Osamu Kurasawa
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View article: A CDC7 inhibitor sensitizes DNA-damaging chemotherapies by suppressing homologous recombination repair to delay DNA damage recovery
A CDC7 inhibitor sensitizes DNA-damaging chemotherapies by suppressing homologous recombination repair to delay DNA damage recovery Open
Potential combination partners of a CDC7 inhibitor TAK-931 were identified to guide its clinical development strategy.
View article: CCDC 2009266: Experimental Crystal Structure Determination
CCDC 2009266: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2009267: Experimental Crystal Structure Determination
CCDC 2009267: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: New Series of Potent Allosteric Inhibitors of Deoxyhypusine Synthase
New Series of Potent Allosteric Inhibitors of Deoxyhypusine Synthase Open
Deoxyhypusine synthase (DHPS) is the primary enzyme responsible for the hypusine modification and, thereby, activation of the eukaryotic translation initiation factor 5A (eIF5A), which is key in regulating the protein translation processes…
View article: Discovery of NovelAllosteric Inhibitors of DeoxyhypusineSynthase
Discovery of NovelAllosteric Inhibitors of DeoxyhypusineSynthase Open
Deoxyhypusine\nsynthase (DHPS) utilizes spermidine and NAD as cofactors\nto incorporate a hypusine modification into the eukaryotic translation\ninitiation factor 5A (eIF5A). Hypusine is essential for eIF5A activation,\nwhich, in turn, pla…
View article: Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase
Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase Open
Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor 5A (eIF5A). Hypusine is essential for eIF5A activation, which, in turn, plays a…
View article: CCDC 1918342: Experimental Crystal Structure Determination
CCDC 1918342: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1918343: Experimental Crystal Structure Determination
CCDC 1918343: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1918344: Experimental Crystal Structure Determination
CCDC 1918344: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-<i>d</i>]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-<i>d</i>]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent Open
In our pursuit of developing a novel, potent, and selective cell division cycle 7 (Cdc7) inhibitor, we optimized the previously reported thieno[3,2-d]pyrimidinone analogue I showing time-dependent Cdc7 kinase inhibition and s…
View article: Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode
Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode Open
General control nonderepressible 2 (GCN2) is a master regulator kinase of amino acid homeostasis and important for cancer survival in the tumor microenvironment under amino acid depletion. We initiated studies aiming at the discovery of no…
View article: Molecular mechanism and potential target indication of TAK-931, a novel CDC7-selective inhibitor
Molecular mechanism and potential target indication of TAK-931, a novel CDC7-selective inhibitor Open
A next generation cancer drug candidate, a CDC7 inhibitor, TAK-931, was developed, which is being evaluated in clinical trials.
View article: Inhibition of GCN2 sensitizes ASNS-low cancer cells to asparaginase by disrupting the amino acid response
Inhibition of GCN2 sensitizes ASNS-low cancer cells to asparaginase by disrupting the amino acid response Open
Significance l -asparaginase (ASNase) is a critical component of treatment protocols for acute lymphoblastic leukemia (ALL). Although the cure rates have dramatically improved, the prognosis for patients with recurrent ALL remains poor. Ge…
View article: Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents
Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents Open
View article: CCDC 1511207: Experimental Crystal Structure Determination
CCDC 1511207: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1511402: Experimental Crystal Structure Determination
CCDC 1511402: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: 2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase
2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase Open
View article: Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones
Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones Open
View article: Using a biologically annotated library to analyze the anticancer mechanism of serine palmitoyl transferase (SPT) inhibitors
Using a biologically annotated library to analyze the anticancer mechanism of serine palmitoyl transferase (SPT) inhibitors Open
Mechanistic understanding is crucial to anticancer drug discovery. Here, we reveal that inhibition of serine palmitoyl transferase (SPT), the rate‐limiting enzyme in sphingolipid synthesis, induced death in a lung cancer cell line via a ne…
View article: CCDC 1520568: Experimental Crystal Structure Determination
CCDC 1520568: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1520566: Experimental Crystal Structure Determination
CCDC 1520566: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1520567: Experimental Crystal Structure Determination
CCDC 1520567: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …