Mangostanin Derivatives as Novel and Orally Active Phosphodiesterase 4 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis with Improved Safety.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01085
Abstract: Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease, and its incidence rate is rapidly rising. However, effective therapies for the treatment of IPF are still lacking. Phosphodiesterase 4 (PDE4) inhibitors were reported to be… read more here.
Keywords: improved safety; fibrosis; idiopathic pulmonary; novel orally ... See more keywords
Puquitinib, a novel orally available PI3Kδ inhibitor, exhibits potent antitumor efficacy against acute myeloid leukemia
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Science"
DOI: 10.1111/cas.13263
Abstract: The PI3Kδ isoform (PIK3CD), also known as P110δ, is predominately expressed in leukocytes and has been implicated as a potential target in the treatment of hematological malignancies. In this report, we detailed the pharmacologic properties… read more here.
Keywords: pi3k; inhibitor; novel orally; efficacy ... See more keywords
Pharmacological profile of asundexian, a novel, orally bioavailable inhibitor of factor XIa
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Thrombosis and Haemostasis"
DOI: 10.1111/jth.15700
Abstract: Activated coagulation factor XI (FXIa) contributes to the development and propagation of thrombosis but plays only a minor role in hemostasis; therefore, it is an attractive antithrombotic target. read more here.
Keywords: profile asundexian; pharmacological profile; asundexian novel; novel orally ... See more keywords
Abstract 1185: H3B-8800, a novel orally available SF3b modulator, shows preclinical efficacy across spliceosome mutant cancers
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-1185
Abstract: Genomic characterization of hematologic and solid cancers has revealed recurrent somatic mutations affecting genes encoding the RNA splicing factors SF3B1, U2AF1, SRSF2 and ZRSR2. Recent data reveal that these mutations confer an alteration of function… read more here.
Keywords: novel orally; h3b; h3b 8800; spliceosome mutant ... See more keywords
S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth.
Sign Up to like & getrecommendations! Published in 2018 at "Oncotarget"
DOI: 10.2210/pdb6gl8/pdb
Abstract: Escape from apoptosis is one of the major hallmarks of cancer cells. The B-cell Lymphoma 2 (BCL-2) gene family encodes pro-apoptotic and anti-apoptotic proteins that are key regulators of the apoptotic process. Overexpression of the… read more here.
Keywords: selective potent; potent inhibitor; s55746; novel orally ... See more keywords