Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01279
Abstract: Although Bruton's tyrosine kinase (BTK) has been recognized as a validated drug target for the treatment of B-cell malignances, the emergence of clinical resistance to the first-generation covalent BTK inhibitors is becoming a serious concern.… read more here.
Keywords: potent selective; inhibitor; btk; orally available ... See more keywords
Discovery of Selenium-Containing STING Agonists as Orally Available Antitumor Agents.
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DOI: 10.1021/acs.jmedchem.2c00634
Abstract: Activation of the stimulator of interferon genes (STING) pathway to achieve antitumor response is an attractive approach for cancer immunotherapy. In this study, we report the identification of BSP16 (LF250) as a potent, orally available… read more here.
Keywords: selenium containing; antitumor; sting agonists; orally available ... See more keywords
A conformation-specific ON-switch for controlling CAR T cells with an orally available drug
Sign Up to like & getrecommendations! Published in 2020 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.1911154117
Abstract: Significance Molecular ON-switches are important tools in chemical biology, enabling protein–protein interactions to be regulated by small molecules. However, currently available ON-switches that induce conditional heterodimerization are suboptimal for therapeutic applications. In this study, we… read more here.
Keywords: protein; small molecule; switch; drug ... See more keywords
Apixaban, an orally available anticoagulant, inhibits SARS-CoV-2 replication and its major protease in a non-competitive way
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Molecular Cell Biology"
DOI: 10.1093/jmcb/mjac039
Abstract: Dear Editor, The severe coronavirus disease 2019 (COVID-19) is associated with coagulopathy. Anticoagulants, such as low-molecular-weight heparin, warfarin, thrombin inhibitors, and factor Xa (FXa) inhibitors, are thus recommended by the American Society of Hematology and… read more here.
Keywords: adam 2021; protease; orally available; apixaban orally ... See more keywords
Antifungal chemotherapies and immunotherapies for the future
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DOI: 10.1111/pim.12960
Abstract: Human fungal pathogens cause a broad plethora of infections, spanning cutaneous dermatophytoses to invasive infections in immunocompromised hosts. As eukaryotic pathogens are capable of morphotype switching, they present unique challenges both for drug development and… read more here.
Keywords: fungal disease; orally available; antifungal chemotherapies; chemotherapies immunotherapies ... See more keywords
Abstract 515: Discovery of potent and orally available small molecule inhibitors of the SOS1-KRAS interaction
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-515
Abstract: Abnormal activating mutation of KRAS is frequently found in many human cancers, including pancreatic ductal adenocarcinoma (PDAC), colorectal cancer (CRC), and non-small cell lung cancer (NSCLC). KRAS activating mutations lead to hyperactivation of the MAPK/ERK… read more here.
Keywords: interaction; orally available; discovery potent; sos1 kras ... See more keywords