Azaguanine
Leptospira interrogans serovar icterohaemorrhagiae
Methylthioinosine
Azauridine
Hypoxanthines
Antimetabolites
Pentosyltransferases
Purines
Leptospira
Pharmacology
Centella
Batch Cell Culture Techniques
Commerce
The interchange of goods or commodities, especially on a large scale, between different countries or between populations within the same country. It includes trade (the buying, selling, or exchanging of commodities, whether wholesale or retail) and business (the purchase and sale of goods to make a profit). (From Random House Unabridged Dictionary, 2d ed, p411, p2005 & p283)
Medicine, Chinese Traditional
Microscopy
The use of instrumentation and techniques for visualizing material and details that cannot be seen by the unaided eye. It is usually done by enlarging images, transmitted by light or electron beams, with optical or magnetic lenses that magnify the entire image field. With scanning microscopy, images are generated by collecting output from the specimen in a point-by-point fashion, on a magnified scale, as it is scanned by a narrow beam of light or electrons, a laser, a conductive probe, or a topographical probe.
Dupuytren Contracture
Small Molecule Libraries
Pharmaceutical Preparations
Drug Design
The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.
Fibroblasts
Gout Suppressants
Hyperuricemia
Excessive URIC ACID or urate in blood as defined by its solubility in plasma at 37 degrees C; greater than 0.42mmol per liter (7.0mg/dL) in men or 0.36mmol per liter (6.0mg/dL) in women. This condition is caused by overproduction of uric acid or impaired renal clearance. Hyperuricemia can be acquired, drug-induced or genetically determined (LESCH-NYHAN SYNDROME). It is associated with HYPERTENSION and GOUT.
Gout
Allopurinol
Xanthine Oxidase
Uric Acid
Antibodies, Catalytic
Metals
Antibodies
Haptens
Antibody Specificity
Exosomes
Synaptic Vesicles
Membrane-bound compartments which contain transmitter molecules. Synaptic vesicles are concentrated at presynaptic terminals. They actively sequester transmitter molecules from the cytoplasm. In at least some synapses, transmitter release occurs by fusion of these vesicles with the presynaptic membrane, followed by exocytosis of their contents.
Cardiovascular Diseases
Cytoplasmic Vesicles
Transport Vesicles
Secretory Vesicles
Lipids
A generic term for fats and lipoids, the alcohol-ether-soluble constituents of protoplasm, which are insoluble in water. They comprise the fats, fatty oils, essential oils, waxes, phospholipids, glycolipids, sulfolipids, aminolipids, chromolipids (lipochromes), and fatty acids. (Grant & Hackh's Chemical Dictionary, 5th ed)
Micelles
Particles consisting of aggregates of molecules held loosely together by secondary bonds. The surface of micelles are usually comprised of amphiphatic compounds that are oriented in a way that minimizes the energy of interaction between the micelle and its environment. Liquids that contain large numbers of suspended micelles are referred to as EMULSIONS.
Dioctyl Sulfosuccinic Acid
Drug Carriers
Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers.
Hydrophobic and Hydrophilic Interactions
Polymers
Polyethylene Glycols
Polymers of ETHYLENE OXIDE and water, and their ethers. They vary in consistency from liquid to solid depending on the molecular weight indicated by a number following the name. They are used as SURFACTANTS, dispersing agents, solvents, ointment and suppository bases, vehicles, and tablet excipients. Some specific groups are NONOXYNOLS, OCTOXYNOLS, and POLOXAMERS.
