Introduction
An Overview of DAPK
Death-associated protein kinase (DAPK) is the member of a family of calmodulin (CaM) -regulated serine/threonine kinases that functions as a positive mediator of apoptosis. Apoptosis is one of the most effective methods for tumor therapeutics. It is closely related to the initiation, progression and metastasis of tumors. DAPK is a tumor suppressor involved in diverse apoptosis pathways, and it is involved in apoptosis induced by multiple pathways and is considered to be a tumor suppressor gene. Besides, DAPK can regulate or execute cell death through a variety of stimuli, including activation of death receptors, activation of cytokines, matrix desorption, and neuromycination.
The Major Types of DAPK
The DAPK family has five members: DAPK, DRP1/DAPK2 (dynamin-related protein 1 /death-associated protein kinase 2), DLK/ZIPK (DAP-like kinase /zipper interacting protein kinase), DRAK1 and DRAK2 (Death-associated protein kinase related apoptosis-inducing protein kinase 1 /Death-associated protein kinase related apoptosis-inducing protein kinase 2).
The Inhibition of DAPK
Aberrant methylation of DNA is an early event of tumorigenesis, so clinical diagnosis and treatment will benefit from methylation detection. Drugs including 5-azacytidine and 5-azido-2-deoxycytidine have been approved for clinical use. 5-azacytidine is unstable and cannot be used orally, so clinical applications are limited. 1-(β-ribonitrosourea)-1, 2-Dihydroquinidine is a new demethylation drug, which is chemically stable and has been shown to significantly reduce bladder cancer tumor volume. TC-DAPK 6 is a potent ATP-competitive selective DAPK inhibitor that acts on DAPK1 and DAPK3.
Death-associated protein kinase (DAPK) is the member of a family of calmodulin (CaM) -regulated serine/threonine kinases that functions as a positive mediator of apoptosis. Apoptosis is one of the most effective methods for tumor therapeutics. It is closely related to the initiation, progression and metastasis of tumors. DAPK is a tumor suppressor involved in diverse apoptosis pathways, and it is involved in apoptosis induced by multiple pathways and is considered to be a tumor suppressor gene. Besides, DAPK can regulate or execute cell death through a variety of stimuli, including activation of death receptors, activation of cytokines, matrix desorption, and neuromycination.
The Major Types of DAPK
The DAPK family has five members: DAPK, DRP1/DAPK2 (dynamin-related protein 1 /death-associated protein kinase 2), DLK/ZIPK (DAP-like kinase /zipper interacting protein kinase), DRAK1 and DRAK2 (Death-associated protein kinase related apoptosis-inducing protein kinase 1 /Death-associated protein kinase related apoptosis-inducing protein kinase 2).
The Inhibition of DAPK
Aberrant methylation of DNA is an early event of tumorigenesis, so clinical diagnosis and treatment will benefit from methylation detection. Drugs including 5-azacytidine and 5-azido-2-deoxycytidine have been approved for clinical use. 5-azacytidine is unstable and cannot be used orally, so clinical applications are limited. 1-(β-ribonitrosourea)-1, 2-Dihydroquinidine is a new demethylation drug, which is chemically stable and has been shown to significantly reduce bladder cancer tumor volume. TC-DAPK 6 is a potent ATP-competitive selective DAPK inhibitor that acts on DAPK1 and DAPK3.
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