Adenosine deaminase inhibitors. Medical search

Drugs that inhibit ADENOSINE DEAMINASE activity.

A ribonucleoside antibiotic synergist and adenosine deaminase inhibitor isolated from Nocardia interforma and Streptomyces kaniharaensis. It is proposed as an antineoplastic synergist and immunosuppressant.

A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.

An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.

Catalyze the hydrolysis of nucleosides with the elimination of ammonia.

A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.

Nucleosides in which the purine or pyrimidine base is combined with ribose. (Dorland, 28th ed)

Adenosine molecules which can be substituted in any position, but are lacking one hydroxyl group in the ribose part of the molecule.

An enzyme that catalyzes the formation of ADP plus AMP from adenosine plus ATP. It can serve as a salvage mechanism for returning adenosine to nucleic acids. EC 2.7.1.20.

A purine base and a fundamental unit of ADENINE NUCLEOTIDES.

A purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It is an intermediate in the degradation of purines and purine nucleosides to uric acid and in pathways of purine salvage. It also occurs in the anticodon of certain transfer RNA molecules. (Dorland, 28th ed)

An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.

An inhibitor of nucleotide metabolism.

A nucleoside antibiotic isolated from Streptomyces antibioticus. It has some antineoplastic properties and has broad spectrum activity against DNA viruses in cell cultures and significant antiviral activity against infections caused by a variety of viruses such as the herpes viruses, the VACCINIA VIRUS and varicella zoster virus.

An enzyme which catalyzes the catabolism of S-ADENOSYLHOMOCYSTEINE to ADENOSINE and HOMOCYSTEINE. It may play a role in regulating the concentration of intracellular adenosylhomocysteine.

A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).

An enzyme that catalyzes the deamination of AMP to IMP. EC 3.5.4.6.

The removal of an amino group (NH2) from a chemical compound.

A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.

A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.

An enzyme that catalyzes the deamination of cytidine, forming uridine. EC 3.5.4.5.

A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.

An enzyme which catalyzes the deamination of CYTOSINE resulting in the formation of URACIL. It can also act on 5-methylcytosine to form THYMIDINE.

Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.

An enzyme that catalyzes the hydrolytic deamination of deoxycytidylic acid to deoxyuridylic acid and ammonia. It plays an important role in the regulation of the pool of deoxynucleotides in higher organisms. The enzyme also acts on some 5-substituted deoxycytidylic acids. EC 3.5.4.12.

A subclass of adenosine A2 receptors found in the CECUM, the COLON, the BLADDER, and a variety of other tissues. It is generally considered to be a low affinity receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.

An enzyme that catalyzes the deamination of guanine to form xanthine. EC 3.5.4.3.

A common genetically determined, chronic, inflammatory skin disease characterized by rounded erythematous, dry, scaling patches. The lesions have a predilection for nails, scalp, genitalia, extensor surfaces, and the lumbosacral region. Accelerated epidermopoiesis is considered to be the fundamental pathologic feature in psoriasis.

Lymphocytes responsible for cell-mediated immunity. Two types have been identified - cytotoxic (T-LYMPHOCYTES, CYTOTOXIC) and helper T-lymphocytes (T-LYMPHOCYTES, HELPER-INDUCER). They are formed when lymphocytes circulate through the THYMUS GLAND and differentiate to thymocytes. When exposed to an antigen, they divide rapidly and produce large numbers of new T cells sensitized to that antigen.

The external, nonvascular layer of the skin. It is made up, from within outward, of five layers of EPITHELIUM: (1) basal layer (stratum basale epidermidis); (2) spinous layer (stratum spinosum epidermidis); (3) granular layer (stratum granulosum epidermidis); (4) clear layer (stratum lucidum epidermidis); and (5) horny layer (stratum corneum epidermidis).

A plant genus of the family BORAGINACEAE. Members contain lithospermans and lithospermic acid.

A genus of PSYCHODIDAE which functions as the vector of a number of pathogenic organisms, including LEISHMANIA DONOVANI; LEISHMANIA TROPICA; Bartonella bacilliformis, and the Pappataci fever virus (SANDFLY FEVER NAPLES VIRUS).

Small, hairy, moth-like flies which are of considerable public health importance as vectors of certain pathogenic organisms. Important disease-related genera are PHLEBOTOMUS, Lutzomyia, and Sergentomyia.

A genus of mosquitoes (CULICIDAE) commonly found in tropical regions. Species of this genus are vectors for ST. LOUIS ENCEPHALITIS as well as many other diseases of man and domestic and wild animals.

Proteins found in any species of insect.

A calcium-activated enzyme that catalyzes the hydrolysis of ATP to yield AMP and orthophosphate. It can also act on ADP and other nucleoside triphosphates and diphosphates. EC 3.6.1.5.

Glands that secrete SALIVA in the MOUTH. There are three pairs of salivary glands (PAROTID GLAND; SUBLINGUAL GLAND; SUBMANDIBULAR GLAND).

A group of lymphomas exhibiting clonal expansion of malignant T-lymphocytes arrested at varying stages of differentiation as well as malignant infiltration of the skin. MYCOSIS FUNGOIDES; SEZARY SYNDROME; LYMPHOMATOID PAPULOSIS; and PRIMARY CUTANEOUS ANAPLASTIC LARGE CELL LYMPHOMA are the best characterized of these disorders.

A group of heterogeneous lymphoid tumors representing malignant transformations of T-lymphocytes.

A form of cutaneous T-cell lymphoma manifested by generalized exfoliative ERYTHRODERMA; PRURITUS; peripheral lymphadenopathy, and abnormal hyperchromatic mononuclear (cerebriform) cells in the skin, LYMPH NODES, and peripheral blood (Sezary cells).

A chronic, malignant T-cell lymphoma of the skin. In the late stages, the LYMPH NODES and viscera are affected.

A general term for various neoplastic diseases of the lymphoid tissue.

Substances that inhibit or prevent the proliferation of NEOPLASMS.

Tumors or cancer of the SKIN.

A chromatographic technique that utilizes the ability of biological molecules to bind to certain ligands specifically and reversibly. It is used in protein biochemistry. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)

Occupations of medical personnel who are not physicians, and are qualified by special training and, frequently, by licensure to work in supporting roles in the health care field. These occupations include, but are not limited to, medical technology, physical therapy, physician assistant, etc.

Development of a library collection, including the determination and coordination of selection policy, assessment of needs of users and potential users, collection use studies, collection evaluation, identification of collection needs, selection of materials, planning for resource sharing, collection maintenance and weeding, and budgeting.

Books used in the study of a subject that contain a systematic presentation of the principles and vocabulary of a subject.

Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.

Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.

The extracellular versus intracellular mechanisms of inhibition of TCR-triggered activation in thymocytes by adenosine under conditions of inhibited adenosine deaminase. (1/193)

The absence or low levels of adenosine deaminase (ADA) in humans result in severe combined immunodeficiency (SCID), which is characterized by hypoplastic thymus, T lymphocyte depletion and autoimmunity. Deficiency of ADA causes increased levels of both intracellular and extracellular adenosine, although only the intracellular lymphotoxicity of accumulated adenosine is considered in the pathogenesis of ADA SCID. It is shown that extracellular but not intracellular adenosine selectively inhibits TCR-triggered up-regulation of activation markers and apoptotic events in thymocytes under conditions of ADA deficiency. The effects of intracellular adenosine are dissociated from effects of extracellular adenosine in experiments using an adenosine transporter blocker. We found that prevention of toxicity of intracellular adenosine led to survival of TCR-cross-linked thymocytes in long-term (4 days) assays, but it was not sufficient for normal T cell differentiation under conditions of inhibited ADA. Surviving TCR-cross-linked thymocytes had a non-activated phenotype due to extracellular adenosine-mediated, TCR-antagonizing signaling. Taken together the data suggest that both intracellular toxicity and signaling by extracellular adenosine may contribute to pathogenesis of ADA SCID. Accordingly, extracellular adenosine may act on thymocytes, which survived intracellular toxicity of adenosine during ADA deficiency by counteracting TCR signaling. This, in turn, could lead to failure of positive and negative selection of thymocytes, and to additional elimination of thymocytes or autoimmunity of surviving T cells. (+info)

Nucleotide pool imbalance and adenosine deaminase deficiency induce alterations of N-region insertions during V(D)J recombination. (2/193)

Template-independent nucleotide additions (N regions) generated at sites of V(D)J recombination by terminal deoxynucleotidyl transferase (TdT) increase the diversity of antigen receptors. Two inborn errors of purine metabolism, deficiencies of adenosine deaminase (ADA) and purine nucleoside phosphorylase (PNP), result in defective lymphoid development and aberrant pools of 2'-deoxynucleotides that are substrates for TdT in lymphoid precursors. We have asked whether selective increases in dATP or dGTP pools result in altered N regions in an extrachromosomal substrate transfected into T-cell or pre-B-cell lines. Exposure of the transfected cells to 2'-deoxyadenosine and an ADA inhibitor increased the dATP pool and resulted in a marked increase in A-T insertions at recombination junctions, with an overall decreased frequency of V(D)J recombination. Sequence analysis of VH-DH-JH junctions from the IgM locus in B-cell lines from ADA-deficient patients demonstrated an increase in A-T insertions equivalent to that found in the transfected cells. In contrast, elevation of dGTP pools, as would occur in PNP deficiency, did not alter the already rich G-C content of N regions. We conclude that the frequency of V(D)J recombination and the composition of N-insertions are influenced by increases in dATP levels, potentially leading to alterations in antigen receptors and aberrant lymphoid development. Alterations in N-region insertions may contribute to the B-cell dysfunction associated with ADA deficiency. (+info)

Quantification of extracellular and intracellular adenosine production: understanding the transmembranous concentration gradient. (3/193)

BACKGROUND: Inhibitors of adenosine membrane transport cause vasodilation and enhance the plasma adenosine concentration. However, it is unclear why the plasma adenosine concentration rises rather than falls when membrane transport is inhibited. We tested the hypothesis that the cytosolic adenosine concentration exceeds the interstitial concentration under well-oxygenated conditions. METHODS AND RESULTS: In isolated, isovolumically working guinea pig hearts (n=50), the release rate of adenosine and accumulation of S-adenosylhomocysteine (after 20 minutes of 200 micromol/L homocysteine), a measure of the free cytosolic adenosine concentration, were determined in the absence and presence of specific and powerful blockers of adenosine membrane transport (nitrobenzylthioinosine 1 micromol/L), adenosine deaminase (erythro-9-hydroxy-nonyl-adenine 5 micromol/L), and adenosine kinase (iodotubericidine 10 micromol/L). Data analysis with a distributed multicompartment model revealed a total cardiac adenosine production rate of 2294 pmol. min-1. g-1, of which 8% was produced in the extracellular region. Because of a high rate of intracellular metabolism, however, 70.3% of extracellularly produced adenosine was taken up into cellular regions, an effect that was effectively eliminated by membrane transport block. The resulting approximately 2.8-fold increase of the interstitial adenosine concentration evoked near-maximal coronary dilation. CONCLUSIONS: We rejected the hypothesis that the cytosolic adenosine concentration exceeds the interstitial. Rather, there is significant extracellular production, and the parenchymal cell represents a sink, not a source, for adenosine under well-oxygenated conditions. (+info)

