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  1. AU="Zhong, Boyu"
  2. AU=Gimeno-Costa Ricardo AU=Gimeno-Costa Ricardo
  3. AU="Wu, Jiangbo"
  4. AU="MacIntyre, Michael F"
  5. AU="Moon, H K"
  6. AU="Clark, Mindie"
  7. AU="Nichols, Aaron L"
  8. AU="Cash-Goldwasser, Shama"
  9. AU="Christopher B. Daniels"
  10. AU="Wakama, Hitoshi"
  11. AU="Crowe, K"
  12. AU="Merz, Sabine"
  13. AU=Rossolatos George
  14. AU="Nalla, Shahed"
  15. AU="Alvarado, Miriam"
  16. AU="Garduño-Sánchez, Marco"
  17. AU="Khan, Sherbano"
  18. AU="Kakava, Felicia"

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  1. Artikel ; Online: Meeting the potential emergency global drug supply challenge of hydroxychloroquine for COVID-19.

    Zhang, Tony Y / Zhong, Boyu

    Medicine in drug discovery

    2020  Band 5, Seite(n) 100036

    Abstract: This paper provides an overview of the current global market and manufacturing landscape for hydroxychloroquine (HCQ). The capacity and capabilities of global producers to meet the potential demand for treating patients inflicted with COVID-19 by the ... ...

    Abstract This paper provides an overview of the current global market and manufacturing landscape for hydroxychloroquine (HCQ). The capacity and capabilities of global producers to meet the potential demand for treating patients inflicted with COVID-19 by the novel corona virus SARS-CoV-2, should HCQ's efficacy be established by more definitive clinical trials, is also assessed. Given the large existing manufacturing base and abundance of raw materials for HCQ, the supply challenge can be met with considerable efforts and international cooperation. Preemptive and coordinated emergency efforts among global governments, regulatory agencies, chemical and pharmaceutical industries are imperative for meeting the potential surge in demand.
    Schlagwörter covid19
    Sprache Englisch
    Erscheinungsdatum 2020-04-09
    Erscheinungsland Netherlands
    Dokumenttyp Journal Article ; Review
    ISSN 2590-0986
    ISSN (online) 2590-0986
    DOI 10.1016/j.medidd.2020.100036
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  2. Artikel ; Online: Meeting the potential emergency global drug supply challenge of hydroxychloroquine for COVID-19

    Zhang, Tony Y. / Zhong, Boyu

    Medicine in Drug Discovery

    2020  Band 5, Seite(n) 100036

    Schlagwörter covid19
    Sprache Englisch
    Verlag Elsevier BV
    Erscheinungsland us
    Dokumenttyp Artikel ; Online
    ISSN 2590-0986
    DOI 10.1016/j.medidd.2020.100036
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  3. Artikel: Meeting the Potential Emergency Global Drug Supply Challenge of Hydroxychloroquine for COVID-19

    Zhang, Tony Y / Zhong, Boyu

    Med Drug Discov

    Abstract: This paper provides an overview of the current global market and manufacturing landscape for hydroxychloroquine (HCQ). The capacity and capabilities of global producers to meet the potential demand for treating patients inflicted with COVID-19 by the ... ...

    Abstract This paper provides an overview of the current global market and manufacturing landscape for hydroxychloroquine (HCQ). The capacity and capabilities of global producers to meet the potential demand for treating patients inflicted with COVID-19 by the novel corona virus SARS-CoV-2, should HCQ's efficacy be established by more definitive clinical trials, is also assessed. Given the large existing manufacturing base and abundance of raw materials for HCQ, the supply challenge can be met with considerable efforts and international cooperation. Preemptive and coordinated emergency efforts among global governments, regulatory agencies, chemical and pharmaceutical industries are imperative for meeting the surge in demand.
    Schlagwörter covid19
    Verlag WHO
    Dokumenttyp Artikel
    Anmerkung WHO #Covidence: #32292908
    Datenquelle COVID19

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  4. Artikel: Poly(ethylene glycol)-supported enzyme inactivators. Efficient identification of the site of covalent attachment to alpha-chymotrypsin by PEG-TPCK.

    Schering, Christine A / Zhong, Boyu / Woo, Jonathan C G / Silverman, Richard B

    Bioconjugate chemistry

    2004  Band 15, Heft 4, Seite(n) 673–676

    Abstract: A new methodology utilizing an enzyme inactivator covalently attached to poly(ethylene glycol) (PEG) is described in which the PEG affords facile and mild quantification, isolation, and identification of the site of enzyme inactivation. As proof of ... ...

