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Takashi Tsukamoto

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Chemicals & Drugs

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Takashi Tsukamoto; Kwang-Hwan Jung; Naoki Kamo; Takashi Kikukawa; Takuro Kurata; Makoto Demura
Salt bridge in the conserved His-Asp cluster in Gloeobacter rhodopsin contributes to trimer formation.
Krupa Shukla; Barbara Slusher; M Stathis; Ajit G Thomas; Yan Xiang; Jesse Alt; Chi Dang; Greg Delahanty; Bridget Duvall; Dana Ferraris; Ping Gao; Rana Rais; Camilo Rojas; Takashi Tsukamoto
Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors.
Krystyna M Wozniak; Ying Wu; Takashi Tsukamoto; James J Vornov; Rena Lapidus; Rana Rais; Camilo Rojas; Barbara Slusher
The orally active glutamate carboxypeptidase II inhibitor E2072 exhibits sustained nerve exposure and attenuates peripheral neuropathy.

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2013: Takashi Tsukamoto; Kwang-Hwan Jung; Naoki Kamo; Takashi Kikukawa; Takuro Kurata; Makoto Demura
Salt bridge in the conserved His-Asp cluster in Gloeobacter rhodopsin contributes to trimer formation.
FEBS letters 2013;587(4):322-7.
2012: Krupa Shukla; Barbara Slusher; M Stathis; Ajit G Thomas; Yan Xiang; Jesse Alt; Chi Dang; Greg Delahanty; Bridget Duvall; Dana Ferraris; Ping Gao; Rana Rais; Camilo Rojas; Takashi Tsukamoto
Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors.
Journal of medicinal chemistry 2012;55(23):10551-63.
2012: Krystyna M Wozniak; Ying Wu; Takashi Tsukamoto; James J Vornov; Rena Lapidus; Rana Rais; Camilo Rojas; Barbara Slusher
The orally active glutamate carboxypeptidase II inhibitor E2072 exhibits sustained nerve exposure and attenuates peripheral neuropathy.
The Journal of pharmacology and experimental therapeutics 2012;343(3):746-54.
2012: Rana Rais; Camilo Rojas; Michelle A Rudek; Jesse Alt; Randall Hoover; Takashi Tsukamoto; Krystyna Wozniak; Barbara Slusher
Reversible disulfide formation of the glutamate carboxypeptidase II inhibitor E2072 results in prolonged systemic exposures in vivo.
Drug metabolism and disposition: the biological fate of chemicals 2012;40(12):2315-23.
2012: Rana Rais; Camilo Rojas; Akira Sawa; Barbara Slusher; Christine A Strick; Ajit G Thomas; Nicholas J Brandon; Sandra J Engle; Hanna Jaaro-Peled; Krystyna Wozniak; Ying Wu; Takashi Tsukamoto
Pharmacokinetics of oral D-serine in D-amino acid oxidase knockout mice.
Drug metabolism and disposition: the biological fate of chemicals 2012;40(11):2067-73.
2012: Doris Stoermer; Dilrukshi Vitharana; Krystyna M Wozniak; Ying Wu; Greg Delahanty; Bridget Duvall; Dana Ferraris; Brian S Grella; Niyada Hin; Randall Hoover; Camilo Rojas; Megan K Shanholtz; Barbara Slusher; Kyle P Smith; M Stathis; Takashi Tsukamoto
Design, synthesis, and pharmacological evaluation of glutamate carboxypeptidase II (GCPII) inhibitors based on thioalkylbenzoic acid scaffolds.
Journal of medicinal chemistry 2012;55(12):5922-32.
2012: Takashi Tsukamoto; Tomoyasu Aizawa; Kazuhiro J Fujimoto; Masakatsu Kamiya; Naoki Kamo; Keiichi Kawano; Takashi Kikukawa; Takanori Sasaki; Makoto Demura
Homotrimer formation and dissociation of pharaonis halorhodopsin in detergent system.
Biophysical journal 2012;102(12):2906-15.
2012: Mariia O Yuneva; Thaddeus D Allen; Francisco J Alonso; Xin Chen; Teresa W-M Fan; Dana V Ferraris; Richard M Higashi; José M Matés; Youngho Seo; Takashi Tsukamoto; Chunmei Wang; J Michael Bishop
The metabolic profile of tumors depends on both the responsible genetic lesion and tissue type.
Cell metabolism 2012;15(2):157-70.
2012: Anne Le; Sminu Bose; Haixia Zhang; Max Hamaker; Joseph Barbi; Richard M Higashi; Daniel C Liebler; Andrew N Lane; Camilio J Rojas; Arvin Gouw; Pawel Lorkiewicz; Lisa J Zimmerman; Barbara Slusher; Teresa W M Fan; Robbert J C Slebos; Takashi Tsukamoto; Chi Dang
Glucose-independent glutamine metabolism via TCA cycling for proliferation and survival in B cells.