Diinosine pentaphosphate (IP5I) is a potent antagonist at recombinant rat P2X1 receptors. (4/193)

1. The antagonist activity of a series of diinosine polyphosphates (IpnI, where n=3, 4, 5) was assessed against ATP-activated inward currents at rat P2X(1-4) receptors expressed in Xenopus oocytes and studied under voltage-clamp conditions. 2. Diinosine polyphosphates were prepared by the enzymatic degradation of their corresponding diadenosine polyphosphates (e.g., Ap5A into Ip5I) using 5'-adenylic deaminase, and purified using reverse-phase chromatography. 3. Against ATP-responses at rP2X1 receptors, the potency order for antagonism was (pIC50): Ip5I (8.5)>Ip4I (6.3)>Ip3I (>4.5). Ip5I (10-100 nM) caused a concentration-dependent rightwards displacement of the ATP concentration-response curve without reducing the maximum ATP effect. However, the Schild plot was non-linear which indicated Ip5I is not a competitive antagonist. Blockade by micromolar concentrations of Ip5I was not surmountable. Ip4I also behaved as a non-surmountable antagonist. 4. Against ATP-responses at rP2X3 receptors, the potency order for antagonism was (pIC50): Ip4I (6. 0)>Ip5I (5.6)>Ip3I (>4.5). Blockade by Ip4I (pA2, 6.75) and Ip5I (pA2, 6.27) was surmountable at micromolar concentrations. 5. Diinosine polyphosphates failed to inhibit ATP-responses at rP2X2 receptors, whereas agonist responses at rP2X4 were reversibly potentiated by Ip4I and Ip5I. None of the parent diadenosine polyphosphates behave as antagonists at rP2X1 - 4 receptors. 6. Thus, Ip5I acted as a potent and relatively-selective antagonist at the rP2X1 receptor. This dinucleotide pentaphosphate represents a high-affinity antagonist for the P2X1 receptor, at which it acts in a competitive manner at low (100 nM) concentrations. (+info)

The anticonvulsant BW534U87 depresses epileptiform activity in rat hippocampal slices by an adenosine-dependent mechanism and through inhibition of voltage-gated Na+ channels. (5/193)

1. The cellular and molecular actions of BW534U87 were studied using intracellular and extracellular recordings from the CA1 region of rat hippocampal slices and whole-cell voltage-clamp recordings of recombinant human brain type IIA Na+ channels expressed in Chinese hamster ovary (CHO) cells. 2. Normal excitatory and inhibitory postsynaptic potentials evoked in hippocampal slices were unaffected by BW534U87 or the adenosine deaminase inhibitor EHNA. However, epileptiform activity was depressed by BW534U87 (50 micronM) and this inhibition was reversed by the adenosine receptor antagonist 8-phenyl theophylline (8-PT, 30 micronM). EHNA (10 micronM) mimicked the effects of BW534U87. Furthermore, BW534U87 enhanced the inhibitory effects of exogenous adenosine on evoked synaptic potentials. BW534U87 (50 micronM) also voltage- and use-dependently inhibited action potentials elicited by current injection, independent of the adenosine system, since it was not affected by 8-PT. 3. In CHO cells expressing the recombinant human brain Na+ channel, BW534U87 produced a concentration- and voltage-dependent inhibition of Na+ currents with a half-maximal inhibitory concentration of 10 micronM at a Vh of -60 mV. Use-dependent inhibition was evident at high-frequencies (20x20 ms pulse train at 10 Hz). 4 In conclusion, BW534U87 blocks hippocampal epileptiform activity by a dual mechanism. The first action is similar to that produced by EHNA and is dependent on endogenous adenosine probably by inhibition of adenosine deaminase. Secondly, BW534U87 directly inhibits voltage-gated Na+ channels in a voltage- and frequency-dependent manner. Both actions of BW534U87 are activity-dependent and may synergistically contribute to its overall anticonvulsant effects in animal models of epilepsy. (+info)

A normal level of adenosine deaminase activity in the red cell lysates of carriers and patients with severe combined immunodeficiency disease. (6/193)

The red cell lysates of two children with severe combined immunodeficiency disease (SCID) exhibited a virtually total absence of adenosine deaminase (adenosine aminohydrolase, EC 3.5.4.4) when standard volumes were assayed. Under these conditions the parents exhibited depressed specific activity except for one mother, whose lysate showed a normal value for activity. Upon storage of the lysate at 4 degrees, a significant amount of activity appeared in one of the SCID children, and the activity of the heterozygous carriers was stimulated. With the use of a sensitive spectrophotometric assay based on conversion of inosine to uric acid, it was shown that the specific enzymatic activity in each of the SCID patients increased progressively as the volume of lysate assayed was lowered. With the smallest amount of lysate this specific activity was in the normal range. Similarly, the specific activity of each of the parents' lysates increased to the level of normal (or, in one case, about twice normal) as smaller volumes were assayed. The activity in the SCID patient was inhibitable by 2-fluoroadenosine and N6-methyladenosine, known competitive inhibitors of human red cell adenosine deaminase. The lysate from the SCID patient was also shown to inhibit adenosine deaminase partially purified from a normal individual. The results are interpreted in terms of a genetically programmed production of an adenosine deaminase inhibitor in at least one variant of the severe combined immunodeficiency disease. (+info)

Age-related changes in A(1)-adenosine receptor-mediated bradycardia. (7/193)

The impact of age on functional sensitivity to A(1)-adenosine receptor activation was studied in Langendorff-perfused hearts from young (1-2 mo) and old (12-18 mo) male Wistar rats. Adenosine mediated bradycardia in young and old hearts, with sensitivity enhanced approximately 10-fold in old [negative logarithm of EC(50) (pEC(50)) = 4.56 +/- 0.11] versus young hearts (pEC(50) = 3.70 +/- 0. 09). Alternatively, the nonmetabolized A(1) agonists N(6)-cyclohexyladenosine and (R)-N(6)-phenylisopropyladenosine were equipotent in young (pEC(50) = 7.43 +/- 0.12 and 6.61 +/- 0.19, respectively) and old hearts (pEC(50) = 7.07 +/- 0.10 and 6.80 +/- 0. 11, respectively), suggesting a role for uptake and/or catabolism in age-related changes in adenosine sensitivity. In support of this suggestion, [(3)H]-adenosine uptake was approximately twofold greater in young than in old hearts (from 3-100 microM adenosine). However, although inhibition of adenosine deaminase and adenosine transport with 10 microM erythro-9-(2-hydroxy-3-nonyl)adenine hydrochloride and 10 microM S-(4-nitrobenzyl)-6-thioinosine increased adenosine sensitivity three- to fourfold, it failed to abolish the sensitivity difference in old (pEC(50) = 4.95 +/- 0.08) versus young (pEC(50) = 4.29 +/- 0.13) hearts. Data indicate that 1) age increases functional A(1) receptor sensitivity to adenosine without altering the sensitivity of the A(1) receptor itself, and 2) age impairs adenosine transport and/or catabolism, but this does not explain differing functional sensitivity to adenosine. This increased functional sensitivity to adenosine may have physiological significance in the older heart. (+info)

Adenosine-mediated killing of cultured epithelial cancer cells. (8/193)

Because micromolar concentrations of adenosine (Ado) have been documented recently in the interstitial fluid of carcinomas growing in animals, we examined the effects of low concentrations of Ado on the growth of cultured human carcinoma cells. Ado alone had little effect upon cell growth. In the presence of one of a number of Ado deaminase (ADA) inhibitors, Ado led to significant growth inhibition of all cell lines tested. Similar effects were found when ATP, ADP, or AMP was substituted for Ado. Surprisingly, the ADA inhibitor coformycin (CF) had a much greater potentiating effect than did 2'-deoxycoformycin (DCF), although DCF is a more potent ADA inhibitor. The growth inhibition of the Ado/CF combination was not abrogated by pyrimidines or caffeine, a nonspecific Ado receptor blocker. Toxicity was prevented by the addition of the Ado transport inhibitor dipyridamole or the Ado kinase inhibitor 5'-amino 5'-deoxyadenosine. S-Adenosylhomocysteine hydrolase is not involved because neither homocysteine thiolactone nor an S-adenosylhomocysteine hydrolase inhibitor (adenosine dialdehyde) potentiated toxicity of the Ado/CF combination. Unexpectedly, substitution of 2'-deoxyadenosine (the toxic moiety in congenital ADA deficiency) for Ado, did not lead to equivalent toxicity. The Ado/CF combination inhibited DNA synthesis and brought about morphological changes consistent with apoptosis. Together, these findings indicate that the Ado-mediated killing proceeds via an intracellular route that requires the action of Ado kinase. The enhanced cofactor activity of CF may be attributable to its being a more potent inhibitor of AMP deaminase than is DCF. (+info)

... then adenosine deaminase creates inosine Alternatively, AMP deaminase creates inosinic acid, then a nucleotidase creates ... Purine synthesis inhibitors inhibit the proliferation of cells, especially leukocytes. These inhibitors include azathioprine, ... Some of the diseases are: Severe immunodeficiency by loss of adenosine deaminase. Hyperuricemia and Lesch-Nyhan syndrome by the ... So IMP, GMP and AMP are inhibitors while PRPP is an activator. Between the formation of 5'-phosphoribosyl, aminoimidazole and ...

https://en.wikipedia.org/wiki/Purine_metabolism

EHNA is also a very potent adenosine deaminase inhibitor with an IC50 ~2 nM. This dual inhibition would lead to the ... Theoretically, this problem can be resolved if the effect of adenosine accumulated by EHNA, a result of adenosine deaminase ... "Adenosine deaminase inhibition enhances the inotropic response mediated by A1 adenosine receptor in hyperthyroid guinea pig ... Although EHNA potently inhibits adenosine deaminase, it has been successfully used with the proper controls as a tool to probe ...

https://en.wikipedia.org/wiki/Phosphodiesterase_2

Note: adenosine is first metabolized to inosine via the enzyme adenosine deaminase. Nucleoside phosphorylase is an enzyme which ... Attempts are being made to develop an inhibitor for the enzyme for use in cancer chemotherapy. This protein may use the ... PNPase, together with adenosine deaminase (ADA), serves a key role in purine catabolism, referred to as the salvage pathway. ... Adenosine uses the enzyme adenosine kinase, which is a very important enzyme in the cell. ...

https://en.wikipedia.org/wiki/Purine_nucleoside_phosphorylase

... is a potent adenosine deaminase inhibitor, which also acts as a phosphodiesterase inhibitor that selectively inhibits ...

https://en.wikipedia.org/wiki/EHNA

... (DPP4), also known as adenosine deaminase complexing protein 2 or CD26 (cluster of differentiation 26) ... The MEROPS online database for peptidases and their inhibitors: S09.003. *Dipeptidyl-Peptidase+IV at the US National Library of ... Kameoka J, Tanaka T, Nojima Y, Schlossman SF, Morimoto C (Jul 1993). "Direct association of adenosine deaminase with a T cell ... DPP-4 also binds the enzyme adenosine deaminase specifically and with high affinity. The significance of this interaction has ...

