A subtype of equilibrative nucleoside transporter proteins that is sensitive to inhibition by 4-nitrobenzylthioinosine.
A subtype of equilibrative nucleoside transporter proteins that is insensitive to inhibition by 4-nitrobenzylthioinosine.
Proteins involved in the transport of NUCLEOSIDES across cellular membranes.
Sulfhydryl analog of INOSINE that inhibits nucleoside transport across erythrocyte plasma membranes, and has immunosuppressive properties. It has been used similarly to MERCAPTOPURINE in the treatment of leukemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p503)
A class of sodium-independent nucleoside transporters that mediate the facilitative transport of NUCLEOSIDES.
Coronary vasodilator with some antiarrhythmic activity.
Purine or pyrimidine bases attached to a ribose or deoxyribose. (From King & Stansfield, A Dictionary of Genetics, 4th ed)
Pyrazolopyrimidine ribonucleosides isolated from Nocardia interforma. They are antineoplastic antibiotics with cytostatic properties.
Uridine is a nucleoside, specifically a derivative of pyrimidine, that is composed of a uracil molecule joined to a ribose sugar molecule through a β-N1 glycosidic bond, and has significant roles in RNA synthesis, energy transfer, and cell signaling.
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.
A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)
Purines with a RIBOSE attached that can be phosphorylated to PURINE 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)
Membrane proteins whose primary function is to facilitate the transport of molecules across a biological membrane. Included in this broad category are proteins involved in active transport (BIOLOGICAL TRANSPORT, ACTIVE), facilitated transport and ION CHANNELS.
Proteins involved in the transport of nucleobases such as PYRIMIDINES and PURINES across membranes.
The movement of materials (including biochemical substances and drugs) through a biological system at the cellular level. The transport can be across cell membranes and epithelial layers. It also can occur within intracellular compartments and extracellular compartments.
A purine nucleoside that has guanine linked by its N9 nitrogen to the C1 carbon of ribose. It is a component of ribonucleic acid and its nucleotides play important roles in metabolism. (From Dorland, 28th ed)
Agents that affect ION PUMPS; ION CHANNELS; ABC TRANSPORTERS; and other MEMBRANE TRANSPORT PROTEINS.
A purine and a reaction intermediate in the metabolism of adenosine and in the formation of nucleic acids by the salvage pathway.
An enzyme that catalyzes reversibly the phosphorylation of deoxycytidine with the formation of a nucleoside diphosphate and deoxycytidine monophosphate. Cytosine arabinoside can also act as an acceptor. All natural nucleoside triphosphates, except deoxycytidine triphosphate, can act as donors. The enzyme is induced by some viruses, particularly the herpes simplex virus (HERPESVIRUS HOMINIS). EC 2.7.1.74.
A pyrimidine nucleoside formed in the body by the deamination of CYTARABINE.
Transport proteins that carry specific substances in the blood or across cell membranes.
Deoxycytidine is a nucleoside consisting of the pentose sugar deoxyribose linked to the nitrogenous base cytosine, which plays a crucial role in DNA replication and repair processes within cells.
Analogs of those substrates or compounds which bind naturally at the active sites of proteins, enzymes, antibodies, steroids, or physiological receptors. These analogs form a stable covalent bond at the binding site, thereby acting as inhibitors of the proteins or steroids.
A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.
Antimetabolites that are useful in cancer chemotherapy.
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).
The rate dynamics in chemical or physical systems.
Pyrimidines with a RIBOSE attached that can be phosphorylated to PYRIMIDINE NUCLEOTIDES.
Female germ cells derived from OOGONIA and termed OOCYTES when they enter MEIOSIS. The primary oocytes begin meiosis but are arrested at the diplotene state until OVULATION at PUBERTY to give rise to haploid secondary oocytes or ova (OVUM).
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 commonest and widest ranging species of the clawed "frog" (Xenopus) in Africa. This species is used extensively in research. There is now a significant population in California derived from escaped laboratory animals.
Benzothiepins is a class of heterocyclic compounds that have been used in the development of various therapeutic drugs, particularly those with antipsychotic and anti-inflammatory properties, although none are currently in clinical use due to their significant side effects.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
2-Chloroadenosine. A metabolically stable analog of adenosine which acts as an adenosine receptor agonist. The compound has a potent effect on the peripheral and central nervous system.
An enzyme of the oxidoreductase class that catalyzes the formation of 2'-deoxyribonucleotides from the corresponding ribonucleotides using NADPH as the ultimate electron donor. The deoxyribonucleoside diphosphates are used in DNA synthesis. (From Dorland, 27th ed) EC 1.17.4.1.
Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.
General term for the abnormal appearance of histiocytes in the blood. Based on the pathological features of the cells involved rather than on clinical findings, the histiocytic diseases are subdivided into three groups: HISTIOCYTOSIS, LANGERHANS CELL; HISTIOCYTOSIS, NON-LANGERHANS-CELL; and HISTIOCYTIC DISORDERS, MALIGNANT.
An aquatic genus of the family, Pipidae, occurring in Africa and distinguished by having black horny claws on three inner hind toes.
Established cell cultures that have the potential to propagate indefinitely.
Proteins found in any species of protozoan.
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.