Cell metabolism 2012;15(1):110-21.
2012: Dana Ferraris; K Shukla; Takashi Tsukamoto
Structure-activity relationships of glutamate carboxypeptidase II (GCPII) inhibitors.
Current medicinal chemistry 2012;19(9):1282-94.
2011: Jesse Alt; Dana Ferraris; Camilo Rojas; Takashi Tsukamoto; Krystyna Wozniak; Ying Wu; Barbara Slusher
Development of a high-throughput method for the determination of pharmacological levels of plasma D-serine.
Analytical biochemistry 2011;419(2):106-9.
2011: Yasutaka Yamashita; Tomoyasu Aizawa; Masakatsu Kamiya; Naoki Kamo; Keiichi Kawano; Takashi Kikukawa; Seiji Miyauchi; Takashi Tsukamoto; Makoto Demura
Expression of salinarum halorhodopsin in Escherichia coli cells: solubilization in the presence of retinal yields the natural state.
Biochimica et biophysica acta 2011;1808(12):2905-12.
2011: Krupa Shukla; Barbara Slusher; Ajit G Thomas; Jesse Alt; Dana Ferraris; Niyada Hin; Camilo Rojas; Rita Sattler; Takashi Tsukamoto
Inhibition of xc⁻ transporter-mediated cystine uptake by sulfasalazine analogs.
Bioorganic & medicinal chemistry letters 2011;21(20):6184-7.
2011: Mohamed H Farah; Baohan Pan; Paul N Hoffman; Dana Ferraris; Takashi Tsukamoto; THIEN NGUYEN; Philip C Wong; Donald L Price; Barbara Slusher; John W Griffin
Reduced BACE1 activity enhances clearance of myelin debris and regeneration of axons in the injured peripheral nervous system.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2011;31(15):5744-54.
2011: Yuto Takatsu; Yuko Fujita; Takashi Tsukamoto; Barbara Slusher; Kenji Hashimoto
Orally active glutamate carboxypeptidase II inhibitor 2-MPPA attenuates dizocilpine-induced prepulse inhibition deficits in mice.
Brain research 2011;1371():82-6.
2011: Dana V Ferraris; Takashi Tsukamoto
Recent advances in the discovery of D-amino acid oxidase inhibitors and their therapeutic utility in schizophrenia.
Current pharmaceutical design 2011;17(2):103-11.
2010: Brian Grella; Jessica Adams; James F Berry; Greg Delahanty; Dana V Ferraris; Pavel Majer; Chiyou Ni; Krupa Shukla; Scott A Shuler; Barbara Slusher; Marigo Stathis; Takashi Tsukamoto
The discovery and structure-activity relationships of indole-based inhibitors of glutamate carboxypeptidase II.
Bioorganic & medicinal chemistry letters 2010;20(24):7222-5.
2010: Meghan J Seltzer; Bryson D Bennett; Avadhut Joshi; Ping Gao; Ajit G Thomas; Dana V Ferraris; Takashi Tsukamoto; Camilo J Rojas; Barbara Slusher; Joshua D Rabinowitz; Chi Dang; Gregory J Riggins
Inhibition of glutaminase preferentially slows growth of glioma cells with mutant IDH1.
Cancer research 2010;70(22):8981-7.
2009: Kenji Hashimoto; Yuko Fujita; Mao Horio; Shinsui Kunitachi; Masaomi Iyo; Dana Ferraris; Takashi Tsukamoto
Co-administration of a D-amino acid oxidase inhibitor potentiates the efficacy of D-serine in attenuating prepulse inhibition deficits after administration of dizocilpine.
Biological psychiatry 2009;65(12):1103-6.
2009: Valerie Humblet; Preeti Misra; Kumar R Bhushan; Khaled Nasr; Yao-Sen Ko; Takashi Tsukamoto; Nadine Pannier; John V Frangioni; Wolfgang Maison
Multivalent scaffolds for affinity maturation of small molecule cell surface binders and their application to prostate tumor targeting.
Journal of medicinal chemistry 2009;52(2):544-50.
2008: Dana Ferraris; Bridget Duvall; Yao-Sen Ko; Ajit G Thomas; Camilo Rojas; Pavel Majer; Kenji Hashimoto; Takashi Tsukamoto
Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
Journal of medicinal chemistry 2008;51(12):3357-9.
2008: Cyril Barinka; Klara Hlouchova; Miroslava Rovenska; Pavel Majer; Miroslawa Dauter; Niyada Hin; Yao-Sen Ko; Takashi Tsukamoto; Barbara Slusher; Jan Konvalinka; Jacek Lubkowski
Structural basis of interactions between human glutamate carboxypeptidase II and its substrate analogs.