https://en.wikipedia.org/wiki/Dipeptidyl_peptidase-4

Patients with adenosine deaminase deficiency (ADA) tend to have elevated intracellular dATP concentrations because adenosine ... since dATP acts as a noncompetitive inhibitor for the DNA synthesis enzyme ribonucleotide reductase. ... Adenosine triphosphate (ATP) Adenosine deaminase deficiency (ADA) Dilated cardiomyopathy (DCM) Ribonucleotide reductases (RNR) ... deaminase normally curbs adenosine levels by converting it into inosine. Deficiency of the enzyme adenosine deaminase is known ...

https://en.wikipedia.org/wiki/Deoxyadenosine_triphosphate

AdoHcyase is significantly associated with adenosine deaminase deficiency, which classically manifests in severe combine ... a potent inhibitor of methyl transfer reactions. This protein may use the morpheein model of allosteric regulation. Hu Y, ... deoxyadenosine in adenosine deaminase-deficient patients". J Clin Invest. 63 (4): 807-811. doi:10.1172/JCI109367. PMC 372019. ... responsible for the reversible hydration of S-adenosyl-L-homocysteine into adenosine and homocysteine. AdoHcyase is a ...

https://en.wikipedia.org/wiki/S-adenosyl-L-homocysteine_hydrolase

The use of an inhibitor of adenosine deaminase to increase the half-life of vidarabine has also been tried, and drugs such as ... It is prone to deamination by adenosine deaminase to inosine. This metabolite still possesses antiviral activity, but is 10- ... As you can see from figure 1.1 that it is a stereoisomer of adenosine. It has a half-life of 60 minutes, and its solubility is ... This is the active form of vidarabine and is both an inhibitor and a substrate of viral DNA polymerase. When used as a ...

https://en.wikipedia.org/wiki/Vidarabine

... it is broken down by adenosine deaminase, which is present in red blood cells and the vessel wall. Dipyridamole, an inhibitor ... Adenosine deaminase deficiency is a known cause of immunodeficiency. The adenosine analog NITD008 has been reported to directly ... Adenosine receptor Adenosine reuptake inhibitor List of growth hormone secretagogues Nelson, David L.; Cox, Michael M. (2005). ... Adenosine is believed to be an anti-inflammatory agent at the A2A receptor. Topical treatment of adenosine to foot wounds in ...

https://en.wikipedia.org/wiki/Adenosine

EHNA is also a very potent adenosine deaminase inhibitor with an IC50 ~2 nM.[13] This dual inhibition would lead to the ... "Adenosine deaminase inhibition enhances the inotropic response mediated by A1 adenosine receptor in hyperthyroid guinea pig ... this problem can be resolved if the effect of adenosine accumulated by EHNA, a result of adenosine deaminase inhibition, can be ... Structure and bonding of the inhibitors[edit]. Comparison of these inhibitors with the natural substrates of the enzyme, cAMP ...

https://en.wikipedia.org/wiki/PDE2

The most common treatment for DADA2 is TNF inhibitors. This therapy tends to prevent vasculitis-related manifestations such as ... The protein product of this gene, adenosine deaminase 2 (ADA2), is an extracellular enzyme that breaks down adenosine and may ... Carmona-Rivera C (2019). "Deficiency of adenosine deaminase triggers adenosine-mediated NETosis and TNF production in patients ... "The extracellular adenosine deaminase growth factor, ADGF/CECR1, plays a role in Xenopus embryogenesis via the adenosine/P1 ...

https://en.wikipedia.org/wiki/Adenosine_deaminase_2_deficiency

APC Adenosine deaminase deficiency, partial; 102700; ADA Adenosine triphosphate, elevated, of erythrocytes; 102900; PKLR ... Lutheran inhibitor; 111150; KLF1 Bloom syndrome; 210900; RECQL3 Blue cone monochromacy; 303700; OPN1MW Blue cone monochromacy; ... KRT1 Plasminogen activator inhibitor, type I; 613329; PAI1 Platelet disorder, familial, with associated myeloid malignancy; ... response to tyrosine kinase inhibitor in; 211980; EGFR Nonsmall cell lung cancer, somatic; 211980; IRF1 Nonsmall cell lung ...

https://en.wikipedia.org/wiki/List_of_OMIM_disorder_codes

It is deaminated intracellularly by adenosine deaminase to dioxolane guanine (DXG). DXG-triphosphate, the active form of the ... protease inhibitors, entry inhibitors, co-receptor inhibitors and integrase inhibitors. The reverse transcriptase of HIV-1 has ... Inhibitors Discovery and Development of HIV Protease Inhibitors Reverse-transcriptase inhibitor Protease inhibitor Entry ... non-nucleoside reverse-transcriptase inhibitors and protease inhibitors. Currently, there are several NRTIs in various stages ...

https://en.wikipedia.org/wiki/Discovery_and_development_of_nucleoside_and_nucleotide_reverse-transcriptase_inhibitors

However, editing by cellular enzyme adenosine deaminase-1 changes the stop codon to UGG, allowing the large-HDAg to be produced ... HDAg-L, in contrast, is produced during the later stages of an infection, acts as an inhibitor of viral replication, and is ...

https://en.wikipedia.org/wiki/Hepatitis_D

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ... Thus it is an HDAC inhibitor. Many HDAC inhibitors are potential treatments for cancer through the ability to epigenetically ... Wei, D etal., (2014). ""Histone Deacetylase Inhibitor Romidepsin Induces HIV Expression in CD4 T Cells from Patients on ... The trial also compared the effect of romidepsin to another histone deacetylase inhibitor, Vorinostat [9] ...

https://en.wikipedia.org/wiki/Romidepsin

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ... RET inhibitors: Vandetanib (also VEGFR and EGFR). Entrectinib (ALK, ROS1, NTRK). c-MET inhibitor: Cabozantinib (also VEGFR2). ... Generating Inhibitors of P-Glycoprotein: Where to, Now?. Springer Protocols. pp. 405-432.. ... Topoisomerase inhibitors are drugs that affect the activity of two enzymes: topoisomerase I and topoisomerase II. When the DNA ...

https://en.wikipedia.org/wiki/Chemotherapeutics

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ...

https://en.wikipedia.org/wiki/Ecteinascidin_743

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ... PI3K inhibitor. References[edit]. *^ a b c d e f g h i j k l Pópulo, Helena; Lopes, José Manuel; Soares, Paula (2012). "The ... The second generation of mTOR inhibitors is known as ATP-competitive mTOR kinase inhibitors.[7] mTORC1/mTORC2 dual inhibitors ... mTOR/PI3K dual inhibitors[edit]. Several, so-called mTOR/PI3K dual inhibitors (TPdIs), have been developed and are in early- ...

https://en.wikipedia.org/wiki/MTOR_inhibitor

Dipyridamole also inhibits the enzyme adenosine deaminase, the enzyme that catalyzes the breakdown of adenosine. Fenfluramine ... Wang YX, Bowersox SS, Pettus M, Gao D (1999). "Antinociceptive properties of fenfluramine, a serotonin reuptake inhibitor, in a ... Dipyridamole inhibits reuptake of adenosine, resulting in greater extracellular concentrations of adenosine. ...

https://en.wikipedia.org/wiki/Indirect_agonist

Dipeptidyl peptidáza-4 (DPP4) -- známá rovněž jako komplexační protein adenosin deaminázy 2 (adenosine deaminase complexing ... DPPIV inhibitors extend GLP-2 mediated tumour promoting effects on intestinal cancer cells. Regul Pept.. 2006, roč. 137, čís. 3 ... Kameoka J, Tanaka T, Nojima Y, Schlossman SF, Morimoto C. Direct association of adenosine deaminase with a T cell activation ... Barnett A. DPP-4 inhibitors and their potential role in the management of type 2 diabetes. Int. J. Clin. Pract.. November 2006 ...

https://cs.wikipedia.org/wiki/Dipeptidylpeptidáza_4

AMPD2 adenosine monophosphate deaminase 2 [ Homo sapiens (human) ]». Gene. NCBI. 4. juni 2017. Henta 26. juni 2017.. ... AZIN2 antizyme inhibitor 2 [ Homo sapiens (human) ]». Gene. NCBI. 6. juni 2017. Henta 26. juni 2017.. ...

https://nn.m.wikipedia.org/wiki/Humant_kromosom_1

3. Crystallization and characterization of adenosine 5′-monophosphate-dependent threonine deaminase from Escherichia coli". J. ... Robert A. Copeland (2013). Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and ... http://books.google.com/books/about/Evaluation_of_Enzyme_Inhibitors_in_Drug.html?id=l2rMy8QNUk0C. ...

https://sh.wikipedia.org/wiki/Treoninska_amonijak-lijaza

If the nucleoside is adenosine, it is acted upon by adenosine deaminases to convert it into inosine. This metabolite, in turn, ... "Establishment of correlation between in-silico and in-vitro test analysis against Leishmania HGPRT to inhibitors". ... The nucleosides cytidine and deoxycytidine can be salvaged along the uracil pathway by cytidine deaminase, which converts them ...

https://en.wikipedia.org/wiki/Nucleotide_salvage

... adenosine kinase and adenosine deaminase in tissues from vertebrates and invertebrates in relation to the control of the ... Kowaluk EA, Jarvis MF (March 2000). "Therapeutic potential of adenosine kinase inhibitors". Expert Opinion on Investigational ... Adenosine kinase (AdK; EC 2.7.1.20) is an enzyme that catalyzes the transfer of gamma-phosphate from Adenosine triphosphate ( ... As such, there is much interest in developing specific inhibitors of AdK. Many AdK inhibitors, some of which show useful ...

https://en.wikipedia.org/wiki/Adenosine_kinase

The deamination of adenosine is catalyzed by the double-stranded RNA-specific adenosine deaminase (ADAR), which typically acts ... Curran J, Boeck R, Kolakofsky D (October 1991). "The Sendai virus P gene expresses both an essential protein and an inhibitor ... These genes share close identity with the bacterial deaminases involved in nucleotide metabolism. The adenosine deaminase of E ... Carter CW (1998). "Nucleoside deaminases for cytidine and adenosine: comparisons with deaminases acting on RNA". In Grosjean H ...

https://en.wikipedia.org/wiki/RNA_editing

C1-inhibitor (Angioedema/Hereditary angioedema). *Complement 2 deficiency/Complement 4 deficiency. *MBL deficiency ... autosomal: Adenosine deaminase deficiency. *Omenn syndrome. *ZAP70 deficiency. *Bare lymphocyte syndrome. Acquired. *AIDS ...

https://en.wikipedia.org/wiki/Hyperimmunoglobulin_E_syndrome

Mendicino, J. and Muntz, J.A. (1958). "The activating effect of adenosine triphosphate on brain adenylic deaminase". J. Biol. ... Robert A. Copeland (2013). Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and ... Turner, D.H. and Turner, J.F. (1961). "Adenylic deaminase of pea seeds". Biochem. J. 79: 143-147. PMID 13778717. ... Lee, Y.-P. (1957). "5′-Adenylic acid deaminase. III. Properties and kinetic studies". J. Biol. Chem. 227: 999-1007. PMID ...

