Inhibition of Akt and other AGC kinases: A target for clinical cancer therapy?
Sign Up to like & getrecommendations! Published in 2018 at "Seminars in cancer biology"
DOI: 10.1016/j.semcancer.2017.04.011
Abstract: AGC kinases have been identified to contribute to cancer development and progression. Currently, most AGC inhibitors in clinical development are Akt inhibitors such as MK-2206 or GDC-0068, which are known to promote cell growth arrest… read more here.
Keywords: inhibition akt; agc kinases; akt inhibitors; clinical development ... See more keywords
Chemical Phosphoproteomics Sheds New Light on the Targets and Modes of Action of AKT Inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "ACS chemical biology"
DOI: 10.1021/acschembio.0c00872
Abstract: Due to its important roles in oncogenic signaling, AKT has been subjected to extensive drug discovery efforts leading to small molecule inhibitors investigated in advanced clinical trials. To better understand how these drugs exert their… read more here.
Keywords: sheds new; akt; chemical phosphoproteomics; akt inhibitors ... See more keywords
A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity
Sign Up to like & getrecommendations! Published in 2020 at "British Journal of Cancer"
DOI: 10.1038/s41416-020-0889-4
Abstract: Background AKT, a critical effector of the phosphoinositide 3-kinase (PI3K) signalling cascade, is an intensely pursued therapeutic target in oncology. Two distinct classes of AKT inhibitors have been in clinical development, ATP-competitive and allosteric. Class-specific… read more here.
Keywords: akt; akt inhibitors; drug; class specific ... See more keywords
Distinct resistance mechanisms arise to allosteric vs. ATP-competitive AKT inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Nature communications"
DOI: 10.1038/s41467-022-29655-0
Abstract: The AKT kinases have emerged as promising therapeutic targets in oncology and both allosteric and ATP-competitive AKT inhibitors have entered clinical investigation. However, long-term efficacy of such inhibitors will likely be challenged by the development… read more here.
Keywords: allosteric atp; resistance; atp competitive; akt inhibitors ... See more keywords
Targeting AKT for cancer therapy
Sign Up to like & getrecommendations! Published in 2019 at "Expert Opinion on Investigational Drugs"
DOI: 10.1080/13543784.2019.1676726
Abstract: ABSTRACT Introduction: Targeted therapies in cancer aim to inhibit specific molecular targets responsible for enhanced tumor growth. AKT/PKB (protein kinase B) is a serine threonine kinase involved in several critical cellular pathways, including survival, proliferation,… read more here.
Keywords: akt inhibitors; akt cancer; cancer; cancer therapy ... See more keywords
Histone Deacetylase Inhibitors with or without AKT Inhibition Potentially Increase the Efficacy of Daratumumab in Multiple Myeloma By Enhancing the Antibody-Dependent Cell-Mediated and Complement-Dependent Cytotoxicity As Well As Apoptosis
Sign Up to like & getrecommendations! Published in 2018 at "Blood"
DOI: 10.1182/blood-2018-99-110709
Abstract: Multiple myeloma (MM) is one of the many types of hematological malignancies, and many novel drugs, including histone deacetylase (HDAC) inhibitors such as panobinostat (pan-HDAC), romidepsin (HDAC1-3-specific), ACY-1215 and ACY-241 (HDAC6-specific) are currently undergoing preclinical… read more here.
Keywords: akt inhibitors; antibody; hdac inhibitors; expression ... See more keywords
Allosteric AKT Inhibitors Target Synthetic Lethal Vulnerabilities in E-Cadherin-Deficient Cells
Sign Up to like & getrecommendations! Published in 2019 at "Cancers"
DOI: 10.3390/cancers11091359
Abstract: The CDH1 gene, encoding the cell adhesion protein E-cadherin, is one of the most frequently mutated genes in gastric cancer and inactivating germline CDH1 mutations are responsible for hereditary diffuse gastric cancer syndrome (HDGC). Using… read more here.
Keywords: cadherin deficient; akt inhibitors; gastric cancer; target synthetic ... See more keywords