Nucleoside transport in human colonic epithelial cell lines: evidence for two Na+-independent transport systems in T84 and Caco-2 cells. (1/46)

RT-PCR of RNA isolated from monolayers of the human colonic epithelial cell lines T84 and Caco-2 demonstrated the presence of mRNA for the two cloned Na+-independent equilibrative nucleoside transporters, ENT1 and ENT2, but not for the cloned Na+-dependent concentrative nucleoside transporters, CNT1 and CNT2. Uptake of [3H]uridine by cell monolayers in balanced Na+-containing and Na+-free media confirmed the presence of only Na+-independent nucleoside transport mechanisms. This uptake was decreased by 70-75% in the presence of 1 microM nitrobenzylthioinosine, a concentration that completely inhibits ENT1, and was completely blocked by the addition of 10 microM dipyridamole, a concentration that inhibits both ENT1 and ENT2. These findings indicate the presence in T84 and Caco-2 cells of two functional Na+-independent equilibrative nucleoside transporters, ENT1 and ENT2.  (+info)

Kinetic and pharmacological properties of cloned human equilibrative nucleoside transporters, ENT1 and ENT2, stably expressed in nucleoside transporter-deficient PK15 cells. Ent2 exhibits a low affinity for guanosine and cytidine but a high affinity for inosine. (2/46)

We stably transfected the cloned human equilibrative nucleoside transporters 1 and 2 (hENT1 and hENT2) into nucleoside transporter-deficient PK15NTD cells. Although hENT1 and hENT2 are predicted to be 50-kDa proteins, hENT1 runs as 40 kDa and hENT2 migrates as 50 and 47 kDa on SDS-polyacrylamide gel electrophoresis. Peptide N-glycosidase F and endoglycosidase H deglycosylate hENT1 to 37 kDa and hENT2 to 45 kDa. With hENT1 being more sensitive, there is a 7000-fold and 71-fold difference in sensitivity to nitrobenzylthioinosine (NBMPR) (IC(50), 0.4 +/- 0.1 nM versus 2.8 +/- 0.3 microM) and dipyridamole (IC(50), 5.0 +/- 0.9 nM versus 356 +/- 13 nM), respectively. [(3)H]NBMPR binds to ENT1 cells with a high affinity K(d) of 0.377 +/- 0.098 nM, and each ENT1 cell has 34,000 transporters with a turnover number of 46 molecules/s for uridine. Although both transporters are broadly selective, hENT2 is a generally low affinity nucleoside transporter with 2.6-, 2.8-, 7. 7-, and 19.3-fold lower affinity than hENT1 for thymidine, adenosine, cytidine, and guanosine, respectively. In contrast, the affinity of hENT2 for inosine is 4-fold higher than hENT1. The nucleobase hypoxanthine inhibits [(3)H]uridine uptake by hENT2 but has minimal effect on hENT1. Taken together, these results suggest that hENT2 might be important in transporting adenosine and its metabolites (inosine and hypoxanthine) in tissues such as skeletal muscle where ENT2 is predominantly expressed.  (+info)

Retroviral transfer of the hENT2 nucleoside transporter cDNA confers broad-spectrum antifolate resistance in murine bone marrow cells. (3/46)