    Abstract A new methodology utilizing an enzyme inactivator covalently attached to poly(ethylene glycol) (PEG) is described in which the PEG affords facile and mild quantification, isolation, and identification of the site of enzyme inactivation. As proof of concept, the known affinity labeling agent for alpha-chymotrypsin, N-tosyl-L-phenylalanine chloromethyl ketone (TPCK), was linked to PEG. The synthesis of the PEG-bound inactivator PEG-TPCK was carried out in good yields using standard solution-phase chemistry. Inactivation of alpha-chymotrypsin with PEG-TPCK was monitored via UV-vis spectroscopy in aqueous conditions, which resulted in less than 3% remaining activity, indicating that 97% of the alpha-chymotrypsin was covalently modified with PEG-TPCK. The MALDI-TOF mass spectrum showed only one new peak that was distinct in shape and corresponded to the mass of PEG-TPCK-alpha-chymotrypsin. Following proteolytic digestion, the PEG-TPCK-peptide was easily discernible from the rest of the digest in a HPLC trace because of its characteristic prolonged retention time and broad polymer shape. MALDI-TOF MS was used to determine the mass of the PEGylated peptide. Without prior removal of the PEG, the amino acid site to which PEG-TPCK covalently bound was determined via Edman sequencing. In comparison to other methods, the PEG-supported inactivator system is significantly cheaper and safer than the synthesis of radiolabeled compounds; furthermore, isolation of the PEGylated peptide is milder and more selective than standard affinity binding columns. Edman sequencing provides an exact determination of the site of inactivator covalent attachment without extensive, tedious LC-MS analysis of a complex peptide mixture. The method described here could be applied to a variety of enzymes as an alternative to current techniques.
    Mesh-Begriff(e) Chromatography, High Pressure Liquid ; Chymotrypsin/antagonists & inhibitors ; Chymotrypsin/chemistry ; Chymotrypsin/metabolism ; Enzyme Activation ; Enzyme Inhibitors/chemistry ; Molecular Structure ; Polyethylene Glycols/chemistry ; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization ; Tosylphenylalanyl Chloromethyl Ketone/chemistry
    Chemische Substanzen Enzyme Inhibitors ; Polyethylene Glycols (30IQX730WE) ; Tosylphenylalanyl Chloromethyl Ketone (402-71-1) ; Chymotrypsin (EC 3.4.21.1) ; alpha-chymotrypsin (EC 3.4.21.1)
    Sprache Englisch
    Erscheinungsdatum 2004-07
    Erscheinungsland United States
    Dokumenttyp Journal Article ; Research Support, U.S. Gov't, P.H.S.
    ZDB-ID 1024041-x
    ISSN 1520-4812 ; 1043-1802
    ISSN (online) 1520-4812
    ISSN 1043-1802
    DOI 10.1021/bc049940p
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  5. Artikel ; Online: Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.

    Zhang, Peilong / Dong, Jiaqiang / Zhong, Boyu / Zhang, Deyi / Yuan, Hongbin / Jin, Can / Xu, Xiangyuan / Li, Hailong / Zhou, Yong / Liang, Zhi / Ji, Minghua / Xu, Tao / Song, Guowei / Zhang, Ling / Chen, Gang / Meng, Xuejing / Sun, Desheng / Shih, Joe / Zhang, Ruihao /
    Hou, Guojun / Wang, Chengcheng / Jin, Ying / Yang, Qiong

    Bioorganic & medicinal chemistry letters

    2016  Band 26, Heft 8, Seite(n) 1910–1918

    Abstract: Anaplastic lymphoma kinase (ALK) is a highly attractive therapeutic target for the treatment of some non-small cell lung cancer patients. This Letter describes the further SAR exploration on the novel 3-sulfonylpyrazol-4-amino pyrimidine scaffold. This ... ...