Journal of molecular biology 2008;376(5):1438-50.
2007: Mary M Robinson; Steven J McBryant; Takashi Tsukamoto; Camilo Rojas; Dana V Ferraris; Sean K Hamilton; Jeffrey C Hansen; Norman P Curthoys
Novel mechanism of inhibition of rat kidney-type glutaminase by bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES).
The Biochemical journal 2007;406(3):407-14.
2007: Takashi Tsukamoto; Krystyna M Wozniak; Barbara Slusher
Progress in the discovery and development of glutamate carboxypeptidase II inhibitors.
Drug discovery today 2007;12(17-18):767-76.
2007: Cyril Barinka; Miroslava Rovenská; Petra Mlcochová; Klára Hlouchová; Anna Plechanovová; Pavel Majer; Takashi Tsukamoto; Barbara Slusher; Jan Konvalinka; Jacek Lubkowski
Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.
Journal of medicinal chemistry 2007;50(14):3267-73.
2007: Nathan Erdmann; Jianxing Zhao; Alicia L Lopez; Shelley Herek; Norman P Curthoys; Terry D Hexum; Takashi Tsukamoto; Dana Ferraris; Jialin Charles Zheng
Glutamate production by HIV-1 infected human macrophage is blocked by the inhibition of glutaminase.
Journal of neurochemistry 2007;102(2):539-49.
2006: Pavel Majer; Bunda Hin; Doris Stoermer; Jessica Adams; Weizheng Xu; Bridget R Duvall; Greg Delahanty; Qun Liu; Marigo J Stathis; Krystyna M Wozniak; Barbara Slusher; Takashi Tsukamoto
Structural optimization of thiol-based inhibitors of glutamate carboxypeptidase II by modification of the P1' side chain.
Journal of medicinal chemistry 2006;49(10):2876-85.
2006: Jeroen R Mesters; Cyril Barinka; Weixing Li; Takashi Tsukamoto; Pavel Majer; Barbara Slusher; Jan Konvalinka; Rolf Hilgenfeld
Structure of glutamate carboxypeptidase II, a drug target in neuronal damage and prostate cancer.
The EMBO journal 2006;25(6):1375-84.
2006: Ajit G Thomas; Krystyna M Wozniak; Takashi Tsukamoto; David Calvin; Ying Wu; Camilo Rojas; James J Vornov; Barbara Slusher
Glutamate carboxypeptidase II (NAALADase) inhibition as a novel therapeutic strategy.
Advances in experimental medicine and biology 2006;576():327-37; discussion 361-3.
2005: Valerie Humblet; Rena Lapidus; Larry R Williams; Takashi Tsukamoto; Camilo Rojas; Pavel Majer; Bunda Hin; Shunsuke Ohnishi; Alec M De Grand; Atif Zaheer; Jürgen T Renze; Akira Nakayama; Barbara Slusher; John V Frangioni
High-affinity near-infrared fluorescent small-molecule contrast agents for in vivo imaging of prostate-specific membrane antigen.
Molecular imaging 2005;4(4):448-62.
2005: Takashi Tsukamoto; Pavel Majer; Dilrukshi Vitharana; Chiyou Ni; Bunda Hin; X-C May Lu; Ajit G Thomas; Krystyna M Wozniak; David Calvin; Ying Wu; Barbara Slusher; David Scarpetti; George W Bonneville
Enantiospecificity of glutamate carboxypeptidase II inhibition.
Journal of medicinal chemistry 2005;48(7):2319-24.
2003: Nathaniel J Cosper; David L Bienvenue; Jacob E Shokes; Danuta M Gilner; Takashi Tsukamoto; Robert A Scott; Richard C Holz
The dapE-encoded N-succinyl-l,l-diaminopimelic acid desuccinylase from Haemophilus influenzae is a dinuclear metallohydrolase.
Journal of the American Chemical Society 2003;125(48):14654-5.
2003: Ghanashyam D Ghadge; Barbara Slusher; Amos Bodner; Mauro Dal Canto; Krystyna M Wozniak; Ajit G Thomas; Camilo Rojas; Takashi Tsukamoto; Pavel Majer; Richard J Miller; Anna Liza Monti; Raymond P Roos
Glutamate carboxypeptidase II inhibition protects motor neurons from death in familial amyotrophic lateral sclerosis models.
Proceedings of the National Academy of Sciences of the United States of America 2003;100(16):9554-9.
2003: Doris Stoermer; Qun Liu; Monicia R Hall; Juliet M Flanary; Ajit G Thomas; Camilo Rojas; Barbara Slusher; Takashi Tsukamoto
Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II.