Antifolate drugs such as methotrexate are commonly used in cancer chemotherapy. It may be possible to increase the antitumor activity of antifolates by the coadministration of drugs that inhibit nucleoside transport, thereby blocking the capacity of tumor cells to salvage nucleotide precursors. An important limitation of this approach is severe myelosuppression caused by many of these drug combinations. For this reason, we have developed a gene therapy strategy to protect bone marrow cells against combined treatment with antifolates and nitrobenzylmercaptopurine riboside (NBMPR), a potent inhibitor of the es nucleoside transporter. A retroviral vector (MeiIRG) was constructed that expressed the NBMPR-insensitive ei transporter, hypothesizing that transduced bone marrow cells would survive drug treatment because of the preservation of nucleoside salvage pathways. In vitro clonogenic assays confirmed that the MeiIRG vector did protect myeloid progenitors against the toxic effects of 3 different antifolates when each was combined with NBMPR. On testing this system in vivo, decreased myelosuppression was observed in mice transplanted with MeiIRG-transduced bone marrow cells and subsequently treated with trimetrexate and NBMPR-P. In these mice, significant increases were noted in absolute neutrophil count nadirs, reticulocyte indices, and the numbers of myeloid progenitors in the bone marrow. Furthermore, a survival advantage was associated with transfer of the MeiIRG vector, indicating that significant dose intensification was possible with this approach. In summary, the MeiIRG vector can decrease the toxicity associated with the combined use of antifolates and NBMPR-P and thereby may provide a strategy for simultaneously sensitizing tumor cells while protecting hematopoietic cells.  (+info)

Molecular cloning and functional characterization of inhibitor-sensitive (mENT1) and inhibitor-resistant (mENT2) equilibrative nucleoside transporters from mouse brain. (4/46)

Mammalian cells express at least two subtypes of equilibrative nucleoside transporters, i.e. ENT1 and ENT2, which can be distinguished functionally by their sensitivity and resistance respectively to inhibition by nitrobenzylthioinosine. The ENT1 transporters exhibit distinctive species differences in their sensitivities to inhibition by dipyridamole, dilazep and draflazine (human>mouse>rat). A comparison of the ENT1 structures in the three species would facilitate the identification of the regions involved in the actions of these cardioprotective agents. We now report the molecular cloning and functional expression of the murine (m)ENT1 and mENT2 transporters. mENT1 and mENT2 encode proteins containing 458 and 456 residues respectively, with a predicted 11-transmembrane-domain topology. mENT1 has 88% and 78% amino acid identity with rat ENT1 and human ENT1 respectively; mENT2 is more highly conserved, with 94% and 88% identity with rat ENT2 and human ENT2 respectively. We have also isolated two additional distinct cDNAs that encode proteins similar to mENT1; these probably represent distinct mENT1 isoforms or alternative splicing products. One cDNA encodes a protein with two additional amino acids (designated mENT1b) that adds a potential protein kinase CK2 phosphorylation site in the central intracellular loop of the transporter, and is similar, in this regard, to the human and rat ENT1 orthologues. The other cDNA has a 5'-untranslated region sequence that is distinct from that of full-length mENT1. Microinjection of mENT1, mENT1b or mENT2 cRNA into Xenopus oocytes resulted in enhanced uptake of [(3)H]uridine by the oocytes relative to that seen in water-injected controls. mENT1-mediated, but not mENT2-mediated, [(3)H]uridine uptake was inhibited by nitrobenzylthioinosine and dilazep. Dipyridamole inhibited both mENT1 and mENT2, but was significantly more effective against mENT1. Adenosine inhibited both systems with a similar potency, as did a range of other purine and pyrimidine nucleosides. These results are compatible with the known characteristics of the native mENT1 and mENT2 transporters.  (+info)

Identification of Cys140 in helix 4 as an exofacial cysteine residue within the substrate-translocation channel of rat equilibrative nitrobenzylthioinosine (NBMPR)-insensitive nucleoside transporter rENT2. (5/46)

The human and rat equilibrative nucleoside transporter proteins hENT1, rENT1, hENT2 and rENT2 belong to a family of integral membrane proteins with 11 potential transmembrane segments (TMs), and are distinguished functionally by differences in transport of nucleobases and sensitivity to inhibition by nitrobenzylthioinosine (NBMPR) and vasoactive drugs. In the present study, we have produced recombinant hENT1, rENT1, hENT2 and rENT2 in Xenopus oocytes and investigated uridine transport following exposure to the impermeant thiol-reactive reagent p-chloromercuriphenyl sulphonate (PCMBS). PCMBS caused reversible inhibition of uridine influx by rENT2, but had no effect on hENT1, hENT2 or rENT1. This difference correlated with the presence in rENT2 of a unique Cys residue (Cys(140)) in the outer half of TM4 that was absent from the other ENTs. Mutation of Cys(140) to Ser produced a functional protein (rENT2/C140S) that was insensitive to inhibition by PCMBS, identifying Cys(140) as the exofacial Cys residue in rENT2 responsible for PCMBS inhibition. Uridine protected wild-type rENT2 against PCMBS inhibition, suggesting that Cys(140) in TM4 lies within or is closely adjacent to the substrate-translocation channel of the transporter. TM4 has been shown previously to be within a structural domain (TMs 3-6) responsible for interactions with NBMPR, vasoactive drugs and nucleobases.  (+info)