Characterization of the mutational profile of (+)-7R,8S-dihydroxy-9S, 10R-epoxy-7,8,9,10-tetrahydrobenzo[a]pyrene at the hypoxanthine (guanine) phosphoribosyltransferase gene in repair-deficient Chinese hamster V-H1 cells. (1/71)
Earlier studies have shown that the profile of mutations induced by (+)-7R,8S-dihydroxy-9S,10R-epoxy-7,8,9,10-tetrahydrobenzo[a]pyrene (+)-BPDE at the hypoxanthine (guanine) phosphoribosyltransferase (hprt) gene of Chinese hamster V79 cells was dependent on the concentration of (+)-BPDE. In the present study, we examined the effect of the concentration of (+)-BPDE on its mutational profile at the hprt gene in repair-deficient V-H1 cells (a derivative of V79 cells) to explore the role of DNA repair in the dose-dependent mutational profile of (+)-BPDE. Independent hprt mutant clones were isolated after exposing V-H1 cells to dimethylsulfoxide (DMSO) or to low (4-6 nM; 95% cell survival) or high (40-48 nM; 31% cell survival) concentrations of (+)-BPDE in DMSO. The mutation frequencies for the DMSO control and for the low and high concentration groups were 0.1, 2.1 and 32.9 mutant colonies/10(5) survivors, respectively. The profile of mutations at the hprt gene was characterized for 148 (+)-BPDE-induced mutant clones and the results from the present study were compared with those obtained earlier with V79 cells. The data indicated that: (i) V-H1 cells were approximately 9-fold more sensitive to the cytotoxic effects of (+)-BPDE than V79 cells; (ii) the mutation frequency in V-H1 cells was similar to that observed in V79 cells following exposure to similar concentrations of (+)-BPDE; (iii) (+)-BPDE-induced mutations at guanine on the transcribed strand of the hprt gene were common in V-H1 cells but were extraordinarily rare in V79 cells; (iv) (+)-BPDE-induced mutations at adenine on the transcribed strand of the hprt gene were common in both V-H1 and V79 cells; (v) although exposure of V79 cells to different doses of (+)-BPDE resulted in a dose-dependent mutational profile at the hprt gene, this was not observed in V-H1 cells. Our observations indicate a defect in the transcription-coupled repair of (+)-BPDE-DNA adducts in V-H1 cells and that the repair activity deficient in V-H1 cells is essential for the dose-dependent mutational profile observed with (+)-BPDE in V79 cells. (+info)Mutability of different genetic loci in mammalian cells by metabolically activated carcinogenic polycyclic hydrocarbons. (2/71)
The relationship between carcinogenesis and mutagenesis in mammalian cells has been determined with 10 polycyclic hydrocarbons with different degrees of carcinogenicity. Mutagenesis was determined in Chinese hamster cells with genetic markers that affect the surface membrane, nucleic-acid synthesis, and protein synthesis. The mutations were characterized by resistance to ouabain, 8-azaguanine, and temperature. Mutagenesis by the carcinogens required metabolic activation and this was provided by the presence of lethally irradiated metabolizing cells. The degree of carcinogenicity was related to the degree of mutagenicity for all three genetic markers. The most potent carcinogen, 7,12-dimethylbenz[a]anthracene, gave the highest mutagenicity and mutagenicity was obtained with 0.01 mug/ml. Treatment of the cells with aminophylline, which increases polycyclic hydrocarbon metabolism, increased mutagenesis by the carcinogens. It is suggested that such an experimental system with these and other mammalian cells should be useful as a sensitive assay for hazardous environmental chemicals. (+info)Genetic modification of substrate specificity of hypoxanthine phosphoribosyltransferase in Salmonella typhimurium. (3/71)
Salmonella typhimurium strain GP660 (proAB-gpt deletion, purE) lacks guanine phosphoribosyltransferase and hence cannot utilize guanine as a purine source and is resistant to inhibition by 8-azaguanine. Strain GP660 was mutagenized and a derivative strain (GP36) was isolated for utilization of guanine and hypoxanthine, but not xanthine, as purine sources. This alteration was designated sug. The strain was then sensitive to inhibition by 8-azaguanine. Column chromatographic analysis revealed the altered phosphoribosyltransferase peaks for both hypoxanthine and guanine to be located together, in the same position as hypoxanthine phosphoribosyltransferase (hpt gene product) of the wild-type strain. Genetic analysis showed the sug mutation to be allelic with hpt. Therefore sug represented a modification of the substrate specificity of the hpt gene product. (+info)Requirement for cell dispersion prior to selection of induced azaguanine-resistant colonies of Chinese hamster cells. (4/71)