Bioorganic & medicinal chemistry letters 2003;13(13):2097-100.
2003: Pavel Majer; Paul F Jackson; Greg Delahanty; Brian S Grella; Yao-Sen Ko; Weixing Li; Qun Liu; Keith M Maclin; Jana Poláková; Kathryn A Shaffer; Doris Stoermer; Dilrukshi Vitharana; Eric Wang; Anthony Zakrzewski; Camilo Rojas; Barbara Slusher; Krystyna M Wozniak; Eric Burak; Tharin Limsakun; Takashi Tsukamoto
Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor.
Journal of medicinal chemistry 2003;46(10):1989-96.
2003: Camilo Rojas; Ajit G Thomas; Pavel Majer; Takashi Tsukamoto; X M Lu; James J Vornov; Krystyna M Wozniak; Barbara Slusher
Glutamate carboxypeptidase II inhibition as a novel therapeutic target.
Advances in experimental medicine and biology 2003;524():205-13.
2002: Bunda Hin; Pavel Majer; Takashi Tsukamoto
Facile synthesis of alpha-substituted acrylate esters.
The Journal of organic chemistry 2002;67(21):7365-8.
2002: Takashi Tsukamoto; Juliet M Flanary; Camilo Rojas; Barbara Slusher; Nadya Valiaeva; James K Coward
Phosphonate and phosphinate analogues of N-acylated gamma-glutamylglutamate. potent inhibitors of glutamate carboxypeptidase II.
Bioorganic & medicinal chemistry letters 2002;12(16):2189-92.
2002: Weixian Zhang; Barbara Slusher; Yuichi Murakawa; Krystyna M Wozniak; Takashi Tsukamoto; Paul F Jackson; Anders A F Sima
GCPII (NAALADase) inhibition prevents long-term diabetic neuropathy in type 1 diabetic BB/Wor rats.
Journal of the neurological sciences 2002;194(1):21-8.
2001: Kunihiko Tani; Masaomi Iyo; H Matsumoto; Masayoshi Kawai; Katsuaki Suzuki; Yasuhide Iwata; T Won; Takashi Tsukamoto; Yoshimoto Sekine; M Sakanoue; Kenji Hashimoto; Y Ohashi; Nori Takei; Norio Mori
The effects of dentate granule cell destruction on behavioural activity and Fos protein expression induced by systemic methamphetamine in rats.
British journal of pharmacology 2001;134(7):1411-8.
2001: Paul F Jackson; K L Tays; K M Maclin; Yao-Sen Ko; Weixing Li; Dilrukshi Vitharana; Takashi Tsukamoto; Doris Stoermer; X-C May Lu; Krystyna M Wozniak; Barbara Slusher
Design and pharmacological activity of phosphinic acid based NAALADase inhibitors.
Journal of medicinal chemistry 2001;44(24):4170-5.
2001: Takashi Tsukamoto; Masaomi Iyo; Kunihiko Tani; Yoshimoto Sekine; Kenji Hashimoto; Y Ohashi; Katsuaki Suzuki; Yasuhide Iwata; Norio Mori
The effects of FK506, a specific calcineurin inhibitor, on methamphetamine-induced behavioral change and its sensitization in rats.
Psychopharmacology 2001;158(2):107-13.
1999: James J Vornov; Krystyna M Wozniak; M Lu; P Jackson; Takashi Tsukamoto; Eric Wang; Barbara Slusher
Blockade of NAALADase: a novel neuroprotective strategy based on limiting glutamate and elevating NAAG.
Annals of the New York Academy of Sciences 1999;890():400-5.
1998: Takashi Tsukamoto; William H Haile; John J McGuire; James K Coward
Mechanism-based inhibition of human folylpolyglutamate synthetase: design, synthesis, and biochemical characterization of a phosphapeptide mimic of the tetrahedral intermediate.
Archives of biochemistry and biophysics 1998;355(1):109-18.
1996: Takashi Tsukamoto; W H Haile; John J McGuire; James K Coward
Synthesis and biological evaluation of N alpha-(4-amino-4-deoxy-10-methylpteroyl)-DL-4,4-difluoroornithine.
Journal of medicinal chemistry 1996;39(13):2536-40.
1996: Takashi Tsukamoto; T Kitazume; John J McGuire; James K Coward
Synthesis and biological evaluation of DL-4,4-difluoroglutamic acid and DL-gamma,gamma-difluoromethotrexate.
Journal of medicinal chemistry 1996;39(1):66-72.
1996: John J McGuire; Takashi Tsukamoto; B P Hart; James K Coward; T I Kalman; John Galivan
Exploitation of folate and antifolate polyglutamylation to achieve selective anticancer chemotherapy.
Investigational new drugs 1996;14(3):317-23.