Results 41 to 50 of about 70 (70)

Synthesis of Novel Carbocyclic Adenosine Analogues as Inhibitors of Adenosine Kinase

The Journal of Organic Chemistry, 1999
Several new 4‘-amino substituted carbocyclic adenosine analogues (6, 7, 31) were prepared as potential inhibitors of the enzyme adenosine kinase. Three different heterocyclic base moieties (adenine, 8-azaadenine, and pyrazolo[3,4-d]pyrimidine) were incorporated into carbocyclic nucleoside analogues through the use of two different synthetic strategies.
Marlon D. Cowart, Michael J. Bennett, James F. Kerwin   +2 more
openaire   +2 more sources

Production of Adenosine and Nucleoside Analogues by an Exchange Reaction Catalyzed by Adenosine Kinase

1995
We have shown previously that rat liver adenosine kinase can catalyze an exchange reaction between adenosine (Ado) and AMP in the absence of ATP (1). This exchange reaction was potently stimulated by ADP. When measured in the absence of added ADP, the exchange could be due to a slight (0.001 %) contamination by ADP of analytical grade AMP (2).
Françoise Bontemps, Georges Van den Berghe, Mohsine Mimouni   +2 more
openaire   +3 more sources

QSAR STUDIES ON ADENOSINE KINASE INHIBITORS

Medicinal Chemistry Research, 2004
The present study reports QSAR study on adenosine kinase inhibitors pyrrolo[2, 3-d] pyrimidine nucleoside analogous. The equalized electronegativity along with a large pool of topological indices are used for the purpose. The regression analysis has shown that equalized electronegativity is a good parameter which in combination with topological indices
Kamana Singh, Padmakar V. Khadikar, Vijay K. Agrawal   +2 more
openaire   +2 more sources

Pyridopyrimidine analogues as novel adenosine kinase inhibitors

Bioorganic & Medicinal Chemistry Letters, 2001
A novel series of pyridopyrimidine analogues 9 was identified as potent adenosine kinase inhibitors based on the SAR and computational studies. Substitution of the C7 position of the pyridopyrimidino core with C2' substituted pyridino moiety increased the in vivo potency and enhanced oral bioavailability of these adenosine kinase inhibitors.
Mark A. Matulenko, Katharine L. Chu, John R. Koenig, Michael F. Jarvis, Carol T. Wismer, Ki H. Kim, Chih-Hung Lee, Mei Qun Jiang, Steve McGaraughty, Yui Mao, Haixia Yu, Guo Zhu Zheng, Steve Muchmore, Kennan C. Marsh, Richard J. Perner, Elizabeth A. Kowaluk, Karen M. Alexander, Andrew O. Stewart, Joseph P. Mikusa, Shripad S. Bhagwat, John K. Pratt, Arthur Gomtsyan, Kathy L. Kohlhaas   +22 more
openaire   +3 more sources

The influence of inorganic phosphate on the activity of adenosine kinase

Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology, 2000
The enzyme adenosine kinase (AK; EC 2.7.1.20) shows a dependence upon inorganic phosphate (Pi) for activity. The degree of dependence varies among enzyme sources and the pH at which the activity is measured. At physiological pH, recombinant AK from Chinese hamster ovary (CHO) cells and AK from beef liver (BL) show higher affinities for the substrate ...
Bhag Singh, Mary C. Maj, Radhey S. Gupta
openaire   +3 more sources

Structure-Activity Studies on Mammalian Adenosine Kinase

Biochemical and Biophysical Research Communications, 2000
The structure-activity relationship for Chinese hamster adenosine kinase (AK) was examined by making systematic deletions from the N- and C-terminal ends. The first 16 a.a. residues from the N-terminal end, which likely form a random coil, can be deleted without any effect on AK activity or stability.
Bhag Singh, Mary C. Maj, Radhey S. Gupta
openaire   +3 more sources

Adenosine kinase and the control of adenosine concentration in the heart [PDF]

Biochemical Journal, 1985
Eric A. Newsholme, M. N. Fisher
openaire   +1 more source

Adenosine Kinase: Regulation by Substrates, Magnesium and pH

1980
Adenosine kinase phosphorylates many pharmacologically active nucleosides1,2. Several studies have been carried out on the partially purified enzyme from a number of species (see Refs. in 3 and Ref. 4). A striking observation from these reports is the large number of “optimal conditions” reported for the assay of the enzyme from these different sources.
Richard L. Miller, David L. Adamczyk
openaire   +3 more sources

Trends in kinase drug discovery: targets, indications and inhibitor design

Nature Reviews Drug Discovery, 2021
Helgi B Schiöth, Misty M Attwood, Stefan Knapp   +2 more
exaly  

Kinase drug discovery 20 years after imatinib: progress and future directions

Nature Reviews Drug Discovery, 2021
Darren Cross, Pasi A Jänne, Philip Cohen   +2 more
exaly