With V79 Chinese hamster cell cultures treated with a mutagen, the maximum frequency of colonies resistant to 8-azaguanine (AZG) was attained when the cells were dispersed after a suitable expression time before adding the selection medium. V79-4 cells were exposed to 500 muM MMS, 7 muM AFAA, or 10 muM MNNG and allowed to multiply before being reseeded at 4 times 10-4 cells/60 mm dish and selected with 10 mu-g/ml AZG. Maximum frequencies of 4 times 10-5, 4 times 10-4, and 2.4 times 10-3 were obtained about 100, 130, and 200 hrs after exposure to MMS, AFAA, and MNNG, respectively. The maximum frequencies following MMS or MNNG treatments were about 10-fold greater than those obtained when induction and selection of AZG-resistant colonies were performed in the same culture dish. The reseeding of treated cells eliminated the possibility of metabolic cooperation within mosaic colonies of wild-type and mutant cells and achieved expression of the induced changes before intercolony crossfeeding reduced the frequency of resistant colonies. - AZG-resistant colonies were selected in medium containing dialyzed fetal bovine serum, and the selection medium replacement were necessary for consistent achievement of background frequencies of resistant colonies near 10-6. Reconstruction experiments with AZG-resistant V79 lines showed that the efficiency of recovery of resistant cells in the selection medium was constant over a range of 0-20 colonies observed/dish. A mixed population of V79 and AZG-resistant cells was also correctly analyzed by the procedure used in mutagenesis studies. (+info)Mechanisms of action of 6-thioguanine, 6-mercaptopurine, and 8-azaguanine. (5/71)
The effects of 6-thioguanine on purine biosynthesis and cell viability have been examined in H.Ep. 2 cells grown in culture. Toxicity is not reversed by aminoimidazolecarboxamide, suggesting that inhibition of purine biosynthesis de novo is not the sole mechanism of toxicity. Also, 6-(methylmercapto)purine ribonucleoside, a potent inhibitor of purine biosynthesis de novo, produces more marked reductions in cellular pools of purines than does 6-thioguanine without killing cells. There is no apparent inhibition by 6-thioguanosine 5'-monophosphate of other enzymes leading to the synthesis of guanosine 5'-triphosphate as determined in whole cells by measurements of radioactive hypoxanthine or guanine incorporation. Inhibition of DNA synthesis by 1 mM thymidine protects cells from 6-mercaptopurine or 6-thioguanine but fails to protect cells from 8-azaguanine toxicity. On the other hand, inhibition of RNA synthesis by 6-azauridine plus deoxycytidine protects cells against 8-azaguanine but does not protect against 6-thioguanine or 6-mercaptopurine toxicity. In agreement with the in vitro data, arabinosylcytosine (a potent inhibitor of DNA synthesis) fails to protect mice against 8-azaguanine but has previously been shown to protect mice from 6-mercaptopurine or 6-thioguanine toxicity. The results support the hypotheses of others that incorporation into DNA (as 6-thioguanine nucleotide) is a mechanism of toxicity for these thiopurines, whereas 8-azaguanine is toxic due to its incorporation into RNA. (+info)Mutant enrichment in the colonial alga, Eudorina elegans. (6/71)
An enrichment procedure has been developed that results in at least a 200 X increase in mutation frequency in the colonial alga, Eudorina elegans. A period of nitrogen starvation followed by treatment with 8-azaguanine results in the death of wild-type cells and the maintenance of mutants. N'-nitro-N-nitro-soguanidine-induced acetate, p-aminobenzoic acid and reduced nitrogen requiring mutants have been isolated by this procedure. (+info)Characterisation of methionine adenosyltransferase from Mycobacterium smegmatis and M. tuberculosis. (7/71)
