منابع مشابه
Small Molecule Therapeutics PRIMA-1/APR-246 Displays High Antitumor Activity in Multiple Myeloma By Induction of p73 and Noxa
Targeting p53 by the small-molecule PRIMA-1/APR-246 has shown promising preclinical activity in various cancer types. However, the mechanism of PRIMA-1–induced apoptosis is not completely understood and its effect on multiple myeloma cells is unknown. In this study, we evaluated antitumor effect of PRIMA-1 alone or its combination with current antimyeloma agents in multiple myeloma cell lines, ...
متن کاملAPR-246/PRIMA-1(MET) rescues epidermal differentiation in skin keratinocytes derived from EEC syndrome patients with p63 mutations.
p53 and p63 share extensive sequence and structure homology. p53 is frequently mutated in cancer, whereas mutations in p63 cause developmental disorders manifested in ectodermal dysplasia, limb defects, and orofacial clefting. We have established primary adult skin keratinocytes from ectrodactyly, ectodermal dysplasia, and cleft lip/palate (EEC) syndrome patients with p63 mutations as an in vit...
متن کاملPRIMA-1met (APR-246) inhibits growth of colorectal cancer cells with different p53 status through distinct mechanisms
PRIMA-1met (APR-246) is a methylated derivative and structural analog of PRIMA-1 (p53 re-activation and induction of massive apoptosis). PRIMA-1met has been reported to restore both the wild type (wt) structure and function of mutant p53. Here, we show that PRIMA-1met is highly effective at limiting the growth of CRC cells regardless of p53 status. However, PRIMA-1met induces robust apoptosis o...
متن کاملPRIMA-1 and PRIMA-1Met (APR-246): From Mutant/Wild Type p53 Reactivation to Unexpected Mechanisms Underlying Their Potent Anti-Tumor Effect in Combinatorial Therapies
p53 protects cells from genetic assaults by triggering cell-cycle arrest and apoptosis. Inactivation of p53 pathway is found in the vast majority of human cancers often due to somatic missense mutations in TP53 or to an excessive degradation of the protein. Accordingly, reactivation of p53 appears as a quite promising pharmacological approach and, effectively, several attempts have been made in...
متن کاملPRIMA-1Met/APR-246 displays high antitumor activity in multiple myeloma by induction of p73 and Noxa.
Targeting p53 by the small-molecule PRIMA-1(Met)/APR-246 has shown promising preclinical activity in various cancer types. However, the mechanism of PRIMA-1(Met)-induced apoptosis is not completely understood and its effect on multiple myeloma cells is unknown. In this study, we evaluated antitumor effect of PRIMA-1(Met) alone or its combination with current antimyeloma agents in multiple myelo...
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ژورنال
عنوان ژورنال: Klinicka onkologie
سال: 2018
ISSN: 0862-495X,1802-5307
DOI: 10.14735/amko20182s71