Small molecules in targeted cancer therapy: advances ... - Nature
2021年5月31日 · Since the first tyrosine kinase inhibitor imatinib was approved to enter the market by the US Food and Drug Administration (FDA) in 2001, an increasing number of small-molecule targeted drugs...
Small Molecule Kinase Inhibitor Drugs (1995–2021): Medical …
2021年10月8日 · FDA-approved small molecule kinase inhibitors from 1999 to 2020 for the treatment of cancer (orange), noncancerous indications (blue), or both (orange-blue lines).
Small molecules, big impact: 20 years of targeted therapy in oncology
2020年3月28日 · Several small molecule inhibitors target cellular metabolic vulnerabilities, including inhibitors of fatty acid synthase, nicotinamide phosphoribosyltransferase, isocitrate dehydrogenase, glutaminase, and polyamine and arginine metabolism.
Small molecule inhibitors targeting the cancers - PubMed
2022年10月13日 · Small molecule inhibitors are one of the primary targeted therapies for cancer. Due to their advantages in a wide range of targets, convenient medication, and the ability to penetrate into the central nervous system, many efforts have been devoted to developing more small molecule inhibitors.
Small molecule inhibitors targeting PD-L1, CTLA4, VISTA, TIM-3, …
The development of small-molecule inhibitors targeting CTLA-4 is confronted with significant challenges because of the unique properties of the CTLA-4 protein and its interactions with ligands CD80 and CD86. One major difficulty is the nature of the CTLA-4 binding interface, which is relatively flat and hydrophobic. ...
Small molecule inhibitors targeting the PD-1/PD-L1 signaling …
2020年3月9日 · In this review, we summarized a number of small molecule inhibitors based on three different therapeutic approaches interfering PD-1/PD-L1 signaling pathway: (1) blocking direct interaction...
Discovery of Small Molecule Interleukin 17A Inhibitors with …
2024年4月4日 · Herein, we report the discovery of a novel class of small molecule IL17A inhibitors, identified via a DNA-encoded chemical library screen, and their subsequent optimization to provide in vivo efficacious inhibitors.
Small molecule inhibitors targeting the cancers - Liu - 2022
Small molecule inhibitors are one of the primary targeted therapies for cancer. Due to their advantages in a wide range of targets, convenient medication, and the ability to penetrate into the central nervous system, many efforts have been devoted …
Small molecule inhibitors for cancer immunotherapy and …
2023年10月31日 · Following the success of cancer immunotherapy using large molecules against immune checkpoint inhibitors, the concept of using small molecules to interfere with intracellular negative regulators of anti-tumor immune responses has emerged in recent years.
A recent update on small‐molecule kinase inhibitors for targeted …
2022年3月21日 · In recent decades, numerous small-molecule kinase inhibitors have been developed and revolutionized the cancer treatment landscape. Despite their great potential, challenges remain in developing highly selective and effective kinase inhibitors, with toxicity and resistance issues frequently arising.