaches of outer space and the tiny world of subatomic physics. In everyday conversation, to accelerate means to speed up. For instance, we are familiar with the acceleration of our car; the harder we apply our foot to the gas pedal, the faster we accelerate. The greater the acceleration, the greater the change in velocity over a given time. Acceleration is widely seen in experimental physics. In...
14.0K
Instantaneous Acceleration01:16

Instantaneous Acceleration

Acceleration is in the direction of the change in velocity, but it is not always in the direction of motion. When an object slows down, its acceleration is opposite to the direction of its motion. Although commonly referred to as deceleration, this causes confusion in our analysis as deceleration is not a vector, and does not point to a specific direction with respect to a coordinate system. Therefore, the term deceleration is not used. For example, when a subway train slows down, it...
23.2K