BACKGROUND: Tuberculosis remains a serious world-wide health threat which requires the characterisation of novel drug targets for the development of future antimycobacterials. One of the key obstacles in the definition of new targets is the large variety of metabolic alterations that occur between cells in the active growth and chronic/dormant phases of tuberculosis. The ideal biochemical target should be active in both growth phases. Methionine adenosyltransferase, which catalyses the formation of S-adenosylmethionine from methionine and ATP, is involved in polyamine biosynthesis during active growth and is also required for the methylation and cyclopropylation of mycolipids necessary for survival in the chronic phase. RESULTS: The gene encoding methionine adenosyltransferase has been cloned from Mycobacterium tuberculosis and the model organism M. smegmatis. Both enzymes retained all amino acids known to be involved in catalysing the reaction. While the M. smegmatis enzyme could be functionally expressed, the M. tuberculosis homologue was insoluble and inactive under a large variety of expression conditions. For the M. smegmatis enzyme, the Vmax for S-adenosylmethionine formation was 1.30 micromol/min/mg protein and the Km for methionine and ATP was 288 microM and 76 microM respectively. In addition, the enzyme was competitively inhibited by 8-azaguanine and azathioprine with a Ki of 4.7 mM and 3.7 mM respectively. Azathioprine inhibited the in vitro growth of M. smegmatis with a minimal inhibitory concentration (MIC) of 500 microM, while the MIC for 8-azaguanine was >1.0 mM. CONCLUSION: The methionine adenosyltransferase from both organisms had a primary structure very similar those previously characterised in other prokaryotic and eukaryotic organisms. The kinetic properties of the M. smegmatis enzyme were also similar to known prokaryotic methionine adenosyltransferases. Inhibition of the enzyme by 8-azaguanine and azathioprine provides a starting point for the synthesis of higher affinity purine-based inhibitors. (+info)Inhibition of protein syntheses during meiosis and its bearing on intracellular regulation. (8/71)
Several parameters of meiosis have been studied in cultured anthers of Trillium erectum. The accessibility of labeled substrates to meiotic cells and the fate of these substrates in relation to meiotic stage have been determined. Evidence has been adduced for the synthesis of RNA and protein during the meiotic cycle well after chromosome duplication. The effect of interfering with systems directly or indirectly connected with protein formation has been studied by means of chloramphenicol, 8-azaguanine, 5-methyltryptophan, and ethionine. Administration of these reagents at different intervals in the cycle elicits correspondingly different responses thereby indicating a periodicity in the activities of different systems. The following processes have been shown to be affected in these experiments: chromosome segregation, chromosome morphology, cytokinesis, wall synthesis, and enzyme appearance. The possibility of experimentally altering the normal sequence of events has also been shown. (+info)
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Guanine4
- The guanine analog, 8-azaguanine, has been shown to possess carcinostatic properties against transplantable tumors in experimental animals (7, 8). (semanticscholar.org)
- Some earlier drug-resistant cell lines were developed in the 1950 and 1960s using in vivo mouse models, including models resistant to methotrexate ( 2 , 3 ), vinblastine, terephthalanilide ( 4 ), and the guanine analog, 8-azaguanine ( 5 ). (frontiersin.org)
- It has been postulated that guanine is essential for the growth of neoplastic cells and that the growth of certain lymphosarcomas may be inhibited by the administration of 8-azaguanine, a guanine analog. (aacrjournals.org)
- The carbocyclic 2′,3/-didehydro-2′,3′-dideoxy analogues of guanine (7a) and 2,6-diaminopurine (8a), and 8-azaguanine (10a) and 8-aza-2,6-diaminopurine (11a) were prepared from 6a and 9a, respectively. (umn.edu)
Purine analogue2
- 8-Azaguanine was the first purine analogue discovered to inhibit experimental tumors in mice. (wikipedia.org)
- The purine analogue, 8-azaguanine, was added to cultures of the parasporal crystal-forming organism Bacillus cereus var. (rupress.org)
Resistant7
- I. Selection and characterization of mutations auxotrophic for L-glutamine or resistant to 8-azaguanine in Chinese hamster cells in vitro. (atcc.org)
- 1980 ). X-ray induction of 8-azaguanine-resistant mutants in synchronous Chinese hamster ovary cells. (biologists.org)
- Post-DST PBL were fused with an azaguanine-resistant mutant of a human T cell leukemia cell line, CCRF-CEM(AG). (elsevier.com)
- Partially resistant to azaguanine. (phe-culturecollections.org.uk)
- The cells are resistant to 8-azaguanine and are HAT sensitive. (addexbio.com)
- This cell line has been shown to be resistant to 8-azaguanine. (hsanmartino.it)
- The line is resistant to 0.1 mM 8-azaguanine and die in HAT medium. (xiangbio.com)
Nucleic Acids1
- Chantrenne H, Devreux S., Effects of 8-azaguanine on the synthesis of protein and nucleic acids in Bacillus cereus, Nature. (wikipedia.org)