https://sh.wikipedia.org/wiki/AMP_deaminaza

ADA: Adenosine Deaminase (Adenosine Deaminase Deficiency) ANDP: encoding protein Activity-dependent neuroprotector homeobox ... encoding protein cAMP-dependent protein kinase inhibitor gamma PLAGL2: encoding protein Zinc finger protein PLAGL2 POLR3F: ... Albright's hereditary osteodystrophy Arterial tortuosity syndrome Adenosine deaminase deficiency Alagille syndrome Fatal ...

https://en.wikipedia.org/wiki/Chromosome_20

https://en.wikipedia.org/wiki/Antibody-dependent_cellular_cytotoxicity

T-/B- SCID (both T and B cells absent): RAG 1/2 deficiency, DCLRE1C deficiency, adenosine deaminase (ADA) deficiency, reticular ... C1-inhibitor deficiency (hereditary angioedema) Factor I deficiency (pyogenic infections) Factor H deficiency (haemolytic- ... deficiency Membrane attack complex inhibitor (CD59) deficiency Paroxysmal nocturnal hemoglobinuria Immunodeficiency associated ...

https://en.wikipedia.org/wiki/Primary_immunodeficiency

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ...

https://en.wikipedia.org/wiki/Bleomycin

Ruconest (C1-inhibitor). References[edit]. *^ a b c d e f g h i j k l m n o p q r s t Bernstein, JA; Cremonesi, P; Hoffmann, TK ... autosomal: Adenosine deaminase deficiency. *Omenn syndrome. *ZAP70 deficiency. *Bare lymphocyte syndrome. Acquired. *AIDS ... ACE inhibitors can induce angioedema.[13][14][15] ACE inhibitors block the enzyme ACE so it can no longer degrade bradykinin; ... Types I and II are caused by mutations in the SERPING1 gene, which result in either diminished levels of the C1-inhibitor ...

https://en.wikipedia.org/wiki/Angioneurotic_oedema

Guanine deaminase. *Adenosine deaminase. *AMP deaminase. *Inosine monophosphate synthase. *DCMP deaminase. *GTP cyclohydrolase ...

https://en.wikipedia.org/wiki/GTP_cyclohydrolase_II

Guanine deaminase. *Adenosine deaminase. *AMP deaminase. *Inosine monophosphate synthase. *DCMP deaminase. *GTP cyclohydrolase ...

https://en.wikipedia.org/wiki/Succinyl-diaminopimelate_desuccinylase

Adenosine Monophosphate Deaminase Deficiency type 1. Nucleotide salvage. *Lesch-Nyhan syndrome/Hyperuricemia ... Xanthine oxidase inhibitors decrease the production of uric acid, by interfering with xanthine oxidase. Uricosurics increase ... Medications most often used to treat hyperuricemia are of two kinds: xanthine oxidase inhibitors and uricosurics. ... and is a possible weak inhibitor of xanthine dehydrogenase. As a byproduct of its fermentation process, beer additionally ...

https://en.wikipedia.org/wiki/Hyperuricemia

2001). "Adenosine A2B receptors behave as an alternative anchoring protein for cell surface adenosine deaminase in lymphocytes ... Moždano specifični angiogenezni inhibitor (1, 2, 3) • Cadherin (1, 2, 3) • Kalcitonin • CALCRL • CD97 • Kortikotropin- ... Strohmeier GR, Reppert SM, Lencer WI, Madara JL (1995). "The A2b adenosine receptor mediates cAMP responses to adenosine ... alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting ...

https://sh.wikipedia.org/wiki/Adenozinski_A2B_receptor

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ... Ribociclib, sold under the brand name Kisqali,[1] is an inhibitor of cyclin D1/CDK4 and CDK6, and is used for the treatment of ... When used in combination with other drugs such as an ALK or an MEK inhibitor, ribociclib has been shown to have a synergistic ... Examples of such inhibitors include ketoconazole and similar antifungal drugs, ritonavir, clarithromycin, as well as grapefruit ...

https://en.wikipedia.org/wiki/Ribociclib

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ... Carson had studied adenosine deaminase deficiency and recognized that because the lack of adenosine deaminase led to the ... However, unlike adenosine it is relatively resistant to breakdown by the enzyme adenosine deaminase, which causes it to ... which renders it partially resistant to breakdown by adenosine deaminase (ADA). In cells it is phosphorylated into its toxic ...

https://en.wikipedia.org/wiki/Cladribine

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ...

https://en.wikipedia.org/wiki/Intercalation_

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ... Erythromycin, ketoconazole and cyclosporine are CYP3A4 inhibitors and therefore inhibit the metabolic pathway of docetaxel.[13] ... Docetaxel is also used in combination with capecitabine, a DNA synthesis inhibitor.[21] ...

https://en.wikipedia.org/wiki/Docetaxel

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ...

https://en.wikipedia.org/wiki/Photodynamic_therapy

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ... Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells.[1] ...

https://en.wikipedia.org/wiki/Pralatrexate

Methotrexate, a competitive inhibitor of DHFR, is one such anticancer drug that inhibits DHFR.[34] Other drugs include ... Adenosine deaminase. *Purine nucleoside phosphorylase. *Guanine deaminase. *Xanthine oxidase. *Urate oxidase. Pyrimidine ... Main article: Dihydrofolate reductase inhibitor. Since folate is needed by rapidly dividing cells to make thymine, this effect ... Bacteria also need DHFR to grow and multiply and hence inhibitors selective for bacterial DHFR have found application as ...

https://en.wikipedia.org/wiki/Dihydrofolate_reductase

The nucleoside, adenosine, is then deaminated and hydrolyzed to form hypoxanthine via adenosine deaminase and nucleosidase ... ATP, a purine nucleotide, is an activator of pyrimidine synthesis, while CTP, a pyrimidine nucleotide, is an inhibitor of ... and adenosine deaminase deficiency, which causes immunodeficiency.[9][10][11]. Interconversion of nucleotides[edit]. Once the ... Guanine is then deaminated via guanine deaminase to form xanthine which is then converted to uric acid. Oxygen is the final ...

https://en.wikipedia.org/wiki/Nucleic_acid_metabolism

Adenosine deaminase-SCID Leadiant Biosciences Rare pediatric Gamifant Haemophagocytic lymphohistiocytosis Novimmune Tropical ... review time for alirocumab and was part of their strategy to beat Amgen to market with the first approval of a PCSK9 inhibitor. ...

https://en.wikipedia.org/wiki/Priority_review_voucher

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ... As a result, the function of these drugs is to serve as enzyme poisons rather than inhibitors. This can be applied to treat ...

https://en.wikipedia.org/wiki/Crosslinking_of_DNA

"Adenosine receptor-blocking xanthines as inhibitors of phosphodiesterase isozymes". Biochemical Pharmacology. 45 (4): 847-51. ... It is created from guanine by guanine deaminase.. *It is created from hypoxanthine by xanthine oxidoreductase. ... nonselective adenosine receptor antagonists [13] which inhibit sleepiness-inducing adenosine.. But different analogues show ... correlation of behavioral effects with activity as adenosine receptor antagonists and as phosphodiesterase inhibitors". Life ...

https://en.wikipedia.org/wiki/Methylxanthines

Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ... Idelalisib is a competitive inhibitor of the ATP binding site of the PI3Kδ catalytic domain. Its in vitro potency and ... The substance acts as a phosphoinositide 3-kinase inhibitor; more specifically, it blocks P110δ, the delta isoform of the ...

https://en.wikipedia.org/wiki/Idelalisib

Adenosine deaminase. *Adenosylmethionine decarboxylase. *Adenylosuccinate synthase. *AdoMet MTase. *Adrenocorticotropic hormone ... Brain-specific angiogenesis inhibitor. *Branched chain amino acid-cation symporter. *Brassinosteroid insensitive-1 ...

https://en.wikipedia.org/wiki/Category:Protein_pages_needing_a_picture

Most commonly, enzymes known as adenosine deaminases acting on RNA (ADARs) catalyze adenosine to inosine (A to I) transitions. ... MiR-712 targets tissue inhibitor of metalloproteinases 3 (TIMP3). TIMPs normally regulate activity of matrix metalloproteinases ... Lewis BP, Burge CB, Bartel DP (January 2005). "Conserved seed pairing, often flanked by adenosines, indicates that thousands of ... polyadenylated with multiple adenosines (a poly(A) tail), and spliced. Animal miRNAs are initially transcribed as part of one ...

https://en.wikipedia.org/wiki/MicroRNA

Adenosine deaminase inhibitors. Synthesis and biological activity of deaza analogues of erythro-9-(2-hydroxy-3-nonyl)adenine.. ... The results obtained showed that there is no correlation between adenosine deaminase inhibition and antiviral or antitumor ... were synthesized and evaluated for adenosine deaminase (ADA) inhibitory activity and compared with EHNA, 1-deaza-EHNA (2), and ... 3-Deaza-EHNA, the most active inhibitor of ADA among the EHNA deaza analogues, greatly potentiates the antitumor activity of ...

https://www.ncbi.nlm.nih.gov/pubmed/3339608

... adenosine deaminase inhibitor explanation free. What is adenosine deaminase inhibitor? Meaning of adenosine deaminase inhibitor ... Looking for online definition of adenosine deaminase inhibitor in the Medical Dictionary? ... adenosine deaminase inhibitor. adenosine deaminase inhibitor. A drug that interferes with the action of the enzyme adenosine ... Adenosine deaminase inhibitor , definition of adenosine deaminase inhibitor by Medical dictionary https://medical-dictionary. ...

http://medical-dictionary.thefreedictionary.com/adenosine+deaminase+inhibitor

AMPD2 inhibitor 1 Inhibitor AMPD2 inhibitor 1 is an adenosine monophosphate deaminase 2 (AMPD2) inhibitor, used in the research ... Adenosine deaminase Adenosine deaminase is an enzyme that catalyzes the irreversible deamination of adenosine and 2- ... Inhibitor ,98.0% EHNA hydrochloride is a specific inhibitor of adenosine deaminase, prevents dAdo degradation and increases ... Adenosine deaminase is considered one of the key enzymes of purine metabolism. Adenosine deaminase in humans is involved in the ...

https://www.medchemexpress.com/Targets/Adenosine%20Deaminase.html

MedChemExpress provides thousands of inhibitors, modulators and agonists with high purity and quality, excellent customer ... Adenosine Deaminase Neurological Disease AMPD2 inhibitor 1 is an adenosine monophosphate deaminase 2 (AMPD2) inhibitor, used in ... Adenosine Deaminase Cancer 1-Deazaadenosine is a potent Adenosine deaminase (ADA) inhibitor with a Ki value of 0.66 μM. 1- ... Adenosine Deaminase Cancer Pentostatin (CI-825; Deoxycoformycin) is an irreversible inhibitor of adenosine deaminase with Ki of ...

https://www.medchemexpress.com/search.html?q=Adenosine+Deaminase+Inhibitors&ft=&fa=&fp=

Categories Adenosine DeaminaseLeave a comment on The MAPK3 Tpl2 controls innate and adaptive immunity by regulating TLR Because ... Category: Adenosine Deaminase. The MAPK3 Tpl2 controls innate and adaptive immunity by regulating TLR. The MAPK3 Tpl2 controls ... Categories Adenosine DeaminaseTags buy PRT062607 HCL, HLI-98C, Sirt4Leave a comment on is definitely an essential protection ... Categories Adenosine DeaminaseTags Rabbit polyclonal to ADORA3 isoform1, SDZ 205-557 HClLeave a comment on Internet-based HIV ...