    Abstract Anaplastic lymphoma kinase (ALK) is a highly attractive therapeutic target for the treatment of some non-small cell lung cancer patients. This Letter describes the further SAR exploration on the novel 3-sulfonylpyrazol-4-amino pyrimidine scaffold. This work identified a compound 53 with very good in vitro/in vivo efficacies, good DMPK properties together with better hERG tolerability and it is currently being profiled for the evaluation as a potential pre-clinical candidate.
    Mesh-Begriff(e) Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dogs ; Dose-Response Relationship, Drug ; Drug Design ; Drug Screening Assays, Antitumor ; Humans ; Mice ; Models, Molecular ; Molecular Structure ; Neoplasms, Experimental/drug therapy ; Neoplasms, Experimental/pathology ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacology ; Pyrazoles/chemical synthesis ; Pyrazoles/chemistry ; Pyrazoles/pharmacology ; Pyrimidines/chemical synthesis ; Pyrimidines/chemistry ; Pyrimidines/pharmacology ; Rats ; Receptor Protein-Tyrosine Kinases/antagonists & inhibitors ; Receptor Protein-Tyrosine Kinases/metabolism ; Structure-Activity Relationship
    Chemische Substanzen 3-sulfonylpyrazol-4-amino pyrimidine ; Antineoplastic Agents ; Protein Kinase Inhibitors ; Pyrazoles ; Pyrimidines ; Receptor Protein-Tyrosine Kinases (EC 2.7.10.1) ; anaplastic lymphoma kinase (EC 2.7.10.1)
    Sprache Englisch
    Erscheinungsdatum 2016-04-15
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2016.03.017
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  6. Artikel ; Online: Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.

    Zhang, Peilong / Dong, Jiaqiang / Zhong, Boyu / Zhang, Deyi / Jin, Can / Meng, Xuejing / Sun, Desheng / Xu, Xiangyuan / Zhou, Yong / Liang, Zhi / Ji, Minghua / Li, Hailong / Xu, Tao / Song, Guowei / Zhang, Ling / Chen, Gang / Yuan, Hongbin / Shih, Joe / Zhang, Ruihao /
    Hou, Guojun / Jin, Ying / Yang, Qiong

    Bioorganic & medicinal chemistry letters

    2015  Band 25, Heft 17, Seite(n) 3738–3743

    Abstract: A new series of 2,4-diamino pyrimidine derivatives with a sulfone-substituted pyrazole right side-chain were discovered as potent anaplastic lymphoma kinase inhibitors. Structure-activity relationship of the left side-chain on phenyl substitutions were ... ...

    Abstract A new series of 2,4-diamino pyrimidine derivatives with a sulfone-substituted pyrazole right side-chain were discovered as potent anaplastic lymphoma kinase inhibitors. Structure-activity relationship of the left side-chain on phenyl substitutions were explored which delivered many potent ALK inhibitors. Among them, 29a showed favorable pharmacokinetic profiles in rats and dogs together with significant antitumor efficacy in EML4-ALK fusion xenograft model.
    Mesh-Begriff(e) Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Biological Availability ; Chemistry Techniques, Synthetic ; Dogs ; Drug Design ; Drug Discovery ; Humans ; Mice ; Molecular Targeted Therapy ; Oncogene Proteins, Fusion/genetics ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacology ; Pyrimidines/chemistry ; Pyrimidines/pharmacology ; Rats, Sprague-Dawley ; Receptor Protein-Tyrosine Kinases/antagonists & inhibitors ; Receptor Protein-Tyrosine Kinases/genetics ; Structure-Activity Relationship ; Xenograft Model Antitumor Assays/methods
    Chemische Substanzen Antineoplastic Agents ; EML4-ALK fusion protein, human ; Oncogene Proteins, Fusion ; Protein Kinase Inhibitors ; Pyrimidines ; Receptor Protein-Tyrosine Kinases (EC 2.7.10.1) ; anaplastic lymphoma kinase (EC 2.7.10.1)
    Sprache Englisch
    Erscheinungsdatum 2015-09-01
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2015.06.021
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  7. Artikel ; Online: LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models.

    Yan, S Betty / Peek, Victoria L / Ajamie, Rose / Buchanan, Sean G / Graff, Jeremy R / Heidler, Steven A / Hui, Yu-Hua / Huss, Karen L / Konicek, Bruce W / Manro, Jason R / Shih, Chuan / Stewart, Julie A / Stewart, Trent R / Stout, Stephanie L / Uhlik, Mark T / Um, Suzane L / Wang, Yong / Wu, Wenjuan / Yan, Lei /
    Yang, Wei J / Zhong, Boyu / Walgren, Richard A

    Investigational new drugs

    2012  Band 31, Heft 4, Seite(n) 833–844

    Abstract: The HGF/MET signaling pathway regulates a wide variety of normal cellular functions that can be subverted to support neoplasia, including cell proliferation, survival, apoptosis, scattering and motility, invasion, and angiogenesis. MET over-expression ( ... ...

