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  • 1
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    Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 1. Sildenafil analogs (2012)
    Details
    Publication Date: 2022-05-25
    Description: Author Posting. © The Author(s), 2012. This is the author's version of the work. It is posted here by permission of Elsevier B.V. for personal use, not for redistribution. The definitive version was published in Bioorganic & Medicinal Chemistry Letters 22 (2012): 2579-2581, doi:10.1016/j.bmcl.2012.01.119.
    Description: Parasitic diseases, such as African sleeping sickness, have a significant impact on the health and well-being in the poorest regions of the world. Pragmatic drug discovery efforts are needed to find new therapeutic agents. In this report we describe target repurposing efforts focused on trypanosomal phosphodiesterases. We outline the synthesis and biological evaluation of analogs of sildenafil (1), a human PDE5 inhibitor, for activities against trypanosomal PDEB1 (TbrPDEB1). We find that, while low potency analogs can be prepared, this chemical class is a sub-optimal starting point for further development of TbrPDE inhibitors.
    Description: This work was supported by the National Institutes of Health (R01AI082577), Boston University and Northeastern University.
    Keywords: Neglected disease ; Trypanosoma brucei ; Target repurposing ; Phosphodiesterase inhibitors ; TbrPDEB1 ; PDE5 ; Sildenafil
    Repository Name: Woods Hole Open Access Server
    Type: Preprint
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  • 2
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    Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 2. Tadalafil analogs (2012)
    Details
    Publication Date: 2022-05-25
    Description: Author Posting. © The Author(s), 2012. This is the author's version of the work. It is posted here by permission of Elsevier B.V. for personal use, not for redistribution. The definitive version was published in Bioorganic & Medicinal Chemistry Letters 22 (2012): 2582-2584, doi:10.1016/j.bmcl.2012.01.118.
    Description: In this report we describe our ongoing target repurposing efforts focused on discovery of inhibitors of the essential trypanosomal phosphodiesterase TbrPDEB1. This enzyme has been implicated in virulence of Trypanosoma brucei, the causative agent of human African trypanosomiasis (HAT). We outline the synthesis and biological evaluation of analogs of tadalafil, a human PDE5 inhibitor currently utilized for treatment of erectile dysfunction, and report that these analogs are weak inhibitors of TbrPDEB1.
    Description: This work was supported by the National Institutes of Health (R01AI082577), Boston University and Northeastern University.
    Keywords: Neglected disease ; Trypanosoma brucei ; Target repurposing ; Phosphodiesterase inhibitors ; TbrPDEB1 ; PDE5 ; Tadalafil
    Repository Name: Woods Hole Open Access Server
    Type: Preprint
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  • 3
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    Myelin tetraspan family proteins but no non-tetraspan family proteins are present in the ascidian (Ciona intestinalis) genome (2006)
    Marine Biological Laboratory
    Details
    Publication Date: 2022-05-25
    Description: Author Posting. © Marine Biological Laboratory, 2005. This article is posted here by permission of Marine Biological Laboratory for personal use, not for redistribution. The definitive version was published in Biological Bulletin 209 (2005): 49-66.
    Description: Several of the proteins used to form and maintain myelin sheaths in the central nervous system (CNS) and the peripheral nervous system (PNS) are shared among different vertebrate classes. These proteins include one-to-several alternatively spliced myelin basic protein (MBP) isoforms in all sheaths, proteolipid protein (PLP) and DM20 (except in amphibians) in tetrapod CNS sheaths, and one or two protein zero (P0) isoforms in fish CNS and in all vertebrate PNS sheaths. Several other proteins, including 2', 3'-cyclic nucleotide 3'-phosphodiesterase (CNP), myelin and lymphocyte protein (MAL), plasmolipin, and peripheral myelin protein 22 (PMP22; prominent in PNS myelin), are localized to myelin and myelin-associated membranes, though class distributions are less well studied. Databases with known and identified sequences of these proteins from cartilaginous and teleost fishes, amphibians, reptiles, birds, and mammals were prepared and used to search for potential homologs in the basal vertebrate, Ciona intestinalis. Homologs of lipophilin proteins, MAL/plasmolipin, and PMP22 were identified in the Ciona genome. In contrast, no MBP, P0, or CNP homologs were found. These studies provide a framework for understanding how myelin proteins were recruited during evolution and how structural adaptations enabled them to play key roles in myelination.
    Description: This work was supported by grant IBN-0402188 from the National Science Foundation (RMG).
    Repository Name: Woods Hole Open Access Server
    Type: Article
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  • 4
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    Synthesis and assessment of catechol diether compounds as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1) (2013)
    Details
    Publication Date: 2022-05-25
    Description: Author Posting. © The Author(s), 2013. This is the author's version of the work. It is posted here by permission of Elsevier B.V. for personal use, not for redistribution. The definitive version was published in Bioorganic & Medicinal Chemistry Letters 23 (2013): 5971-5974, doi:10.1016/j.bmcl.2013.08.057.
    Description: Human African trypanosomiasis (HAT) is a parasitic neglected tropical disease that affects 10,000 patients each year. Current treatments are sub-optimal, and the disease is fatal if not treated. Herein, we report our continuing efforts to repurpose the human phosphodiesterase 4 (hPDE4) inhibitor piclamilast to target trypanosomal phosphodiesterase TbrPDEB1. We prepared a range of substituted heterocyclic replacements for the 4-amino-3,5-dichloro-pyridine head group of piclamilast, and found that these compounds exhibited weak inhibitory activity of TbrPDEB1.
    Description: We acknowledge funding from the National Institutes of Health (R01AI082577).
