Search Results - "Ha, Jae Du"
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Induced protein degradation of anaplastic lymphoma kinase (ALK) by proteolysis targeting chimera (PROTAC)
Published in Biochemical and biophysical research communications (28-10-2018)“…Recently, proteolysis targeting chimera (PROTAC) technology is highlighted in drug discovery area as a new therapeutic approach. PROTAC as a heterobifunctional…”
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2
Design and characterization of cereblon-mediated androgen receptor proteolysis-targeting chimeras
Published in European journal of medicinal chemistry (15-12-2020)“…Proteolysis-targeting chimera (PROTAC)-mediated protein degradation is a rapidly emerging therapeutic intervention that induces the degradation of targeted…”
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3
Combination Treatment with GSK126 and Pomalidomide Induces B-Cell Differentiation in EZH2 Gain-of-Function Mutant Diffuse Large B-Cell Lymphoma
Published in Cancers (07-09-2020)“…Enhancer of zeste 2 polycomb repressive complex 2 subunit (EZH2), the catalytic subunit of polycomb repressive complex 2 (PRC2), regulates genes involved in…”
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4
Synthesis and biological evaluation of rhodanine derivatives as PRL-3 inhibitors
Published in Bioorganic & medicinal chemistry letters (01-06-2006)“…A series of rhodanine derivatives was synthesized and evaluated for their ability to inhibit PRL-3. Benzylidene rhodanine derivative showed good biological…”
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5
Augmentation of the antitumor effects of PARP inhibitors in triple-negative breast cancer via degradation by hydrophobic tagging modulation
Published in European journal of medicinal chemistry (15-10-2020)“…Triple-negative breast cancer (TNBC) has an aggressive phenotype and poor prognosis due to the lack of specific targeted treatments. The development of an…”
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6
Synthesis and structure–activity relationship of aminopyridines with substituted benzoxazoles as c-Met kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-06-2012)“…A series of hydroxybenzoxazole derivatives was synthesized, and their c-Met kinase inhibitory activity was evaluated. Described herein is a potent c-Met…”
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7
Cereblon contributes to cardiac dysfunction by degrading Cav1.2α
Published in European heart journal (21-05-2022)“…Cereblon (CRBN) is a substrate receptor of the E3 ubiquitin ligase complex that was reported to target ion channel proteins. L-type voltage-dependent Ca2+…”
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Design and Synthesis of Novel 3-(2-Aminopyridin-3-yl)-1,2,4-Triazolo [4,3-b]Pyridazine Derivatives as a Reversible Bruton's Tyrosine Kinase Inhibitors
Published in Bulletin of the Korean Chemical Society (2018)“…Bruton's tyrosine kinase, a non-receptor TEC family kinase, plays key role in B cell differentiation, proliferation, and survival. B cell receptor regulates…”
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9
A Novel Series of Highly Potent Small Molecule Inhibitors of Rhinovirus Replication
Published in Journal of medicinal chemistry (13-07-2017)“…Human rhinoviruses (hRVs) are the main causative pathogen for common colds and are associated with the exacerbation of asthma. The wide variety in hRV…”
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10
Discovery of aminopyridines substituted with benzoxazole as orally active c-Met kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (15-07-2010)“…A series of aminopyridines substituted with benzoxazole were designed and synthesized as very potent c-Met kinase inhibitors. We report the synthesis and…”
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11
Disordered region of cereblon is required for efficient degradation by proteolysis-targeting chimera
Published in Scientific reports (23-12-2019)“…Proteolysis targeting chimeras (PROTACs) are an emerging strategy for promoting targeted protein degradation by inducing the proximity between targeted…”
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12
Design and synthesis of triazolopyridazines substituted with methylisoquinolinone as selective c-Met kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-12-2011)“…A series of triazolopyridazines substituted with methylisoquinolinone were designed and synthesized. Some of the triazolopyridazines strongly inhibited c-Met…”
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13
Synthesis and biological evaluation of N9-cis-cyclobutylpurine derivatives for use as cyclin-dependent kinase (CDK) inhibitors
Published in Bioorganic & medicinal chemistry letters (15-09-2017)“…[Display omitted] A novel 6-aminopurine scaffold bearing an N9-cis-cyclobutyl moiety was designed using structure-based molecular design based on two known CDK…”
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14
cIAPs promote the proteasomal degradation of mutant SOD1 linked to familial amyotrophic lateral sclerosis
Published in Biochemical and biophysical research communications (18-11-2016)“…Although the ubiquitin–proteasome system is believed to play an important role in the pathogenesis of familial amyotrophic lateral sclerosis (FALS), caused by…”
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Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor
Published in Bioorganic & medicinal chemistry letters (15-09-2015)“…[Display omitted] A series of novel 2,4-diaminopyrimidine compounds bearing bicyclic aminobenzazepine were synthesized and evaluated for their anti-ALK…”
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Replacing the terminal piperidine in ceritinib with aliphatic amines confers activities against crizotinib-resistant mutants including G1202R
Published in European journal of medicinal chemistry (27-01-2017)“…The piperidine fragment in ceritinib was replaced with diverse aliphatic amines to improve inherent resistance issues of ceritinib. While most of the prepared…”
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4-Substituted quinazoline derivatives as novel EphA2 receptor tyrosine kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-09-2014)“…Erythropoietin-producing hepatocellular receptor tyrosine kinase subtype A2 (EphA2) is an attractive therapeutic target for suppressing tumor progression. In…”
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18
Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-12-2013)“…G-protein-coupled receptor kinase (GRK)-2 and -5 are emerging therapeutic targets for the treatment of cardiovascular disease. In our efforts to discover novel…”
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Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment
Published in Bioorganic & medicinal chemistry letters (15-11-2013)“…The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines is described and their structure–activity-relationship to anaplastic…”
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20
Synthesis and characterization of novel polyimides with 1-octadecyl side chains for liquid crystal alignment layers
Published in Polymers for advanced technologies (01-03-2007)“…A series of poly(amic acid)s have been synthesized from cyclobutane‐1,2,3,4‐tetracarboxylic dianhydride (CBDA), a functional diamine,…”
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