    Abstract The HGF/MET signaling pathway regulates a wide variety of normal cellular functions that can be subverted to support neoplasia, including cell proliferation, survival, apoptosis, scattering and motility, invasion, and angiogenesis. MET over-expression (with or without gene amplification), aberrant autocrine or paracrine ligand production, and missense MET mutations are mechanisms that lead to activation of the MET pathway in tumors and are associated with poor prognostic outcome. We report here preclinical development of a potent, orally bioavailable, small-molecule inhibitor LY2801653 targeting MET kinase. LY2801653 is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. LY2801653 demonstrated in vitro effects on MET pathway-dependent cell scattering and cell proliferation; in vivo anti-tumor effects in MET amplified (MKN45), MET autocrine (U-87MG, and KP4) and MET over-expressed (H441) xenograft models; and in vivo vessel normalization effects. LY2801653 also maintained potency against 13 MET variants, each bearing a single-point mutation. In subsequent nonclinical characterization, LY2801653 was found to have potent activity against several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1/2 and against the serine/threonine kinases MKNK1/2. The potential value of MET and other inhibited targets within a number of malignancies (such as colon, bile ducts, and lung) is discussed. LY2801653 is currently in phase 1 clinical testing in patients with advanced cancer (trial I3O-MC-JSBA, NCT01285037).
    Mesh-Begriff(e) Administration, Oral ; Animals ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Biological Availability ; Blood Vessels/drug effects ; Blood Vessels/pathology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Humans ; Indazoles/administration & dosage ; Indazoles/chemistry ; Indazoles/pharmacology ; Mice ; Mutation/genetics ; Niacinamide/administration & dosage ; Niacinamide/analogs & derivatives ; Niacinamide/chemistry ; Niacinamide/pharmacology ; Protein Kinase Inhibitors/administration & dosage ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacology ; Proto-Oncogene Proteins c-met/antagonists & inhibitors ; Proto-Oncogene Proteins c-met/metabolism ; Receptor Protein-Tyrosine Kinases/antagonists & inhibitors ; Receptor Protein-Tyrosine Kinases/metabolism ; Tetrazoles/administration & dosage ; Tetrazoles/chemistry ; Tetrazoles/pharmacology ; Xenograft Model Antitumor Assays
    Chemische Substanzen Antineoplastic Agents ; Indazoles ; Protein Kinase Inhibitors ; Tetrazoles ; Niacinamide (25X51I8RD4) ; merestinib (5OGS5K699E) ; Proto-Oncogene Proteins c-met (EC 2.7.10.1) ; RON protein (EC 2.7.10.1) ; Receptor Protein-Tyrosine Kinases (EC 2.7.10.1)
    Sprache Englisch
    Erscheinungsdatum 2012-12-29
    Erscheinungsland United States
    Dokumenttyp Clinical Trial, Phase I ; Journal Article
    ZDB-ID 604895-x
    ISSN 1573-0646 ; 0167-6997
    ISSN (online) 1573-0646
    ISSN 0167-6997
    DOI 10.1007/s10637-012-9912-9
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  8. Artikel: Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.

    Hamdouchi, Chafiq / Zhong, Boyu / Mendoza, Jose / Collins, Elizabeth / Jaramillo, Carlos / De Diego, Jose Eugenio / Robertson, Daniel / Spencer, Charles D / Anderson, Bryan D / Watkins, Scott A / Zhang, Faming / Brooks, Harold B

    Bioorganic & medicinal chemistry letters

    2005  Band 15, Heft 7, Seite(n) 1943–1947

    Abstract: Structure-based design approach was successfully used to guide the evolution of imidazopyridine scaffold yielding new structural class of highly selective inhibitors of cyclin dependent kinases that were able to form a new interaction with an identified ... ...