    Repository Name: Woods Hole Open Access Server
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  • 5
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    Evaluation of pyrrolidine and pyrazolone derivatives as inhibitors of trypanosomal phosphodiesterase B1 (TbrPDEB1) (2015)
    Details
    Publication Date: 2022-05-25
    Description: Author Posting. © The Author(s), 2015. This is the author's version of the work. It is posted here by permission of Elsevier for personal use, not for redistribution. The definitive version was published in Tetrahedron Letters 56 (2015): 2832-2835, doi:10.1016/j.tetlet.2015.04.061.
    Description: Human African trypanosomiasis (HAT) is a parasitic disease, caused by the protozoan pathogen Trypanosoma brucei, which affects thousands every year and which is in need of new therapeutics. Herein we report the synthesis and assessment of a series of pyrrolidine and pyrazolone derivatives of human phosphodiesterase 4 (hPDE4) inhibitors for the assessment of their activity against the trypanosomal phosphodiesterase TbrPDEB1. The synthesized compounds showed weak potency against TbrPDEB1.
    Description: We acknowledge funding from the National Institutes of Health (R01AI082577).
    Keywords: Trypanosoma brucei ; Phosphodiesterases ; TbrPDEB1 ; Neglected tropical disease
    Repository Name: Woods Hole Open Access Server
    Type: Preprint
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  • 6
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    Target repurposing for neglected diseases (2011)
    Details
    Publication Date: 2022-05-25
    Description: Author Posting. © The Author(s), 2011. This is the author's version of the work. It is posted here by permission of Future Science for personal use, not for redistribution. The definitive version was published in Future Medicinal Chemistry 3 (2011): 1307-1315, doi:10.4155/fmc.11.92.
    Description: Infectious diseases are an enormous burden to global health, and since drug discovery is costly, those infectious diseases that affect the developing world are often not pursued by commercial drug discovery efforts. Therefore, pragmatic means by which new therapeutics can be discovered are needed. One such approach is target repurposing, where pathogen targets are matched with homologous human targets that have been pursued for drug discovery for other indications. In many cases, the medicinal chemistry, structural biology, and biochemistry knowledge around these human targets can be directly repurposed to launch and accelerate new drug discovery efforts against the pathogen targets. This article describes the overarching strategy of target repurposing as a tool for initiating and prosecuting neglected disease drug discovery programs, highlighting this approach with three case studies.
    Description: Support from the National Institutes of Health (R01 AI082577) is gratefully acknowledged.
    Description: 2012-08-01
    Repository Name: Woods Hole Open Access Server
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  • 7
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    Repurposing human PDE4 inhibitors for neglected tropical diseases : design, synthesis and evaluation of cilomilast analogues as Trypanosoma brucei PDEB1 inhibitors (2014)
    Details
    Publication Date: 2022-05-26
    Description: Author Posting. © The Author(s), 2014. This is the author's version of the work. It is posted here by permission of Elsevier for personal use, not for redistribution. The definitive version was published in Bioorganic & Medicinal Chemistry Letters 24 (2014): 4084-4089, doi:10.1016/j.bmcl.2014.07.063.
    Description: A medicinal chemistry exploration of the human phosphodiesterase 4 (hPDE4) inhibitor cilomilast (1) was undertaken in order to identify inhibitors of phosphodiesterase B1 of Trypanosoma brucei (TbrPDEB1). T. brucei is the parasite which causes African sleeping sickness, a neglected tropical disease that affects thousands each year, and TbrPDEB1 has been shown to be an essential target of therapeutic relevance. Noting that 1 is a weak inhibitor of TbrPDEB1, we report the design and synthesis of analogs of this compound, culminating in 12b, a sub-micromolar inhibitor of TbrPDEB1 that shows modest inhibition of T. brucei proliferation.
    Description: This work was funded by the National Institutes of Health (R01AI082577).
    Keywords: Antiprotozoal agents ; Cilomilast ; Phosphodiesterase inhibitors ; TbrPDEB1 Trypanosoma brucei
    Repository Name: Woods Hole Open Access Server
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  • 8
    Electronic Resource
    Electronic Resource
    Chimeric proteins can exceed the sum of their parts: Implications for evolution and protein design (1997)
    [s.l.] : Nature Publishing Company
    Nature biotechnology 15 (1997), S. 439-443 
    Details
    ISSN: 1546-1696
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Process Engineering, Biotechnology, Nutrition Technology
    Notes: [Auszug] Chimeric analogs derived from pairs of homologous proteins routinely exhibit activities found in one or both parents. We describe chimeras of two glycoprotein hormones, human chorionic gonadotropin (hCG) and human follitropin (hFSH), that exhibit activity unique to a third family member, human ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/nbt0597-439
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    Paper (German National Licenses)
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  • 9
    Electronic Resource
    Electronic Resource
    Co-evolution of ligand-receptor pairs (1994)
    [s.l.] : Nature Publishing Group
    Nature 368 (1994), S. 251-255 
    Details
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] TABLE 1 Receptor binding and activities of hormone and chimaera /?-subunits as a function of amino-acid sequences between Cys(lO) and the C terminus Hormone or analogue Sequence between Cys(lO) and C terminus Activity Cys(lO) Cys(ll) Cys(12) LH-RRA FSH-RRA i ...
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1038/368251a0
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  • 10
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    Chimeric proteins can exceed the sum of their parts: Implications for evolution and protein design (1997)
    Springer Nature
    Details
    Publication Date: 1997-05-01
    Print ISSN: 1087-0156
    Electronic ISSN: 1546-1696
    Topics: Biology , Process Engineering, Biotechnology, Nutrition Technology
    Published by Springer Nature
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