Abigail E. Case
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View article: BRD9 degraders as chemosensitizers in acute leukemia and multiple myeloma
BRD9 degraders as chemosensitizers in acute leukemia and multiple myeloma Open
Bromodomain-containing protein 9 (BRD9), an essential component of the SWI/SNF chromatin remodeling complex termed ncBAF, has been established as a therapeutic target in a subset of sarcomas and leukemias. Here, we used novel small molecul…
View article: The Role of Real‐World Evidence in FDA‐Approved New Drug and Biologics License Applications
The Role of Real‐World Evidence in FDA‐Approved New Drug and Biologics License Applications Open
The US Food and Drug Administration (FDA) is open to accepting real‐world evidence (RWE) to support its assessment of medical products. However, RWE stakeholders lack a shared understanding of FDA’s evidentiary expectations for the use of …
View article: Essential role of the histone lysine demethylase KDM4A in the biology of malignant pleural mesothelioma (MPM)
Essential role of the histone lysine demethylase KDM4A in the biology of malignant pleural mesothelioma (MPM) Open
Background Malignant pleural mesothelioma (MPM) is a highly aggressive cancer with a dismal prognosis. There is increasing interest in targeting chromatin regulatory pathways in difficult-to-treat cancers. In preliminary studies, we found …
View article: Inhibitors of the Transcription Factor STAT3 Decrease Growth and Induce Immune Response Genes in Models of Malignant Pleural Mesothelioma (MPM)
Inhibitors of the Transcription Factor STAT3 Decrease Growth and Induce Immune Response Genes in Models of Malignant Pleural Mesothelioma (MPM) Open
Malignant pleural mesothelioma (MPM) is an aggressive cancer defined by loss-of-function mutations with few therapeutic options. We examined the contribution of the transcription factor Signal transducer and activator of transcription 3 (S…
View article: Inhibition of the deubiquitinase USP10 induces degradation of SYK
Inhibition of the deubiquitinase USP10 induces degradation of SYK Open
Background There is growing evidence that spleen tyrosine kinase (SYK) is critical for acute myeloid leukaemia (AML) transformation and maintenance of the leukemic clone in AML patients. It has also been found to be over-expressed in AML p…
View article: Effects of the multi‐kinase inhibitor midostaurin in combination with chemotherapy in models of acute myeloid leukaemia
Effects of the multi‐kinase inhibitor midostaurin in combination with chemotherapy in models of acute myeloid leukaemia Open
Recently, several targeted agents have been developed for specific subsets of patients with acute myeloid leukaemia (AML), including midostaurin, the first FDA‐approved FLT3 inhibitor for newly diagnosed patients with FLT3 mutations. Howev…
View article: The combination of FLT3 and SYK kinase inhibitors is toxic to leukaemia cells with CBL mutations
The combination of FLT3 and SYK kinase inhibitors is toxic to leukaemia cells with CBL mutations Open
Mutations in the E3 ubiquitin ligase CBL, found in several myeloid neoplasms, lead to decreased ubiquitin ligase activity. In murine systems, these mutations are associated with cytokine‐independent proliferation, thought to result from th…
View article: Comparison of effects of midostaurin, crenolanib, quizartinib, gilteritinib, sorafenib and BLU‐285 on oncogenic mutants of KIT, CBL and FLT3 in haematological malignancies
Comparison of effects of midostaurin, crenolanib, quizartinib, gilteritinib, sorafenib and BLU‐285 on oncogenic mutants of KIT, CBL and FLT3 in haematological malignancies Open
Summary Mutations in two type‐3 receptor tyrosine kinases (RTKs), KIT and FLT3, are common in both acute myeloid leukaemia (AML) and systemic mastocytosis (SM) and lead to hyperactivation of key signalling pathways. A large number of tyros…
View article: Expression of the eight GABAA receptor α subunits in the developing zebrafish central nervous system
Expression of the eight GABAA receptor α subunits in the developing zebrafish central nervous system Open
GABA is a robust regulator of both developing and mature neural networks. It exerts many of its effects through GABAA receptors, which are heteropentamers assembled from a large array of subunits encoded by distinct genes. In mammals, ther…
View article: Expression of the Eight GABA<sub>A</sub> Receptor α Subunits in the Developing Zebrafish Central Nervous System
Expression of the Eight GABA<sub>A</sub> Receptor α Subunits in the Developing Zebrafish Central Nervous System Open
GABA is a robust regulator of both developing and mature neural networks. It exerts many of its effects through GABA A receptors, which are heteropentamers assembled from a large array of subunits encoded by distinct genes. In mammals, the…