Characterization of nucleoside transport systems in cultured rat epididymal epithelium. (6/46)

The nucleoside transport systems in cultured epididymal epithelium were characterized and found to be similar between the proximal (caput and corpus) and distal (cauda) regions of the epididymis. Functional studies revealed that 70% of the total nucleoside uptake was Na(+) dependent, while 30% was Na(+) independent. The Na(+)-independent nucleoside transport was mediated by both the equilibrative nitrobenzylthioinosine (NBMPR)-sensitive system (40%) and the NBMPR-insensitive system (60%), which was supported by a biphasic dose response to NBMPR inhibition. The Na(+)-dependent [(3)H]uridine uptake was selectively inhibited 80% by purine nucleosides, indicating that the purine nucleoside-selective N1 system is predominant. Since Na(+)-dependent [(3)H]guanosine uptake was inhibited by thymidine by 20% and Na(+)-dependent [(3)H]thymidine uptake was broadly inhibited by purine and pyrimidine nucleosides, this suggested the presence of the broadly selective N3 system accounting for 20% of Na(+)-dependent nucleoside uptake. Results of RT-PCR confirmed the presence of mRNA for equilibrative nucleoside transporter (ENT) 1, ENT2, and concentrative nucleoside transporter (CNT) 2 and the absence of CNT1. It is suggested that the nucleoside transporters in epididymis may be important for sperm maturation by regulating the extracellular concentration of adenosine in epididymal plasma.  (+info)

Nucleoside transporter subtype expression: effects on potency of adenosine kinase inhibitors. (7/46)

1. Adenosine kinase (AK) inhibitors can enhance adenosine levels and potentiate adenosine receptor activation. As the AK inhibitors 5' iodotubercidin (ITU) and 5-amino-5'-deoxyadenosine (NH(2)dAdo) are nucleoside analogues, we hypothesized that nucleoside transporter subtype expression can affect the potency of these inhibitors in intact cells. 3. Three nucleoside transporter subtypes that mediate adenosine permeation of rat cells have been characterized and cloned: equilibrative transporters rENT1 and rENT2 and concentrative transporter rCNT2. We stably transfected rat C6 glioma cells, which express rENT2 nucleoside transporters, with rENT1 (rENT1-C6 cells) or rCNT2 (rCNT2-C6 cells) nucleoside transporters. 3. We tested the effects of ITU and NH(2)dAdo on [(3)H]-adenosine uptake and conversion to [(3)H]-adenine nucleotides in the three cell types. NH(2)dAdo did not show any cell type selectivity. In contrast, ITU showed significant inhibition of [(3)H]-adenosine uptake and [(3)H]-adenine nucleotide formation at concentrations < or =100 nM in rENT1-C6 cells, while concentrations > or =3 microM were required for C6 or rCNT2-C6 cells. 4. Nitrobenzylthioinosine (NBMPR; 100 nM), a selective inhibitor of rENT1, abolished the effects of nanomolar concentrations of ITU in rENT1-C6 cells. 5. This study demonstrates that the effects of ITU, but not NH(2)dAdo, in whole cell assays are dependent upon nucleoside transporter subtype expression. Thus, cellular and tissue differences in expression of nucleoside transporter subtypes may affect the pharmacological actions of some AK inhibitors.  (+info)

Mutation of residue 33 of human equilibrative nucleoside transporters 1 and 2 alters sensitivity to inhibition of transport by dilazep and dipyridamole. (8/46)