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Categories Adenosine DeaminaseTags Marimastat enzyme inhibitor, PYST1 Posts navigation. Page 1 Page 2 … Page 5 Next page ... Categories Adenosine DeaminaseTags Mertk, VX-950 inhibitor Lengthy noncoding RNAs (lncRNAs) are from the development, ... Categories Adenosine DeaminaseTags AG-014699 pontent inhibitor, CSF3R Intervertebral disc degeneration (IDD) is certainly an ... Categories Adenosine DeaminaseTags DIAPH1, Favipiravir enzyme inhibitor Picornaviruses replicate their genomes in colaboration ...

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1LRCH11Myricetin enzyme inhibitor. Supplementary MaterialsS1 Fig: Amplification products of 16S rDNA genes and entire. * ... Adenosine Deaminase. Aim: To investigate whether estrogen receptor (ER-) corrections were applied to. *Adenosine Deaminase ... 1Cediranib tyrosianse inhibitor1Rabbit polyclonal to ZNF540. Esophageal cancer is usually a virulent malignancy connected with ... First, Work plots produced from CD data for pairings of SAF-p1 and SAF-p2a, and of SAF-p1-pro4 and Myricetin enzyme inhibitor ...

http://www.monossabios.com/category/adenosine-deaminase/

Doxorubicin is usually a topoisomerase II (TOP2) inhibitor that damages DNA by trapping TOP2 in a TOP2-DNA complex after TOP2 ... S4). Etoposide is usually another TOP2 inhibitor that generates DSBs through TOP2, whereas bleomycin and x-rays directly attack ... Nevertheless, treatment with RNAse inhibitor is essential to avoid degradation from the mRNA through the prolonged exudation ... Marcus with CA inhibitors significantly reduces the power of the bacterias to survive in a acid environment, recommending that ...

http://biodigestor.net/?cat=21&paged=2

Adenosine deaminase inhibitors. Drugs used in the treatment of chronic lymphocytic leukaemia and lymphoma that appear to be ...

https://www.leukaemia.org.au/how-we-can-help/information-and-education-services/glossary-of-terms/

3-DNB is a mixed inhibitor of ADA and may thus lead to increases in extracellular adenosine. The finding may provide insights ... Adenosine is considered neuroprotective, but it is rapidly removed by extracellular deaminases such as adenosine deaminase (ADA ... Mixed inhibition of adenosine deaminase activity by 1,3-dinitrobenzene: a model for understanding cell-selective neurotoxicity ... Kinetics revealed mixed inhibition with 1,3-DNB binding to ADA (K(I) = 520 ± 100 μM, n = 1 ± 0.6) and the ADA-adenosine complex ...

https://pubmed.ncbi.nlm.nih.gov/22106038/

Open up in another window Open up in another window Shape 1 Represent PDK1 inhibitor picture of survivin manifestation. 3.4. ... Blockade of lipid development by various medicines like the COX2 inhibitor celecoxib, decreased tumour development and ... em PDK1 inhibitor P /em ? ?.001; em R /em ?=?.513, em P /em ? ?.001), Ki67 manifestation ( em /em 2?=?30.232, em P /em ? ?.001 ... em PDK1 inhibitor /em 2?=?19.973, em P /em ? ?.001), and survivin manifestation marks ( em /em 2?=?15.555, em P /em ?=?.015) ( ...

http://www.enmd-2076.com/category/adenosine-deaminase/

... an inhibitor of adenosine deaminase, in the rat",. abstract = "The distribution of the potent inhibitor of adenosine deaminase ... Pharmacokinetics of 2′-deoxycoformycin, an inhibitor of adenosine deaminase, in the rat. / Geiger, J. D.; Lewis, J. L.; ... The distribution of the potent inhibitor of adenosine deaminase (ADA), 2′-deoxycoformycin (DCF), in the brain of the rat and ... N2 - The distribution of the potent inhibitor of adenosine deaminase (ADA), 2′-deoxycoformycin (DCF), in the brain of the rat ...

https://experts.nebraska.edu/en/publications/pharmacokinetics-of-2-deoxycoformycin-an-inhibitor-of-adenosine-d

Adenosine deaminase: functional implications and different classes of inhibitors. Med. Res. Rev. 21,105 -128. ... Adenosine deaminase (E.C. 3.5.4.4) catalyses the conversion of adenosine and 2′-deoxyadenosine to inosine and 2′-deoxyinosine, ... Enzymatic activity of recombinant P. duboscqi salivary adenosine deaminase (ADA). A cuvette containing 20 μmol l-1 adenosine in ... Adenosine deaminase was previously reported in the saliva of the sand fly Lutzomyia longipalpis but it was not present in the ...

http://jeb.biologists.org/content/210/5/733

Adenosine Deaminase Inhibitors. Enzyme Inhibitors. To Top. *For Patients and Families. *For Researchers ...

https://clinicaltrials.gov/ct2/show/NCT00541034?cond=%22Leukemia%22&intr=%22Pentostatin%22&rank=6

A potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, ... Pentostatin is a potent transition state inhibitor of adenosine deaminase (ADA), the greatest activity of which is found in ... The cytotoxicity that results from prevention of catabolism of adenosine or deoxyadenosine is thought to be due to elevated ...

http://www.rcsb.org/ligand/DCF

... is used to treat adenosine deaminase severe combined immune deficiency (ADA-SCID). Includes Revcovi side effects, interactions ... Xospata Xospata (gilteritinib) is a FLT3 / AXL kinase inhibitor indicated for the... ... Revcovi (elapegademase-lvlr) is a recombinant adenosine deaminase indicated for the treatment of adenosine deaminase severe ... mutations in the ADA gene reduce or eliminate the protective activity of adenosine deaminase, allowing the buildup of adenosine ...

https://www.drugs.com/newdrugs/fda-approves-revcovi-elapegademase-lvlr-adenosine-deaminase-severe-combined-immune-deficiency-ada-4839.html

Pentostatin (a potent adenosine deaminase inhibitor). * Forodesine. * Gemcitabine [130] * Histone deacetylase inhibitors (eg, ... Forodesine is a potent inhibitor of purine nucleoside phosphorylase that promotes apoptosis in T- and B- cells through ... Final results of a multicenter phase II study of the purine nucleoside phosphorylase (PNP) inhibitor forodesine in patients ...

https://www.medscape.com/answers/2139720-90033/359607-overview

T1 - Conversion of a stem cell leukemia from a T-lymphoid to a myeloid phenotype induced by the adenosine deaminase inhibitor 2 ... Conversion of a stem cell leukemia from a T-lymphoid to a myeloid phenotype induced by the adenosine deaminase inhibitor 2- ... Conversion of a stem cell leukemia from a T-lymphoid to a myeloid phenotype induced by the adenosine deaminase inhibitor 2- ... Conversion of a stem cell leukemia from a T-lymphoid to a myeloid phenotype induced by the adenosine deaminase inhibitor 2- ...

https://tmu.pure.elsevier.com/en/publications/conversion-of-a-stem-cell-leukemia-from-a-t-lymphoid-to-a-myeloid

Conversion of a stem cell leukemia from a T-lymphoid to a myeloid phenotype induced by the adenosine deaminase inhibitor 2- ... Conversion of a stem cell leukemia from a T-lymphoid to a myeloid phenotype induced by the adenosine deaminase inhibitor 2- ... Selective failure of lymphoid development occurs in genetic deficiency of adenosine deaminase (ADA). We examined the in vivo ... a potent inhibitor of S-adenosylmethionine-dependent methylation. The influence of these changes on the leukemic phenotype is ...

https://scholars.duke.edu/display/pub732406

Adenosine Deaminase Inhibitors* * Clinical Trials as Topic * Diabetes Mellitus, Type 2 / drug therapy* ... The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes Lancet ... Orally administered DPP-4 inhibitors, such as sitagliptin and vildagliptin, reduce HbA1c by 0.5-1.0%, with few adverse events ... and inhibitors of dipeptidyl peptidase-4 (DPP-4) activity (incretin enhancers). Clinical trials with the incretin mimetic ...

https://pubmed.ncbi.nlm.nih.gov/17098089/?dopt=Abstract

Adenosine deaminase inhibitor: Cladribine, Fludarabine and Pentostatin. Floxuridine is similar to the drug 5-fluorouracil, it ...

http://www.chemocare.com/chemotherapy/drug-info/floxuridine.aspx

Adenosine deaminase inhibitor: Cladribine, Fludarabine and Pentostatin *Ribonucleotide reductase inhibitor: Hydroxyurea. Note: ...

http://chemocare.com/chemotherapy/drug-info/Mylocel.aspx

Here, through analysis of genome-scale loss-of-function datasets, we identify adenosine deaminase acting on RNA (ADAR or ADAR1 ... M.M. and H.S.G. are inventors on a patent application for the use of ADAR1 inhibitors in cancer treatment. The remaining ... Identification of ADAR1 adenosine deaminase dependency in a subset of cancer cells. *Hugh S. Gannon1,2. na1, ... Gannon, H.S., Zou, T., Kiessling, M.K. et al. Identification of ADAR1 adenosine deaminase dependency in a subset of cancer ...

https://www.nature.com/articles/s41467-018-07824-4?error=cookies_not_supported&code=8e3c312d-9450-4123-bb6b-d6ab9aedff6d

Pentostatin (a potent adenosine deaminase inhibitor) * Forodesine * Gemcitabine [129] * Histone deacetylase inhibitors (eg, ... Romidepsin is a histamine deacetylase (HDAC) inhibitor. It is indicated for cutaneous T-cell lymphoma in patients who have ... Forodesine is a potent inhibitor of purine nucleoside phosphorylase that promotes apoptosis in T- and B- cells through ... Final results of a multicenter phase II study of the purine nucleoside phosphorylase (PNP) inhibitor forodesine in patients ...

https://emedicine.medscape.com/article/2139720-medication

... an inhibitor of hENT1. All samples received adenosine deaminase inhibitor (50 μM dCF). (B) Diagram illustrating the position of ... an inhibitor of adenosine deaminase. Cell viability was analyzed after 24 h and 48 h of incubation; 5 μM dAdo (red) was used ... 1979) Adenosine kinase from rabbit liver. II. Substrate and inhibitor specificity. J Biol Chem 254:2346-2352. ... 2016) Adenosine deaminase deficiency-More than just an immunodeficiency. Front Immunol 7:314. ...

https://www.pnas.org/content/115/26/6846

Adenosine deaminase inhibitor. 16. 5. Anti-Retroviral Agents. 16. 1. Survivin Down-Regulation. 15. 13. ...

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Pharmacological Actions : Adenosine deaminase inhibitor. [+] Nettles may reduce blood sugar levels through acting as an insulin ... Pharmacological Actions : Alpha-amylase inhibitor, Alpha-glucosidase inhibitor , Cardioprotective, Nitric Oxide Enhancer, ... Pharmacological Actions : Anti-Inflammatory Agents, Nitric Oxide Inhibitor, Tumor Necrosis Factor (TNF) Alpha Inhibitor ... Pharmacological Actions : Anti-Inflammatory Agents, Interleukin-6 Downregulation, Tumor Necrosis Factor (TNF) Alpha Inhibitor, ...