    Abstract Structure-based design approach was successfully used to guide the evolution of imidazopyridine scaffold yielding new structural class of highly selective inhibitors of cyclin dependent kinases that were able to form a new interaction with an identified residue of the protein, Lys89. Compounds from this series have shown no detectable effect when tested against a representative set of other serine/threonine kinases such as GSK3beta, CAMKII, PKA, PKC-alpha,beta,epsilon,gamma. Compound 2i inhibits proliferation in HCT 116 cells in tissue culture. Synthesis, co-crystal structure of CDK2 in complex with compound 2i, and preliminary SAR study are disclosed.
    Mesh-Begriff(e) Cells, Cultured ; Cyclin-Dependent Kinases/antagonists & inhibitors ; Drug Design ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/pharmacology ; HCT116 Cells ; Humans ; Imidazoles/chemical synthesis ; Imidazoles/pharmacology ; Inhibitory Concentration 50 ; Lysine/chemistry ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/pharmacology ; Pyridines/chemical synthesis ; Pyridines/pharmacology ; Structure-Activity Relationship
    Chemische Substanzen Enzyme Inhibitors ; Imidazoles ; Protein Kinase Inhibitors ; Pyridines ; Cyclin-Dependent Kinases (EC 2.7.11.22) ; Lysine (K3Z4F929H6)
    Sprache Englisch
    Erscheinungsdatum 2005-04-01
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2005.01.052
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  9. Artikel: Europium-labeled melanin-concentrating hormone analogues: ligands for measuring binding to melanin-concentrating hormone receptors 1 and 2.

    Gao, Xiaoying / Hsu, Chiun-King / Heinz, Lawrence J / Morin, John / Shi, Yuguang / Shukla, Nikhil K / Smiley, David L / Xu, Jie / Zhong, Boyu / Slieker, Lawrence J

    Analytical biochemistry

    2004  Band 328, Heft 2, Seite(n) 187–195

    Abstract: We investigated the use of Eu3+ chelate-labeled analogues of melanin-concentrating hormone (MCH) as ligands for both human MCH receptors (MCHR1 and MCHR2). The analogues employed were Ala17 MCH, S36057 (Y-ADO-RC*MLGRVFRPC*W, where ADO=8-amino-3,6- ... ...

    Abstract We investigated the use of Eu3+ chelate-labeled analogues of melanin-concentrating hormone (MCH) as ligands for both human MCH receptors (MCHR1 and MCHR2). The analogues employed were Ala17 MCH, S36057 (Y-ADO-RC*MLGRVFRPC*W, where ADO=8-amino-3,6-dioxyoctanoyl and *=disulfide bond), and R2P (RC*MLGRVFRPC*Y-NH2). The peptides were readily labeled on the alpha-amino residue with the Eu3+ chelate of N1-(p-isothiocyanatobenzyl)-diethylenetriamine-N1,N2,N3,N3-tetraacetic acid and then purified by reverse-phase fast-performance liquid chromatography at neutral pH to maintain Eu3+ chelation. Both labeled Ala17 MCH and S36057 had high affinity for MCHR1 ( Kd = 0.37 and 0.059nM, respectively) while Eu3+ -labeled S36057 and R2P had high affinity for MCHR2 ( Kd = 0.16 and 0.10nM, respectively). Labeled Ala17 MCH had little demonstrable binding affinity for MCHR2. Eu3+ -labeled S36057 and R2P were full agonists at MCHR1 when assessed by measurement of agonist-stimulated GTPgamma(35)S binding. Competition binding experiments with both MCHR isoforms, a series of previously characterized alanine scan MCH analogues, and a recently identified nonpeptide MCHR1-selective antagonist T-226296 confirmed the expected receptor selectivity. These studies further extend the utility of Eu3+ chelate time-resolved fluorescence for the development of high-sensitivity, nonradioactive receptor binding assays and demonstrate the need to select the optimal ligand for labeling.
    Mesh-Begriff(e) Binding, Competitive ; Cell Line ; Cell Membrane/metabolism ; Cloning, Molecular ; Disulfides/chemistry ; Disulfides/metabolism ; Europium/chemistry ; Fluorescence ; Humans ; Ligands ; Melanins/chemistry ; Melanins/metabolism ; Organometallic Compounds/chemistry ; Protein Binding ; Radioligand Assay ; Receptors, Pituitary Hormone/metabolism ; Sensitivity and Specificity ; Staining and Labeling
    Chemische Substanzen Disulfides ; Ligands ; Melanins ; Organometallic Compounds ; Receptors, Pituitary Hormone ; europium(III) chelate-2,2',2'',2'''-((4-((4-isothiocyanatophenyl)ethynyl)pyridine-2,6-diyl)bis(methylenenitrilo))tetrakis(acetic acid) ; melanin-concentrating hormone receptor ; Europium (444W947O8O)
    Sprache Englisch
    Erscheinungsdatum 2004-05-15
    Erscheinungsland United States
    Dokumenttyp Journal Article
    ZDB-ID 1110-1
    ISSN 1096-0309 ; 0003-2697
    ISSN (online) 1096-0309
    ISSN 0003-2697
    DOI 10.1016/j.ab.2004.01.017
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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