Human equilibrative nucleoside transporters (hENT) 1 and 2 differ in that hENT1 is inhibited by nanomolar concentrations of dipyridamole and dilazep, whereas hENT2 is 2 and 3 orders of magnitude less sensitive, respectively. When a yeast expression plasmid containing the hENT1 cDNA was randomly mutated and screened by phenotypic complementation in Saccharomyces cerevisiae to identify mutants with reduced sensitivity to dilazep, clones with a point mutation that converted Met33 to Ile (hENT1-M33I) were obtained. Characterization of the mutant protein in S. cerevisiae and Xenopus laevis oocytes revealed that the mutant had less than one-tenth the sensitivity to dilazep and dipyridamole than wild type hENT1, with no change in nitrobenzylmercaptopurine ribonucleoside (NBMPR) sensitivity or apparent uridine affinity. To determine whether the reciprocal mutation in hENT2 (Ile33 to Met) also altered sensitivity to dilazep and dipyridamole, hENT2-I33M was created by site-directed mutagenesis. Although the resulting mutant (hENT2-I33M) displayed >10-fold higher dilazep and dipyridamole sensitivity and >8-fold higher uridine affinity compared with wild type hENT2, it retained insensitivity to NBMPR. These data established that mutation of residue 33 (Met versus Ile) of hENT1 and hENT2 altered the dilazep and dipyridamole sensitivities in both proteins, suggesting that a common region of inhibitor interaction has been identified.  (+info)

Equilibrative Nucleoside Transporter 1 (ENT1), also known as SLC29A1, is a protein that functions as a membrane transport protein. It is responsible for the facilitated diffusion of nucleosides and some related drugs across the cell membrane. The term "equilibrative" refers to the fact that this transporter moves substrates down their concentration gradient, meaning it facilitates the movement of molecules from an area of high concentration to an area of low concentration. ENT1 is widely expressed in various tissues, including the liver, kidney, intestine, and brain, playing a crucial role in nucleoside homeostasis and the cellular uptake of nucleoside-analog drugs used in cancer chemotherapy.

Equilibrative Nucleoside Transporter 2 (ENT2) is a type of protein found in the cell membrane that facilitates the bidirectional transport of nucleosides, which are the building blocks of DNA and RNA, between the intracellular and extracellular spaces. ENT2 is a member of the solute carrier 29 (SLC29) family of transporters and is widely expressed in various tissues, including the brain, liver, kidney, and intestine.

ENT2 plays an essential role in maintaining nucleoside homeostasis by regulating their uptake and efflux across the cell membrane. It has a high affinity for purine nucleosides such as adenosine and guanosine, and to a lesser extent, pyrimidine nucleosides such as uridine and thymidine. The activity of ENT2 is critical in regulating extracellular adenosine levels, which have important implications for various physiological processes, including neurotransmission, inflammation, and cancer.

In addition to its role in nucleoside transport, ENT2 has been implicated in the development of drug resistance in cancer cells. Certain chemotherapeutic agents, such as nucleoside analogs, utilize ENT2 for their uptake into cells. However, overexpression of ENT2 in cancer cells can lead to increased efflux of these drugs, resulting in reduced intracellular concentrations and decreased therapeutic effectiveness. Therefore, ENT2 is an attractive target for the development of novel strategies to overcome drug resistance in cancer therapy.

Nucleoside transport proteins (NTTs) are membrane-bound proteins responsible for the facilitated diffusion of nucleosides and related deoxynucleosides across the cell membrane. These proteins play a crucial role in the uptake of nucleosides, which serve as precursors for DNA and RNA synthesis, as well as for the salvage of nucleotides in the cell.

There are two main types of NTTs: concentrative (or sodium-dependent) nucleoside transporters (CNTs) and equilibrative (or sodium-independent) nucleoside transporters (ENTs). CNTs mainly facilitate the uptake of nucleosides against a concentration gradient, using the energy derived from the sodium ion gradient. In contrast, ENTs mediate bidirectional transport, allowing for the equalization of intracellular and extracellular nucleoside concentrations.

Nucleoside transport proteins have been identified in various organisms, including humans, and are involved in numerous physiological processes, such as cell proliferation, differentiation, and survival. Dysregulation of NTTs has been implicated in several pathological conditions, including cancer and viral infections, making them potential targets for therapeutic intervention.

Thioinosine is not a medical term itself, but it is a chemical compound that has been studied in the field of medical research. Thioinosine is an analogue of the nucleoside inosine, where the oxygen atom in the heterocyclic ring is replaced by a sulfur atom.

In the context of medical research, thioinosine has been investigated for its potential immunomodulatory and antiviral properties. It has been studied as an inhibitor of certain enzymes involved in the replication of viruses, such as HIV and hepatitis C virus. However, it is not currently approved for use as a medication in clinical practice.

