Nucleoside Phosphonic Acids in Thymidine Phosphorylase Inhibition: Structure - Activity Relationship
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چکیده
منابع مشابه
Inhibition and structure of Toxoplasma gondii purine nucleoside phosphorylase.
The intracellular pathogen Toxoplasma gondii is a purine auxotroph that relies on purine salvage for proliferation. We have optimized T. gondii purine nucleoside phosphorylase (TgPNP) stability and crystallized TgPNP with phosphate and immucillin-H, a transition-state analogue that has high affinity for the enzyme. Immucillin-H bound to TgPNP with a dissociation constant of 370 pM, the highest ...
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INHIBITION AND STRUCTURE OF TOXOPLASMA GONDII PURINE 1 NUCLEOSIDE PHOSPHORYLASE 2 3 4 Running title: Toxoplasma gondii purine nucleoside phosphorylase 5 6 Teraya M. Donaldson, María B. Cassera, Meng-Chiao Ho, Chenyang Zhan, 7 Emilio F. Merino, Gary B. Evans, Peter C. Tyler, Steven C. Almo, Vern L. 8 Schramm, and Kami Kim d, # 9 10 From the Departments of Microbiology and Immunology, Biochemistr...
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The purine salvage pathway of Anopheles gambiae, a mosquito that transmits malaria, has been identified in genome searches on the basis of sequence homology with characterized enzymes. Purine nucleoside phosphorylase (PNP) is a target for the development of therapeutic agents in humans and purine auxotrophs, including malarial parasites. The PNP from Anopheles gambiae (AgPNP) was expressed in E...
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Thymidine phosphorylase (TPase) is one of the key enzymes involved in the pyrimidine nucleoside salvage pathway. However, TPase also stimulates angiogenesis, and its expression correlates well with microvessel density and metastasis in a variety of human tumors. We have shown recently that 5'-O-trityl-inosine (KIN59) allosterically inhibits TPase enzymatic activity. KIN59 also inhibits TPase-in...
متن کاملAntiproliferative activity of purine nucleoside phosphorylase multisubstrate analogue inhibitors containing difluoromethylene phosphonic acid against leukaemia and lymphoma cells.
Potent inhibitors of purine nucleoside phosphorylase (PNP) are expected to act as selective agents against T-cell tumours. Five compounds with guanine, three with hypoxanthine, and five with 9-deazaguanine, all connected by a linker with difluoromethylene phosphonic acid, were studied on their inhibitory potential against human and calf PNPs. Antiproliferative activity of these analogues agains...
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ژورنال
عنوان ژورنال: Nucleic Acids Symposium Series
سال: 2008
ISSN: 0261-3166,1746-8272
DOI: 10.1093/nass/nrn336