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Dextran-Bound Purine Nucleosides-Substrates and Inhibitors of Adenosine Deaminase. Affinity Binding Used as a Tool to ... Multiple Peak Formation in the Reversed Phase Liquid Chromatographic Separation of Soybean Trypsin Inhibitor. N-F Transition of ...

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A drug that interferes with the action of the enzyme adenosine deaminase necessary for the irreversible conversion of adenosine to inosine. (thefreedictionary.com)
Adenosine deaminase is an enzyme that catalyzes the irreversible deamination of adenosine and 2'-deoxyadenosine to inosine and 2'-deoxyinosine, respectively. (medchemexpress.com)
To confirm that the transcript coding for ADA was responsible for the activity observed in the saliva of this sand fly, we cloned this transcript into a prokaryotic expression vector and produced a soluble and active recombinant protein of approximately 60 kDa that was able to convert adenosine to inosine. (biologists.org)
ADA2 catalyzes the reaction of adenosine to inosine and 2'deoxyadenosine in the blood. (wikipedia.org)
In vehicle-treated rabbits, aqueous humor adenosine and inosine levels were 2.7 ± 0.38 and 29 ± 4.2 ng/100 μl, respectively. (arvojournals.org)
Three hours after epinephrine administration, adenosine and inosine levels had significantly increased to 11 ± 1.6 and 66 ± 4.4 ng/100 μl, respectively. (arvojournals.org)
Design By utilising large scale transcriptome sequencing of three paired HCC clinical specimens and their adjacent non-tumour (NT) tissue counterparts at depth, we discovered an average of 20 007 inferred A to I (adenosine to inosine) RNA editing events in transcripts. (bmj.com)
The catalytic efficiency for inosine is 350,000-fold greater than for adenosine. (rcsb.org)
Adenine nucleosides and nucleotides are deaminated by adenosine deaminase and AMP deaminase to their corresponding inosine derivatives which, in turn, may be further degraded. (rcsb.org)
In vivo microdialysis showed that the histamine release in the frontal cortex was decreased by microinjection into the TMN of N 6 -cyclopentyladenosine (CPA), an A 1 R agonist, adenosine or coformycin, an inhibitor of adenosine deaminase, which catabolizes adenosine to inosine. (pnas.org)
Background Adenosine-to-inosine RNA editing is a co-transcriptional/post-transcriptional modification of double-stranded RNA, catalysed by one of two active adenosine deaminases acting on RNA (ADARs), ADAR1 and ADAR2. (bmj.com)

Pentostatin is an irreversible inhibitor of adenosine deaminase with K i of 2.5 pM. (medchemexpress.com)
Pentostatin is a potent transition state inhibitor of adenosine deaminase (ADA), the greatest activity of which is found in cells of the lymphoid system. (rcsb.org)
Be sure to mention adenosine deaminase inhibitors such as pentostatin (Nipent). (medlineplus.gov)
Concomitant adenosine deaminase inhibitors (eg, pentostatin): not recommended. (empr.com)
Pentostatin (Nipent) is a nucleoside analog that inhibits the activity of the enzyme adenosine deaminase. (cancernetwork.com)
It appears that the cytotoxic effect of pentostatin is independent of intracellular concentrations of adenosine deaminase. (cancernetwork.com)
Dr. Nam Dang and colleagues discuss a phase II trial evaluating the role of pentostatin in relapsed/refractory T-cell lymphomas in relation to CD26 expression, which is integral to adenosine deaminase cell surface expression and function. (cancernetwork.com)
Pentostatin (2 -deoxycoformycin, DCF) is a potent inhibitor of adenosine deaminase (ADA). (scialert.net)

It has also been proposed that Adenosine deaminase, in addition to adenosine breakdown, stimulates release of excitatory amino acids and is necessary to the coupling of A1 adenosine receptors and heterotrimeric G proteins. (medchemexpress.com)
Moreover, RDC8 mRNA and adenosine A2 receptors display a very similar distribution in the brain. (nih.gov)
In conclusion, insulin neuroprotection against oxidative stress-mediated damage involves 1 ) stimulation of glucose uptake and metabolism, increasing energy levels and intracellular adenosine and, ultimately, uric acid formation and 2 ) a decrease in extracellular adenosine, which may reduce the facilitatory activity of adenosine receptors. (diabetesjournals.org)
This rise in endogenous levels of adenosine then leads to the activation of ocular adenosine receptors and is in part responsible for the ocular hypotensive action of epinephrine. (arvojournals.org)
Adenosine (ADO) is an immunosuppressive molecule, which suppresses the immune responses by interacting with specific receptors expressed by immune effector cells. (hindawi.com)
In contrast, A2A and A2B receptors are coupled with G proteins Gs or Gq and activate adenylyl cyclase or phospholipase C. Moreover, all adenosine receptors activate mitogen-activated protein kinase (MAPK) pathways, which include extracellular signal regulated kinase 1 (ERK1), ERK2, Jun N-terminal kinase, and p38 MAPK. (hindawi.com)
The different adenosine receptor subtypes (A1, A2A, A2B, and A3) are all seven transmembrane spanning G-protein coupled receptors . (bionity.com)
The A2A and A2B receptors couple to Gάs and mediate the stimulation of adenylate cyclase, while the A1 and A3 adenosine receptors couple to Gάi which inhibits adenylate cyclase activity. (bionity.com)
Additionally, A1 receptors couple to Gάo, which has been reported to mediate adenosine inhibition of Ca2+ conductance, whereas A2B and A3 receptors also couple to Gάq and stimulate phospholipase activity. (bionity.com)
Adenosine is a potent anti-inflammatory agent, acting at its four G-protein coupled receptors. (bionity.com)
2007. Shaping of monocyte and macrophage function by adenosine receptors. (springer.com)
2001. Role of G-protein-coupled adenosine receptors in downregulation of inflammation and protection from tissue damage. (springer.com)
2016. Specific activation of A3, A2A and A1 adenosine receptors in CD73-knockout mice affects B16F10 melanoma growth, neovascularization, angiogenesis and macrophage infiltration. (springer.com)
2008. Blockade of adenosine A2B receptors ameliorates murine colitis. (springer.com)
Adenosine has been proposed to promote sleep through A 1 receptors (A 1 R's) and/or A 2A receptors in the brain. (pnas.org)
Among the four subtypes of adenosine receptors, A 1 , A 2A , A 2B , and A 3 ( 15 ), A 1 R and/or A 2A R subtypes have been reported to mediate the sleep-promoting effect of adenosine. (pnas.org)
Adenosine is released from a variety of cells in response to inflammatory and metabolic stress and exerts its physiological functions by interacting with 4 subtypes of adenosine receptors, including A1, A2A, A2B, and A3 receptor [ 1 , 2 ]. (hindawi.com)

The results obtained showed that there is no correlation between adenosine deaminase inhibition and antiviral or antitumor activity in this series of compounds. (nih.gov)
Kinetics revealed mixed inhibition with 1,3-DNB binding to ADA (K(I) = 520 ± 100 μM, n = 1 ± 0.6) and the ADA-adenosine complex (K(IS) = 262 ± 7 μM, n = 6 ± 0.6, indicating positive cooperativity). (nih.gov)
The distribution of the potent inhibitor of adenosine deaminase (ADA), 2′-deoxycoformycin (DCF), in the brain of the rat and its inhibition of ADA in brain and gut was determined. (nebraska.edu)
The cytotoxicity that results from prevention of catabolism of adenosine or deoxyadenosine is thought to be due to elevated intracellular levels of dATP, which can block DNA synthesis through inhibition of ribonucleotide reductase. (rcsb.org)
Effects of ADA inhibition on leukemia cells during treatment included expansion of the deoxyadenosine nucleotide pool and accumulation of S-adenosylhomocysteine, a potent inhibitor of S-adenosylmethionine-dependent methylation. (elsevier.com)
this suggests that EHNA's inhibition of PDE2, not its effects on adenosine metabolism, mediates its effects on NMDA-stimulated cGMP concentrations. (aspetjournals.org)
ADA inhibition is accompanied by a rise in intracellular deoxyadenosine triphosphate(dATP) and a depletion of adenosine triphosphate. (scialert.net)
Cultured leukemic T-lymphoblasts, incubated in the presence of inhibitors of adenosine deaminase, are exquisitely sensitive to growth inhibition by deoxyadenosine. (aacrjournals.org)
Inhibition of glycolysis by a novel EGFR/HER2 inhibitor KU004 suppresses the growth of HER2+ cancer. (bireme.br)
Alternatively, inhibition of DPP-IV-mediated incretin degradation represents a complementary therapeutic approach, as orally available DPP-IV inhibitors have been shown to lower glucose in experimental diabetic models and human subjects with type 2 diabetes. (diabetesjournals.org)

AMPD2 inhibitor 1 is an adenosine monophosphate deaminase 2 ( AMPD2 ) inhibitor, used in the research of sugar craving, salt craving, umami craving, and addictions including drug, tobacco, nicotine and alcohol addictions. (medchemexpress.com)
Interestingly, nuclease-mediated degradation of neutrophil NETs triggers the formation of deoxyadenosine monophosphate (dAMP), which is converted by S. aureus adenosine synthase A (AdsA) into deoxyadenosine (dAdo) ( 14 ). (pnas.org)
Hypoxia in vitro and in vivo decreased purine oxidation and enhanced purine salvage reactions in human and mouse red blood cells, which was partly explained by decreased adenosine monophosphate deaminase activity. (haematologica.org)
Nuclease digestion of NETs releases 5′- and 3′-monophosphate nucleotides that are converted by S. aureus adenosine synthase A (AdsA), a sortase-anchored surface protein, into deoxyadenosine (dAdo) ( 14 ). (asm.org)
The production of IMP is regulated by the enzyme adenosine monophosphate (AMP) deaminase which functions to convert AMP into IMP. (springer.com)
Adenosine plays an important role in biochemical processes, such as energy transfer - as adenosine triphosphate (ATP) and adenosine diphosphate (ADP) - as well as in signal transduction as cyclic adenosine monophosphate , cAMP. (bionity.com)
These include enzymes that convert ATP to ADP and ADP to AMP (NTPDase-1, also known as ATP diphosphohydrolase, CD 39 and EC 3.6.1.5), 13,14 ATP to AMP and ADP to AMP (5′-monophosphate phosphoanhydrolase/phosphodiesterase, NMPP), 15 and AMP to adenosine (5′-nucleotidase), 13 the latter being an inhibitor of platelet aggregation. (ahajournals.org)