Mutants1
- 8-azaguanine mutants may be cloned out or mutagenized for HAT sensitive cultures. (atcc.org)
Amethopterin1
- In comparative tests, furthermore, the anti-lymphoma serums acted more powerfully upon the lymphoma cells in vivo than did such chemotherapeutic agents as amethopterin, azaguanine, ethionine, azaserine, and 6-mercaptopurine, given singly or in various combinations in maximal tolerated amounts, though their effects were not so powerful as those exerted by normal guinea pig serum on lymphoma cells of two types that are susceptible to its action in vivo . (rupress.org)
Growth1
- Effect of 8-azaguanine on the transition from vegetative growth to presporulation in Bacillus cereus. (semanticscholar.org)
Bacillus2
- The messenger activity of total RNA from normal and 8-azaguanine-treated Bacillus cereus cultures was measured by the stimulation of amino acid incorporation into proteins in the preincubated S-30 Escherichia coli system. (aspetjournals.org)
- The Effect of 8-Azaguanine on Spore and Parasporal Protein Formation in Bacillus cereus var. (rupress.org)
Incorporation1
- RNA from 8-azaguanine-treated cells enhanced the incorporation of various amino acids into proteins to a greater extent than did RNA from normal cells. (aspetjournals.org)
Enzyme3
- The greater metabolic clearance of cabazitaxel is enhanced by the concurrent administration are of phenobarbitone, 8 - azaguanine, and other drugs now that induce hepatic enzyme can function. (rosesturn.com)
- In addition, the enzyme was competitively inhibited by 8-azaguanine and azathioprine with a Ki of 4.7 mM and 3.7 mM respectively. (beds.ac.uk)
- Inhibition of the enzyme by 8-azaguanine and azathioprine provides a starting point for the synthesis of higher affinity purine-based inhibitors. (beds.ac.uk)
Resistance1
- L. Larizza, G. Simoni, M. Stefanini, and L. De Carli, Spontaneous and Griseofulvin induced segregation for 8-Azaguanine resistance in hybrids from a human heteroploid line. (springer.com)
Myeloma6
- I am looking into protocols for making hybridomas and notice that some people grow their myeloma cells in 8-azaguanine and other don't. (cellculturedish.com)
- Some people grow their myeloma cells (Sp2/0, Sp2/0-ag14, NS-0 and NS-1 cells for example) in 8-azaguanine or 6-thioguanineThe reason for this is to ensure that the cell line is 8-azaguanine or 6-thioguanine and HGPRT negative. (cellculturedish.com)
- I suggest that the use of 8-azaguanine or 6-thioguanine at least some of the time is important to ensure the correct myeloma phenotype is maintained and only fused cells ultimately survive. (cellculturedish.com)
- Myeloma cells are immortalized cells that are refined with 8 azaguanine to ensure their sensitivity to the hypoxanthine aminopterin-thymidine (HAT) choice medium utilized after cell combination. (palawanboard.com)
- A week before cell fusion, myeloma cells are developed in 8-azaguanine. (palawanboard.com)
- Institute for Laboratory Animal Research National Research Council, 1999)Step 2: Preparation of Myeloma CellsMyeloma cells are immortalized cells that are refined with 8 azaguanine to ensure their sensitivity to the hypoxanthine aminopterin-thymidine (HAT) choice medium utilized after cell combination. (savedelicious.com)
Cells1
- However, as before, the 8-azaguanine was incorporated into both the acid soluble and RNA of the cells, but not into these fractions of the spores ultimately formed. (rupress.org)
Leukemia1
- Response of patients with leukemia to 8-azaguanine" (PDF). (wikipedia.org)
Effect1
- The effect of 4-amino-5-imidazolecarboxamide on the toxicity of 8-azaguanine. (semanticscholar.org)
Description1
- Useage: It is a type of raw pharmaceutical material and mainly used for Anti-tumor or interleukin (2)8-Azaguanine : CAS: 134-58-7 Molecula Fomula: C4H4N6O Molecula Weight : 152.12 Description: colorless crystallines Useage:It is a type of raw pha. (iraqitradecenter.com)
Laboratory1
- azaguanine a purine antagonist first synthesized in the laboratory and later shown to be identical to an antibiotic synthesized by Streptomyces spectabalis. (damasgate.com)
Normal1
- Enzymatic deamination of 8-azaguanine in normal and neoplastic tissues. (semanticscholar.org)
Materials1
- For the habituation period the Azaguanine-8 pipe was filled up with home bedding materials 20 cm from the very best. (thiazovivin.com)
Human1
- This work reports the structure of human PNP in complex with guanosine (at 2.80 Å resolution), 3′-deoxyguanosine (at 2.86 Å resolution) and 8-azaguanine (at 2.85 Å resolution). (iucr.org)