Search Results - "LAM, Lloyd T"
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Potential mechanisms of resistance to venetoclax and strategies to circumvent it
Published in BMC cancer (02-06-2017)“…Venetoclax (ABT-199), a first-in-class orally bioavailable BCL-2-selective inhibitor, was recently approved by the FDA for use in patients with 17p-deleted…”
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Targeting Lineage-specific MITF Pathway in Human Melanoma Cell Lines by A-485, the Selective Small-molecule Inhibitor of p300/CBP
Published in Molecular cancer therapeutics (01-12-2018)“…Metastatic melanoma is responsible for approximately 80% of deaths from skin cancer. Microphthalmia-associated transcription factor (MITF) is a…”
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3
A loss-of-function RNA interference screen for molecular targets in cancer
Published in Nature (04-05-2006)“…The pursuit of novel therapeutic agents in cancer relies on the identification and validation of molecular targets. Hallmarks of cancer include…”
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Identification of novel resistance mechanisms to NAMPT inhibition via the de novo NAD+ biosynthesis pathway and NAMPT mutation
Published in Biochemical and biophysical research communications (23-09-2017)“…Cancer cells have an unusually high requirement for the central and intermediary metabolite nicotinamide adenine dinucleotide (NAD+), and NAD+ depletion…”
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Small Molecule Inhibitors of IκB Kinase Are Selectively Toxic for Subgroups of Diffuse Large B-Cell Lymphoma Defined by Gene Expression Profiling
Published in Clinical cancer research (01-01-2005)“…Constitutive activation of the NF-κB pathway is required for survival of the activated B cell–like (ABC) subgroup of diffuse large B-cell lymphoma (DLBCL)…”
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A mechanistic rationale for MEK inhibitor therapy in myeloma based on blockade of MAF oncogene expression
Published in Blood (24-02-2011)“…Modulating aberrant transcription of oncogenes is a relatively unexplored opportunity in cancer therapeutics. In approximately 10% of multiple myelomas, the…”
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A microRNA screen to identify modulators of sensitivity to BCL2 inhibitor ABT-263 (navitoclax)
Published in Molecular cancer therapeutics (01-11-2010)“…Evasion of apoptosis is a known feature of cancer cells. One mechanism of deregulating the apoptotic pathway is through overexpression of antiapoptotic BCL2…”
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Compensatory IKKα activation of classical NF-κB signaling during IKKβ inhibition identified by an RNA interference sensitization screen
Published in Proceedings of the National Academy of Sciences - PNAS (30-12-2008)“…A subtype of diffuse large B-cell lymphoma (DLBCL), termed activated B-cell-like (ABC) DLBCL, depends on constitutive nuclear factor-κB (NF-κB) signaling for…”
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A library of gene expression signatures to illuminate normal and pathological lymphoid biology
Published in Immunological reviews (01-04-2006)“…Genomics has provided a lever to pry open lymphoid cells and examine their regulatory biology. The large body of available gene expression data has also…”
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Selective MCL-1 inhibitor ABBV-467 is efficacious in tumor models but is associated with cardiac troponin increases in patients
Published in Communications medicine (25-10-2023)“…Background MCL-1 is a prosurvival B-cell lymphoma 2 family protein that plays a critical role in tumor maintenance and survival and can act as a resistance…”
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Genomic-scale measurement of mRNA turnover and the mechanisms of action of the anti-cancer drug flavopiridol
Published in Genome biology (13-09-2001)“…Flavopiridol, a flavonoid currently in cancer clinical trials, inhibits cyclin-dependent kinases (CDKs) by competitively blocking their ATP-binding pocket…”
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Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours
Published in Nature (London) (05-10-2017)“…A potent and selective catalytic inhibitor of p300/CBP histone acetyltransferases suppresses tumour proliferation across multiple cell lineages, illustrating…”
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MYC Family Amplification Dictates Sensitivity to BET Bromodomain Protein Inhibitor Mivebresib (ABBV075) in Small-Cell Lung Cancer
Published in Molecular cancer research (02-08-2024)“…Small-cell lung cancer (SCLC) accounts for nearly 15% of all lung cancers. Although patients respond to first-line therapy readily, rapid relapse is…”
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Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies
Published in Cancer research (Chicago, Ill.) (01-06-2017)“…ABBV-075 is a potent and selective BET family bromodomain inhibitor that recently entered phase I clinical trials. Comprehensive preclinical characterization…”
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Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors
Published in Molecular cancer therapeutics (01-08-2017)“…Ten percent to 15% of all lung cancers are small-cell lung cancer (SCLC). SCLC usually grows and metastasizes before it is diagnosed and relapses rapidly upon…”
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Statins enhance efficacy of venetoclax in blood cancers
Published in Science translational medicine (13-06-2018)“…Statins have shown promise as anticancer agents in experimental and epidemiologic research. However, any benefit that they provide is likely context-dependent,…”
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Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia
Published in Molecular cancer therapeutics (01-10-2021)“…Dual bromodomain BET inhibitors that bind with similar affinities to the first and second bromodomains across BRD2, BRD3, BRD4, and BRDT have displayed modest…”
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Molecular subtypes of diffuse large B-cell lymphoma arise by distinct genetic pathways
Published in Proceedings of the National Academy of Sciences - PNAS (09-09-2008)“…Gene-expression profiling has been used to define 3 molecular subtypes of diffuse large B-cell lymphoma (DLBCL), termed germinal center B-cell-like (GCB)…”
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Genomic analysis and selective small molecule inhibition identifies BCL-XL as a critical survival factor in a subset of colorectal cancer
Published in Molecular cancer (02-07-2015)“…Background Defects in programmed cell death, or apoptosis, are a hallmark of cancer. The anti-apoptotic B-cell lymphoma 2 (BCL-2) family proteins, including…”
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Design, Synthesis, and Biological Investigation of Thailanstatin A and Spliceostatin D Analogues Containing Tetrahydropyran, Tetrahydrooxazine, and Fluorinated Structural Motifs
Published in Journal of organic chemistry (05-02-2021)“…Thailanstatin A and spliceostatin D, two naturally occurring molecules endowed with potent antitumor activities by virtue of their ability to bind and inhibit…”
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