Discovery of an Allosteric, Inactive Conformation-Selective Inhibitor of Full-Length HPK1 Utilizing a Kinase Cascade Assay.
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DOI: 10.1021/acs.biochem.1c00486
Abstract: Achieving selectivity across the human kinome is a major hurdle in kinase inhibitor drug discovery. Assays using active, phosphorylated protein kinases bias hits toward poorly selective inhibitors that bind within the highly conserved adenosine triphosphate… read more here.
Keywords: inhibitor; kinase; discovery; cascade assay ... See more keywords
The HPK1 Inhibitor A-745 Verifies the Potential of Modulating T Cell Kinase Signaling for Immunotherapy.
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DOI: 10.1021/acschembio.1c00819
Abstract: Hematopoietic progenitor kinase 1 (HPK1) is an MAP4K family member within the Ste20-like serine/threonine branch of the kinome. HPK1 expression is limited to hematopoietic cells and has a predominant role as a negative regulator of… read more here.
Keywords: hpk1 inhibitor; cell; 745 verifies; inhibitor 745 ... See more keywords
Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.1c00473
Abstract: Hematopoietic progenitor kinase 1 (HPK1) is implicated as a negative regulator of T-cell receptor-induced T-cell activation. Studies using HPK1 kinase-dead knock-in animals have demonstrated the loss of HPK1 kinase activity resulted in an increase in… read more here.
Keywords: spiro azaindoline; progenitor kinase; hpk1; kinase ... See more keywords
Abstract 463: GRC 54276, a novel small molecule inhibitor of HPK1 has entered phase 1/2 clinical trial insolid malignancies and Hodgkin’s/non Hodgkin’s lymphoma
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DOI: 10.1158/1538-7445.am2023-463
Abstract: Background: Pre-clinical profile of GRC 54276, a clinical candidate with Phase 1/2 clinical trial ongoing, is presented here. GRC 54276 is a novel small molecule inhibitor of Hematopoietic progenitor kinase 1 (HPK1), a serine/threonine kinase1,2… read more here.
Keywords: 54276 novel; grc; hpk1; clinical trial ... See more keywords
Abstract 5014: HPK1 gene knockout reporter cell line: an efficient drug screening system
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DOI: 10.1158/1538-7445.am2023-5014
Abstract: Immunotherapy is the stimulation of the immune system, improving on the ability of immune system to treat cancer. It is expected to be the most effective therapy for patients with tumor metastasis. Checkpoint inhibitor (CPI)… read more here.
Keywords: system; cell; reporter; cell line ... See more keywords
Abstract LB324: BB3008, a potent and selective small molecular HPK1 inhibitor effective in multiple syngeneic tumor models
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-lb324
Abstract: Introduction: Hematopoietic progenitor kinase 1 (HPK1) is a serine/threonine kinase in the MAP4K family predominantly expressed in immune cells, and has been identified as a negative regulator of T cell and B cell receptor signaling… read more here.
Keywords: hpk1 inhibitor; cell; tumor models; bb3008 ... See more keywords