The SRPK inhibitor N-(2-(piperidin-1-yl)-5-(trifluoromethyl)phenyl) isonicotinamide (SRPIN340) increases the immune response against metastatic melanoma in mice.

Cancers have a strong relationship with immune cells in their microenvironment, which significantly influences tumor proliferation and progression. Thus, pharmacological strategies that stimulate the immune system to combat tumor cells are promising for better therapeutic efficacy. Deregulated expression of the splicing regulatory serine arginine protein kinases (mostly SRPK1 and SRPK2) has been found in different cancer types, leading to the expression of isoforms related to tumor growth and metastasis.

A late-stage diversification via Heck-Matsuda arylation: Straightforward synthesis and cytotoxic/antiproliferative profiling of novel aryl-labdane-type derivatives.

In the current study a late-stage diversification of unactivated olefins labd-8(17)-en-15-oic acid (1a) and methyl labd-8(17)-en-15-oate (1b) via Heck-Matsuda arylation is described. The reaction provided straightforward and practical access to a series of novel aryl-labdane-type derivatives (HM adducts 3a-h) in moderate to good yields in a highly regio- and stereoselective manner at room temperature under air atmosphere. The cytotoxic activity of these compounds was investigated in vitro against three different human cell lines (THP-1, K562, MCF-7).

Biocatalytic production of Ɛ-caprolactone using Geotrichum candidum cells immobilized on functionalized silica.

Immobilization of the Geotrichum candidum (CCT 1205) cell with functionalized silica creates promising biocatalysts for production of ɛ-caprolactone. The results obtained by immobilization of the whole cell on SiO-NH and SiO-SH supports indicate that the presence of reactive functional groups on the support may promote effective chemical bonds with the cell walls resulting the decreased dehydrogenases enzyme activity (5% yield in less than 2h) and consequently, increased Baeyer-Villiger monooxygenases enzyme activity with redacting of 25% of time reaction when is used SiO-NH as support and 50% through use of SiO-SH as support relative to free cells when cyclohexanone is used as a substrate. The catalysts SiO-NH-Geotrichum candidum and SiO-SH-Geotrichum candidum were recycling and reused in the ɛ-caprolactone synthesis from cyclohexanone, and the biocatalysts promoted a quantitative conversion up to the eighth reaction cycle.