CBP/p300 bromodomain: new promising epigenetic target
نویسندگان
چکیده
CREB (cAMP responsive element binding protein) protein (CBP) and adenovirus E1A-associated 300 kDa (p300) are histone acetyltransferases, which necessary for multiple cellular processes. Thus, CBP/p300 promising potential antitumor targets. To date, despite various small molecule inhibitors of bromodomain (BRD) having been reported, no specific inhibitor was approved by U.S. Food Drug Administration (FDA). In this review, we described the discovery, optimization, mode evaluation, selectivity potency therapeutic opportunities our inhibitors, aiming to inspire new design advance drug discovery research in field. One video presents development inhibitors.
منابع مشابه
The KDM1A histone demethylase is a promising new target for the epigenetic therapy of medulloblastoma
BACKGROUND Medulloblastoma is a leading cause of childhood cancer-related deaths. Current aggressive treatments frequently lead to cognitive and neurological disabilities in survivors. Novel targeted therapies are required to improve outcome in high-risk medulloblastoma patients and quality of life of survivors. Targeting enzymes controlling epigenetic alterations is a promising approach recent...
متن کاملEpigenetic changes in pediatric solid tumors: promising new targets.
Cancer is being reinterpreted in the light of recent discoveries related to the histone code and the dynamic nature of epigenetic regulation and control of gene programs during development, as well as insights gained from whole cancer genome sequencing. Somatic mutations in or deregulated expression of genes that encode chromatin-modifying enzymes are being identified with high frequency. Nowhe...
متن کاملApelin: A promising therapeutic target? (Part 1)
Apelin is a recently discovered bioactive peptide, known to be an endogenous high-affinity ligandfor the previously orphan G protein-coupled receptor APJ. Apelin/APJ as a novel signaling pathwayhas been shown to play many crucial roles in cardiovascular function, blood pressure regulation, fluidhomeostasis, feeding behavior, obesity, type 2 diabetes mellitus, adipoinsular axis regulation, cellp...
متن کاملTubulin/microtubules: still a promising target for new chemotherapeutic agents.
Most investigators would agree that the ideal chemotherapeutic agent should be 1) directed at a validated target; 2) potent, preferably active at nanomolar or subnanomolar concentrations; 3) schedule independent, even active in noncycling cells; 4) active against drug-resistant cells; and 5) less toxic or ideally not toxic to normal cells. In this issue of the Journal, Leoni et al. (1) suggest ...
متن کاملEpigenetic mechanisms in migraine: a promising avenue?
Migraine is a disabling common brain disorder typically characterized by attacks of severe headache and associated with autonomic and neurological symptoms. Its etiology is far from resolved. This review will focus on evidence that epigenetic mechanisms play an important role in disease etiology. Epigenetics comprise both DNA methylation and post-translational modifications of the tails of hist...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Visualized cancer medicine
سال: 2022
ISSN: ['2740-4218']
DOI: https://doi.org/10.1051/vcm/2022004