Forodesine is a potent inhibitor of purine nucleoside phosphorylase that promotes apoptosis in T- and B- cells through intracellular accumulation of deoxyguanosine triphosphate. (medscape.com)
16 - 19 These observations, together with early depletion of high energy phosphate compounds, including adenosine triphosphate (ATP) and 2,3-diphosphoglycerate (2,3-DPG), prompted many to question whether the storage lesion compromises RBC transfusion safety and efficacy. (haematologica.org)
Objective- Effects on platelet aggregation of adenosine triphosphate (ATP) released from damaged cells and from platelets undergoing exocytosis have not been clearly established. (ahajournals.org)
Large quantities of adenosine triphosphate (ATP) and adenosine diphosphate (ADP) are present in erythrocytes, platelets, and other cells and tissues and can leave the cells via physical damage or exocytosis. (ahajournals.org)

due to the accumulation of adenosine resulting in severe combined immunodeficiency (SCID). (biologists.org)
For decades, physicians, patients, and their families have relied upon enzyme replacement therapy as a life-saving treatment for adenosine deaminase severe combined immunodeficiency, a disease in which the buildup of toxic metabolites can cripple children's immune systems," said Morna Dorsey, M.D., MMSc, Professor of Pediatrics at the University of California, San Francisco. (drugs.com)
Adenosine deaminase deficiency is a disorder of purine metabolism leading to severe combined immunodeficiency (ADA-SCID). (bloodjournal.org)

1-Deazaadenosine is a potent Adenosine deaminase (ADA) inhibitor with a K i value of 0.66 μM. (medchemexpress.com)
The purpose of the study was to profile host resistance to infection with this organism in mice exposed to 2-deoxycoformycin (2dCF), a potent adenosine deaminase (ADA) inhibitor. (epa.gov)

Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor . (medchemexpress.com)
During infection, staphylococcal nuclease and adenosine synthase A convert neutrophil extracellular traps to deoxyadenosine (dAdo), which kills phagocytes. (pnas.org)
During infection, S. aureus secretes nuclease (Nuc) and adenosine synthase A (AdsA) to generate cytotoxic deoxyadenosine (dAdo) from neutrophil extracellular traps which triggers noninflammatory apoptosis in macrophages. (asm.org)
8 ) that deoxyadenosine, the other substrate of ADA, rather than adenosine, was the toxic metabolite in this disease. (jimmunol.org)
Both thymocyte subpopulations elevated their dATP pools on incubation with μ M concentrations of deoxyadenosine in the presence of erythro-9-[3-(2-hydroxynonyl)]adenosine, an inhibitor of adenosine deaminase. (aacrjournals.org)
Furthermore, these nondividing peripheral blood lymphocytes were killed by μ M concentrations of deoxyadenosine in the presence of an inhibitor of adenosine deaminase. (aacrjournals.org)

EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2) ( IC 50 =4 μM) and adenosine deaminase (ADA) . (medchemexpress.com)
Discovery and development of nucleoside and nucleotide reverse-transcriptase inhibitors (NRTIs and NtRTIs) began in the 1980s when the AIDS epidemic hit Western societies. (wikipedia.org)
Antiretroviral drugs for the treatment of HIV infections belong to six categories: Nucleoside and nucleotide reverse-transcriptase inhibitors, Non-nucleoside reverse-transcriptase inhibitors, protease inhibitors, entry inhibitors, co-receptor inhibitors and integrase inhibitors. (wikipedia.org)
Since zidovudine was approved in 1987, six nucleosides and one nucleotide reverse-transcriptase inhibitor (NRTI) have been approved by FDA. (wikipedia.org)
NRTIs approved by the FDA are zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir and emtricitabine and the only nucleotide reverse-transcriptase inhibitor (NtRTI) approved is tenofovir (see table 4). (wikipedia.org)
Activation of nucleoside and nucleotide reverse-transcriptase inhibitors is primarily dependent on cellular entry by passive diffusion or carrier-mediated transport. (wikipedia.org)
Adenosine deaminase) * dNTP: nucleotide (purine) metabolism, may be involved in N (phosphohistidine) me. (openwetware.org)
This study highlights the changes in umami-related nucleotide and glutamate levels when the AMP deaminase gene was elevated in transgenic tomato. (springer.com)
Elevated AMP deaminase levels resulted in the reduced accumulation of glutamate and increased levels of the umami nucleotide GMP. (springer.com)

Therapeutic approaches for enhancing incretin action include degradation-resistant GLP-1 receptor agonists (incretin mimetics), and inhibitors of dipeptidyl peptidase-4 (DPP-4) activity (incretin enhancers). (nih.gov)

Among several differences between ADA1 and ADA2, two are relevant to their assay in clinical laboratories: the affinity of ADA1 for adenosine is 100-fold greater than that of ADA2, and ADA1 is inhibited by the analogue erythro-9-(2-hydroxy-3-nonyl)adenine (EHNA), but ADA2 is not. (bmj.com)
Two distinct adenosine deaminases, ADA1 and ADA2, are found in humans. (elsevier.com)

Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. (medchemexpress.com)

Dipyridamole, which inhibits adenosine uptake into erythrocytes, inhibited aggregation induced by ATP in whole blood, and adenosine deaminase reversed this. (ahajournals.org)

Selective failure of lymphoid development occurs in genetic deficiency of adenosine deaminase (ADA). (elsevier.com)
Deficiency of Adenosine deaminase 2 (DADA2) is a monogenic disease associated with systemic inflammation and vasculopathy that affects a wide variety of organs in different patients. (wikipedia.org)

The present study tested the hypothesis that ADA is inhibited by 1,3-DNB as a substrate mimic, thereby preventing adenosine catabolism. (nih.gov)
The PDE families are distinguished by their substrate specificity and characteristic regulation by inhibitors and activators. (aspetjournals.org)
These structural differences explain the substrate and inhibitor specificity of adenosine deaminases and provide the basis for a rational design of ADA2-targeting drugs to modulate the immune system responses in pathophysiological conditions. (elsevier.com)

In addition, exposure of DI TNC-1 astrocytes to 10-500 μM 1,3-DNB produced concentration-dependent increases in extracellular adenosine at 24 h. (nih.gov)
Overall, the results demonstrate that 1,3-DNB is a mixed inhibitor of ADA and may thus lead to increases in extracellular adenosine. (nih.gov)
Insulin also increases intracellular and decreases extracellular adenosine, counteracting the effect of oxidative stress. (diabetesjournals.org)
Extracellular adenosine under oxidative stress is largely inhibited after blockade of ecto-5′-nucleotidase, suggesting that extracellular adenosine results preferentially from ATP release and catabolism. (diabetesjournals.org)
Moreover, insulin appears to interfere with the ATP release induced by oxidative stress, regulating extracellular adenosine levels. (diabetesjournals.org)
ADO also has receptor-independent effects, because extracellular adenosine can cross the cell membrane and activate AMP-activated protein kinase (AMPK), adenosine kinase, and S-adenosyl homocysteine hydrolase pathways [ 2 ]. (hindawi.com)

EHNA hydrochloride is a specific inhibitor of adenosine deaminase , prevents dAdo degradation and increases mitochondrial dATP levels in fibroblasts. (medchemexpress.com)
Here we used CRISPR-Cas9 mutagenesis to show that phagocyte intoxication involves uptake of dAdo via the human equilibrative nucleoside transporter 1, dAdo conversion to dAMP by deoxycytidine kinase and adenosine kinase, and signaling via subsequent dATP formation to activate caspase-3-induced cell death. (pnas.org)
The mechanism of staphylococcal dAdo cytotoxicity was investigated using CRISPR/Cas9 mutagenesis to show that destruction of human U937 macrophages involves uptake of dAdo via the human equilibrative nucleoside transporter 1 (hENT1), dAdo conversion to dAMP by deoxycytidine kinase (DCK) and adenosine kinase (ADK), and subsequent dATP formation ( 17 ). (asm.org)

Coformycin, a nucleoside antibiotic, is a potent inhibitor of adenosine deaminase (ADA) from Streptomyces species. (medchemexpress.com)
Furthermore, the bilateral injection of adenosine or coformycin into the rat TMN increased NREM sleep, which was completely abolished by coadministration of 1,3-dimethyl-8-cyclopenthylxanthine, a selective A 1 R antagonist. (pnas.org)

Adenosine is an endogenous purine nucleoside that modulates many physiologic processes. (bionity.com)
2004. Adenosine: An endogenous regulator of innate immunity. (springer.com)
These results indicate that endogenous adenosine in the TMN suppresses the histaminergic system via A 1 R to promote NREM sleep. (pnas.org)

Adenosine deaminase (ADA) is an enzyme involved in purine metabolism. (medchemexpress.com)
Adenosine deaminase is considered one of the key enzymes of purine metabolism. (medchemexpress.com)
A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. (drugbank.ca)
Adenosine deaminase (ADA) deficiency is a rare inherited disorder of purine metabolism characterized by the accumulation of metabolic substrates that lead to abnormalities of immune system development and function and a variety of systemic defects. (bloodjournal.org)
We identify the third gene as Ampd2 , a liver isoform of AMP Deaminase ( Ampd ), a central component of energy and purine metabolism pathways. (biomedcentral.com)

Klahr S, Morrissey JJ (1997) Comparative study of ACE inhibitors and angiotensin II receptor antagonists in interstitial scarring. (springer.com)

The protein product of this gene, adenosine deaminase 2 (ADA2), is an extracellular enzyme that breaks down adenosine and may also serve as a growth factor. (wikipedia.org)
The abundance of adenosine deaminase was considerably down-regulated in diabetic myotubes and as the protein binds propyl dipeptidase (DPP-IV), we speculate whether the reduced binding of adenosine deaminase to DPP-IV may contribute to the diabetic phenotype in vivo by leading to a higher level of free DPP-IV to bind and inactivate the anti-diabetic hormones, glucagon-like peptide-1 and glucose-dependent insulintropic polypeptide. (mcponline.org)
Dipeptidyl peptidase-4 ( DPP4 ), also known as adenosine deaminase complexing protein 2 or CD26 ( cluster of differentiation 26) is a protein that, in humans, is encoded by the DPP4 gene . (wikipedia.org)
Adenosine A3 receptor (A3AR) is a G i -protein-coupled receptor that, when being activated, decreases intracellular cAMP levels [ 3 ]. (hindawi.com)

Adenosine Kinase Inhibitors. (patentgenius.com)

The racemic mixture of a cell-permeable adenine derivative that acts as a PDE II-selective phosphodiesterase inhibitor and adenosine deaminase. (emdmillipore.com)

Two new deaza analogues of erythro-9-(2-hydroxy-3-nonyl)adenine (EHNA, 1), 7-deaza-EHNA (6) and 1,3-dideaza-EHNA (11), were synthesized and evaluated for adenosine deaminase (ADA) inhibitory activity and compared with EHNA, 1-deaza-EHNA (2), and 3-deaza-EHNA (3). (nih.gov)
Substitution of a methine group for a nitrogen atom in the 7-position of the purine moiety of EHNA produces a dramatic drop in the inhibitory activity (Ki = 4 X 10(-4) M) whereas compounds 2 and 3 are still good inhibitors (Ki = 1.2 X 10(-7) M and 6.3 X 10(-9) M respectively). (nih.gov)
EHNA and 1-deaza-EHNA are equiactive as inhibitors of human respiratory syncytial virus (HRSV) replication (MIC = 6.25 micrograms/mL) while the other compounds are inactive. (nih.gov)
3-Deaza-EHNA, the most active inhibitor of ADA among the EHNA deaza analogues, greatly potentiates the antitumor activity of ara-A in vitro. (nih.gov)
In contrast, only the PDE2 inhibitor erythro -9-(2-hydroxy-3-nonyl) adenine (EHNA) enhanced the ability of NMDA to increase cGMP. (aspetjournals.org)
3 Plasma ADA2 activity is therefore performed at a saturating adenosine concentration that is ~10 000-fold higher than physiological, and in the presence of EHNA to inhibit ADA1. (bmj.com)

