The pharmaceutical company AI-Therapeutics (Guilford, CT, USA) has acquired the preclinical drug candidates EC-8042 and EC-70124 in the course of the insolvency proceedings EntreChem was experiencing since February of last year. The insolvency event left unfinished the development of both drugs, that were on the verge of facing the first... read more →
Apr
28
Jun
24
Rhabdoid tumor is a pediatric cancer characterized by the biallelic inactivation of SMARCB1, a subunit of the SWI/SNF chromatin remodeling complex. SMARCB1 inactivation leads to SWI/SNF redistribution to favor a proliferative dedifferentiated cellular state. Although this deletion is the known oncogenic driver, SWI/SNF therapeutic targeting remains a challenge. Mithralog... read more →
May
30
EntreChem, 2 European Universities and Novartis to cooperate in the project "MISSION: Streamlined Streptomyces cell factories for industrial production of valuable natural products." The European Commission has awarded €1.8M to the ERA-CoBiotech project "MISSION - Streamlined Streptomyces cell factories for industrial production of valuable natural products." The project belongs... read more →
Jan
17
Acute Myeloid Leukemia (AML) is the most common myeloid malignancy in adults, and Internal Tandem Duplication (ITD) or kinase domain mutation of FLT3 represent the most frequent genetic alteration, accounting for 30% of cases associated with poor disease outcome. On the other hand, PIM kinases play an important role... read more →
May
02
Sarcoma models derived from human mesenchymal stromal/stem cells (hMSCs) are used to understand better the initiation of sarcomagenesis, not amenable to analysis in patient samples or cell lines. This study shows that the signaling mediated by SP1 is altered in transformed hMSCs able to initiate sarcomas in vivo. The inhibition... read more →
Apr
04
The fusion protein EWS-FLI1 is a constitutively activated transcription factor responsible for the oncogenic phenotype of Ewing sarcoma (EWS). Mithramycin is a potent inhibitor of EWS-FLI1, but its toxicity makes it desirable to identify more potent and/or a less toxic analogs to inhibit EWS-FLI1 at clinically achievable concentrations. EntreChem's mithralog... read more →
Mar
10
Cancer stem cells (CSCs) contribute to disease progression and treatment failure in prostate cancer because of their intrinsic resistance to current therapies. The transcription factors NF-κB and STAT3 are frequently activated in advanced prostate cancer and sustain expansion of prostate CSCs. EC-70124, is a potent dual inhibitor of the NF-kB... read more →
Dec
21
Activated kinases were identified by using phosphokinase arrays with human colorectal tumor samples, including the Epidermal Growth Factor Receptor (EGFR), components of the PI3K/mTOR pathway (AKT and S6), and SRC, among others. EC-7012, a kinase inhibitor, shows high in vitro antiproliferative activity as well as cell migration inhibition. Major effects... read more →
Oct
20
EC-70124, a kinase inhibitor, shows in vitro and in vivo antiproliferative effects mediated by simultaneous inhibition of the PI3K/mTOR y JAK/STAT signaling pathways and also DNA damage induction, causing cell cycle arrest on G2/M. The combination with docetaxel is synergistic, both in vitro and in vivo, offering opportunities for combination... read more →
May
11
EntreChem and three Universities from three European countries to cooperate in the project. The European Commission has awarded €1 million to the ERA-IB project "NeBrasCa - Next Generation Immunosuppressants: Brasilicardin synthesized by Nocardia spp." The project belongs to the European Research Agency - Industrial Biotechnology program (ERA-IB), and it aims... read more →