Search Results - "Griffin, James D"
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A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader
Published in Cell chemical biology (18-01-2018)“…Heterobifunctional molecules that recruit E3 ubiquitin ligases, such as cereblon, for targeted protein degradation represent an emerging pharmacological…”
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Inhibition of USP10 induces degradation of oncogenic FLT3
Published in Nature chemical biology (01-12-2017)“…An inhibitor of the deubiquitinase (DUB) USP10 regulates the degradation of oncogenic FLT3, thus defining USP10 as a DUB for FLT3 and providing a therapeutic…”
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The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors
Published in Blood (24-03-2011)“…The transcription factor STAT5 is an essential mediator of the pathogenesis of chronic myelogenous leukemia (CML). In CML, the BCR/ABL fusion kinase causes the…”
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Nilotinib in Imatinib-Resistant CML and Philadelphia Chromosome–Positive ALL
Published in The New England journal of medicine (15-06-2006)“…This phase 1 study treated 119 patients with imatinib-resistant chronic myelogenous leukemia (CML) with nilotinib, an inhibitor of BCR-ABL tyrosine kinase. The…”
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The roles of FLT3 in hematopoiesis and leukemia
Published in Blood (01-09-2002)“…FLT3 is a receptor tyrosine kinase expressed by immature hematopoietic cells and is important for the normal development of stem cells and the immune system…”
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Anti‐SARS‐CoV‐2 activity of targeted kinase inhibitors: Repurposing clinically available drugs for COVID‐19 therapy
Published in Journal of medical virology (01-01-2023)“…Coronavirus disease 2019 (COVID‐19) remains a major public health concern, and vaccine unavailability, hesitancy, or failure underscore the need for discovery…”
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Functional screening identifies CRLF2 in precursor B-cell acute lymphoblastic leukemia
Published in Proceedings of the National Academy of Sciences - PNAS (05-01-2010)“…The prognosis for adults with precursor B-cell acute lymphoblastic leukemia (B-ALL) remains poor, in part from a lack of therapeutic targets. We identified the…”
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Chimeric Antigen Receptor T Cell Therapy in Acute Myeloid Leukemia: Trials and Tribulations
Published in Hematology reports (01-12-2023)“…Acute myeloid leukemia (AML) is a heterogeneous hematological malignancy that is often associated with relapse and drug resistance after standard chemotherapy…”
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Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor
Published in ACS chemical biology (18-10-2013)“…The DDR1 receptor tyrosine kinase is activated by matrix collagens and has been implicated in numerous cellular functions such as proliferation,…”
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10
Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl
Published in Cancer cell (01-02-2005)“…The Bcr-Abl tyrosine kinase oncogene causes chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL)…”
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Inhibition of Wild-Type p53-Expressing AML by the Novel Small Molecule HDM2 Inhibitor CGM097
Published in Molecular cancer therapeutics (01-10-2015)“…The tumor suppressor p53 is a key regulator of apoptosis and functions upstream in the apoptotic cascade by both indirectly and directly regulating Bcl-2…”
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BRD9 degraders as chemosensitizers in acute leukemia and multiple myeloma
Published in Blood cancer journal (New York) (19-07-2022)“…Bromodomain-containing protein 9 (BRD9), an essential component of the SWI/SNF chromatin remodeling complex termed ncBAF, has been established as a therapeutic…”
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Repurposing clinically available drugs and therapies for pathogenic targets to combat SARS‐CoV‐2
Published in MedComm (2020) (01-06-2023)“…The coronavirus disease 2019 (COVID‐19) pandemic has affected a large portion of the global population, both physically and mentally. Current evidence suggests…”
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Gene expression profiling analysis of CRTC1-MAML2 fusion oncogene-induced transcriptional program in human mucoepidermoid carcinoma cells
Published in BMC cancer (26-10-2015)“…Mucoepidermoid carcinoma (MEC) arises from multiple organs and accounts for the most common types of salivary gland malignancies. Currently, patients with…”
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Reversible resistance induced by FLT3 inhibition: a novel resistance mechanism in mutant FLT3-expressing cells
Published in PloS one (28-09-2011)“…Clinical responses achieved with FLT3 kinase inhibitors in acute myeloid leukemia (AML) are typically transient and partial. Thus, there is a need for…”
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Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 (nilotinib) by a random mutagenesis study
Published in Blood (01-06-2007)“…Patients with advanced stages of chronic myeloid leukemia (CML) often manifest imatinib mesylate resistance associated with point mutations in BCR-ABL. AMN107…”
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The CRTC1-MAML2 fusion is the major oncogenic driver in mucoepidermoid carcinoma
Published in JCI insight (08-04-2021)“…No effective systemic treatment is available for patients with unresectable, recurrent, or metastatic mucoepidermoid carcinoma (MEC), the most common salivary…”
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Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412
Published in Cancer cell (01-06-2002)“…Constitutively activating FLT3 receptor mutations have been found in 35% of patients with acute myeloblastic leukemia (AML). Here we report the identification…”
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FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML
Published in Drug resistance updates (01-06-2009)“…Abstract An appealing therapeutic target in AML is constitutively activated, mutant FLT3, which is expressed in a subpopulation of AML patients and is…”
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Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412
Published in Blood (15-07-2005)“…Constitutively activated forms of the transmembrane receptor tyrosine kinase c-KIT have been associated with systemic mast cell disease, acute myeloid…”
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