Rabbits were pretreated topically with the moderately selective adenosine A 1 antagonist 8-(p-sulfophenyl)theophyline (8-SPT) or the adenosine A 2 antagonist 3,7-dimethyl-l-propargylxanthine (DMPX). (arvojournals.org)

10,16 Also, adenosine can be taken up and neutralized by erythrocytes and other blood cells, thus limiting its potential inhibitory action. (ahajournals.org)
In addition, it also exhibited appropriate (μM) adenosine deaminase inhibitory potency. (eurekaselect.com)

We thank Gao and colleagues for their interest in our recent study on adenosine deaminase 2 (ADA2) as a biomarker of macrophage activation syndrome. (bmj.com)
1 In their letter, the authors demonstrated a strong correlation between total adenosine deaminase (tADA) and ADA2 levels in the peripheral blood of healthy controls and patients with immune-mediated diseases. (bmj.com)
The recently isolated ADA2 belongs to the novel family of adenosine deaminase growth factors (ADGFs), which play an important role in tissue development. (elsevier.com)

8-Azaadenosine is a potent ADAR1 ( adenosine deaminases acting on double-stranded RNA) inhibitor . (medchemexpress.com)
Here, through analysis of genome-scale loss-of-function datasets, we identify adenosine deaminase acting on RNA ( ADAR or ADAR1) as an essential gene for the survival of a subset of cancer cell lines. (nature.com)
We find that lung cancer cell lines expressing high levels of interferon-stimulated genes (ISGs) are vulnerable to deletion of the RNA adenosine deaminase, ADAR or ADAR1. (nature.com)

Measurements of purine metabolites in the body fluids of ADA-deficient patients showed elevated levels of adenosine ( 3 ), one of the two substrates for ADA. (jimmunol.org)

Vorinostat is a histone deacetylase (HDAC) inhibitor. (medscape.com)

Methods and Results- Aggregation, measured using a platelet-counting technique, occurred in response to ATP and was maximal at 10 to 100 μmol/L. It was abolished by MRS2179, AR-C69931, and creatine phosphate/creatine phosphokinase, implying that conversion to adenosine diphosphate (ADP) is required. (ahajournals.org)

Dipeptidyl peptidase-4 (DDP4) inhibitors target the enzymatic degradation of incretin peptides and represent a major advance in the treatment of type 2 diabetes. (diabetesjournals.org)
A class of oral hypoglycemics called dipeptidyl peptidase-4 inhibitors work by inhibiting the action of this enzyme, thereby prolonging incretin effect in vivo. (wikipedia.org)
The objective of this study is to compare the risk of serious adverse events associated with the use of sodium-glucose cotransporter 2 (SGLT2) inhibitors in comparison with the use of dipeptidyl peptidase-4 (DPP-4) inhibitors among patients with type 2 diabetes. (bioportfolio.com)
OBJECTIVE -To examine the mechanisms of action, therapeutic potential, and challenges inherent in the use of incretin peptides and dipeptidyl peptidase-IV (DPP-IV) inhibitors for the treatment of type 2 diabetes. (diabetesjournals.org)

Cladribine is an adenosine deaminase inhibitor used to treat hairy cell leukemia and multiple sclerosis. (medchemexpress.com)

These genes included SMARCA2 and PRKDC 7 , 8 , which have been shown to be synthetic lethal targets in subsets of lung cancers, as well as the adenosine deaminase acting on RNA gene, ADAR . (nature.com)
The roles of the double stranded RNA specific ADAR (Adenosine DeAminase that act on RNA) family members (ADARs) and the altered gene specific editing patterns were investigated in clinical specimens, cell models and mice. (bmj.com)
2008. A2B adenosine receptor gene deletion attenuates murine colitis. (springer.com)

Adenosine is a nucleoside composed of adenine attached to a ribose (ribofuranose) moiety via a β-N 9 - glycosidic bond . (bionity.com)

In addition, the company develops PEGylated adenosine deaminase 2, an immune checkpoint inhibitor that targets adenosine. (yahoo.com)
CD39 and CD73 have been recently proposed as novel checkpoint inhibitor targets, since ADO generated by these ectonucleotidases interferes with antitumor immune responses [ 8 ]. (hindawi.com)

The first nucleoside reverse-transcriptase inhibitor with in vitro anti-HIV activity was zidovudine. (wikipedia.org)
We discover here a setup that requires both oxygenation of the tissue and adenosine deaminase activity in the medium, and supports both growth and proliferation of wing discs for 9 h. (biologists.org)
The combination of growth and proliferation requires oxygenation of the discs, as well as adenosine deaminase activity in the medium. (biologists.org)
RDC8 codes for an adenosine A2 receptor with physiological constitutive activity. (nih.gov)
Thus, in regards to stress or injury, the function of adenosine is primarily that of cytoprotection preventing tissue damage during instances of hypoxia, ischemia , and seizure activity. (bionity.com)

Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3). (bionity.com)

Vasodilators, anticoagulants and inhibitors of platelet aggregation are part of this salivary mixture ( Ribeiro and Francischetti, 2003 ). (biologists.org)

Orally administered DPP-4 inhibitors, such as sitagliptin and vildagliptin, reduce HbA1c by 0.5-1.0%, with few adverse events and no weight gain. (nih.gov)

9 10 However, recent work has concluded that only 50% of the epinephrine-induced increase in outflow facility can be blocked by the use of cyclooxygenase inhibitors. (arvojournals.org)

Dancer JE, Hughes R, Lindell SD (1997) Adenosine-5′-phosphate deaminase (A novel herbicide target). (springer.com)

Adenosine deaminase (ADA) inhibitors have been found to have antitumor activities. (eurekaselect.com)
Here, thirteen potential adenosine deaminase inhibitors 5-amino-1H-pyrazole-4-carboxamide derivatives were designed, synthesized and screened for antitumor activities. (eurekaselect.com)

Adenosine deaminase in humans is involved in the development and maintenance of the immune system. (medchemexpress.com)
Topical administration of adenosine for use in wound healing deficiencies and diabetes mellitus in humans is currently under clinical investigation. (bionity.com)

Investigators quickly showed that adenosine could slow the growth of lymphoid cell lines and the mitogen-induced proliferation of primary lymphocytes ( 3 ). (jimmunol.org)
Adenosine deaminase is concentrated in lymphoid tissue, including both T and B lymphocytes. (cancernetwork.com)
These findings provide impetus for the investigation of adenosine deaminase inhibitors as lympholytic immunosuppressants or as agents cytotoxic to noncycling malignant lymphoid cells. (aacrjournals.org)

Selective inhibitors of the two PDE families will differentially affect the functional consequences of activation of these two signaling pathways by NMDA receptor stimulation. (aspetjournals.org)

Dipyridamole, an adenosine uptake inhibitor, was obtained from Boehringer Ingelheim. (ahajournals.org)

GAITHERSBURG, Md.--(BUSINESS WIRE) October 05, 2018 --Leadiant Biosciences, Inc. today announced that the Food and Drug Administration (FDA) has granted approval to Revcovi™ (elapegademase-lvlr) injection in the U.S. Revcovi is a new enzyme replacement therapy (ERT) for the treatment of adenosine deaminase severe combined immune deficiency (ADA-SCID) in pediatric and adult patients. (drugs.com)

From this source population, a study-specific cohort including all new users of SGLT2 inhibitors or DPP-4 inhibitors between January 1, 2013 and June 30, 2018 (or latest date of data availability at each site) will be created for each safety outcome. (bioportfolio.com)

Anatomy4

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Diseases7

Chemicals and Drugs28

Analytical, Diagnostic and Therapeutic Techniques and Equipment2

Phenomena and Processes1

Disciplines and Occupations1

Information Science4

The extracellular versus intracellular mechanisms of inhibition of TCR-triggered activation in thymocytes by adenosine under conditions of inhibited adenosine deaminase. (1/193)

Nucleotide pool imbalance and adenosine deaminase deficiency induce alterations of N-region insertions during V(D)J recombination. (2/193)

Quantification of extracellular and intracellular adenosine production: understanding the transmembranous concentration gradient. (3/193)

Diinosine pentaphosphate (IP5I) is a potent antagonist at recombinant rat P2X1 receptors. (4/193)

The anticonvulsant BW534U87 depresses epileptiform activity in rat hippocampal slices by an adenosine-dependent mechanism and through inhibition of voltage-gated Na+ channels. (5/193)

A normal level of adenosine deaminase activity in the red cell lysates of carriers and patients with severe combined immunodeficiency disease. (6/193)

Age-related changes in A(1)-adenosine receptor-mediated bradycardia. (7/193)

Adenosine-mediated killing of cultured epithelial cancer cells. (8/193)

Adenosine Deaminase Inhibitors

Coformycin

Pentostatin

Adenosine Deaminase

Nucleoside Deaminases

Adenosine

Ribonucleosides

Deoxyadenosines

Adenosine Kinase

Adenine

Inosine

Tubercidin

Tetrahydrouridine

Vidarabine

Adenosylhomocysteinase

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AMP Deaminase

Deamination

Receptor, Adenosine A2A

Receptor, Adenosine A1

Cytidine Deaminase

Receptor, Adenosine A3

Cytosine Deaminase

Cells, Cultured

DCMP Deaminase

Receptor, Adenosine A2B

Guanine Deaminase

Psoriasis

T-Lymphocytes

Epidermis

Lithospermum

Phlebotomus

Psychodidae

Culex

Insect Proteins

Apyrase

Salivary Glands

Lymphoma, T-Cell, Cutaneous

Lymphoma, T-Cell

Sezary Syndrome

Mycosis Fungoides

Lymphoma

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Chromatography, Affinity

Books

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The extracellular versus intracellular mechanisms of inhibition of TCR-triggered activation in thymocytes by adenosine under conditions of inhibited adenosine deaminase. (1/193)

Nucleotide pool imbalance and adenosine deaminase deficiency induce alterations of N-region insertions during V(D)J recombination. (2/193)

Quantification of extracellular and intracellular adenosine production: understanding the transmembranous concentration gradient. (3/193)

Diinosine pentaphosphate (IP5I) is a potent antagonist at recombinant rat P2X1 receptors. (4/193)

The anticonvulsant BW534U87 depresses epileptiform activity in rat hippocampal slices by an adenosine-dependent mechanism and through inhibition of voltage-gated Na+ channels. (5/193)

A normal level of adenosine deaminase activity in the red cell lysates of carriers and patients with severe combined immunodeficiency disease. (6/193)

Age-related changes in A(1)-adenosine receptor-mediated bradycardia. (7/193)

Adenosine-mediated killing of cultured epithelial cancer cells. (8/193)

Conversion of a stem cell leukemia from a T-lymphoid to a myeloid phenotype induced by the adenosine deaminase inhibitor 2...

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