16018-83-0Relevant articles and documents
BIGUANIDE COMPOUNDS AND USE THEREOF
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Paragraph 0524-0531, (2021/02/16)
The present invention relates to a biguanide compound and uses thereof. More specifically, the present invention relates to: a biguanide derivative exhibiting excellent effects in inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence; a manufacturing method of the biguanide derivative; and a pharmaceutical composition containing the biguanide derivative as an active component.
Identifying Lysophosphatidic Acid Acyltransferase β (LPAAT-β) as the Target of a Nanomolar Angiogenesis Inhibitor from a Phenotypic Screen Using the Polypharmacology Browser PPB2
Poirier, Marion,Awale, Mahendra,Roelli, Matthias A.,Giuffredi, Guy T.,Ruddigkeit, Lars,Evensen, Lasse,Stooss, Amandine,Calarco, Serafina,Lorens, James B.,Charles, Roch-Philippe,Reymond, Jean-Louis
supporting information, p. 224 - 236 (2018/12/13)
By screening a focused library of kinase inhibitor analogues in a phenotypic co-culture assay for angiogenesis inhibition, we identified an aminotriazine that acts as a cytostatic nanomolar inhibitor. However, this aminotriazine was found to be completely inactive in a whole-kinome profiling assay. To decipher its mechanism of action, we used the online target prediction tool PPB2 (http://ppb2.gdb.tools), which suggested lysophosphatidic acid acyltransferase β (LPAAT-β) as a possible target for this aminotriazine as well as several analogues identified by structure–activity relationship profiling. LPAAT-β inhibition (IC50 ≈15 nm) was confirmed in a biochemical assay and by its effects on cell proliferation in comparison with a known LPAAT-β inhibitor. These experiments illustrate the value of target-prediction tools to guide target identification for phenotypic screening hits and significantly expand the rather limited pharmacology of LPAAT-β inhibitors.
NOVEL CYCLIC GMP-AMP SYNTHASE (CGAS) INHIBITORS AND THEIR METHOD OF USE
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Page/Page column 64-65, (2020/01/08)
Methods of treating diseases related to cGAS activation. Small molecule inhibitors of cGAS and pharmaceutical compositions and uses thereof in treating autoimmune diseases or inflammation.
BIGUANIDE COMPOUNDS AND USE THEREOF
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Paragraph 0356; 0357; 0359; 0360, (2015/05/13)
The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for pre