Equilibrative nucleoside transport proteins (ENTs) are a type of membrane transporter that regulate the bidirectional movement of nucleosides across the cell membrane. They facilitate the diffusion of nucleosides down their concentration gradient, hence the term "equilibrative." These transport proteins play a crucial role in maintaining intracellular nucleoside concentrations and ensuring proper nucleotide synthesis for various cellular processes, including DNA replication, repair, and gene expression. There are two major families of ENTs: the human equilibrative nucleoside transporters (hENTs) and the concentrative nucleoside transporters (CNTs). The hENT family includes four members (hENT1-4), while the CNT family consists of three members (CNT1-3). These transport proteins have been identified as potential targets for cancer therapy, as inhibiting their function can selectively sensitize tumor cells to nucleoside analog-based chemotherapies.

Dilazep is a medication that belongs to a class of drugs called calcium channel blockers. It is primarily used in the management of angina pectoris, which is chest pain caused by reduced blood flow to the heart muscle. Dilazep works by relaxing and widening the blood vessels that supply the heart, thereby improving blood flow and reducing the workload on the heart.

The chemical name for Dilazep is (E)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid diamide. It is not commonly used in many countries, and other calcium channel blockers such as verapamil, nifedipine, and amlodipine are more frequently prescribed for the treatment of angina pectoris.

It's important to note that like all medications, Dilazep can have side effects, including headache, dizziness, and swelling in the extremities. It should be used under the close supervision of a healthcare provider, who can monitor its effectiveness and potential side effects.

A nucleoside is a biochemical molecule that consists of a pentose sugar (a type of simple sugar with five carbon atoms) covalently linked to a nitrogenous base. The nitrogenous base can be one of several types, including adenine, guanine, cytosine, thymine, or uracil. Nucleosides are important components of nucleic acids, such as DNA and RNA, which are the genetic materials found in cells. They play a crucial role in various biological processes, including cell division, protein synthesis, and gene expression.

Formycins are a group of antibiotics that are derived from certain strains of Streptomyces bacteria. They include formycin B (also known as pyrazofurin), which is an antiviral and antimetabolite drug that works by interfering with the production of genetic material in cells. Formycins are not widely used in clinical medicine due to their potential toxicity and the availability of other effective antibiotics and antiviral drugs.

Uridine is a nucleoside that consists of a pyrimidine base (uracil) linked to a pentose sugar (ribose). It is a component of RNA, where it pairs with adenine. Uridine can also be found in various foods such as beer, broccoli, yeast, and meat. In the body, uridine can be synthesized from orotate or from the breakdown of RNA. It has several functions, including acting as a building block for RNA, contributing to energy metabolism, and regulating cell growth and differentiation. Uridine is also available as a dietary supplement and has been studied for its potential benefits in various health conditions.

Adenosine is a purine nucleoside that is composed of a sugar (ribose) and the base adenine. It plays several important roles in the body, including serving as a precursor for the synthesis of other molecules such as ATP, NAD+, and RNA.

In the medical context, adenosine is perhaps best known for its use as a pharmaceutical agent to treat certain cardiac arrhythmias. When administered intravenously, it can help restore normal sinus rhythm in patients with paroxysmal supraventricular tachycardia (PSVT) by slowing conduction through the atrioventricular node and interrupting the reentry circuit responsible for the arrhythmia.

Adenosine can also be used as a diagnostic tool to help differentiate between narrow-complex tachycardias of supraventricular origin and those that originate from below the ventricles (such as ventricular tachycardia). This is because adenosine will typically terminate PSVT but not affect the rhythm of VT.

It's worth noting that adenosine has a very short half-life, lasting only a few seconds in the bloodstream. This means that its effects are rapidly reversible and generally well-tolerated, although some patients may experience transient symptoms such as flushing, chest pain, or shortness of breath.

Dipyridamole is a medication that belongs to a class of drugs called antiplatelet agents. It works by preventing platelets in your blood from sticking together to form clots. Dipyridamole is often used in combination with aspirin to prevent stroke and other complications in people who have had a heart valve replacement or a type of irregular heartbeat called atrial fibrillation.

Dipyridamole can also be used as a stress agent in myocardial perfusion imaging studies, which are tests used to evaluate blood flow to the heart. When used for this purpose, dipyridamole is given intravenously and works by dilating the blood vessels in the heart, allowing more blood to flow through them and making it easier to detect areas of reduced blood flow.

The most common side effects of dipyridamole include headache, dizziness, and gastrointestinal symptoms such as diarrhea, nausea, and vomiting. In rare cases, dipyridamole can cause more serious side effects, such as allergic reactions, abnormal heart rhythms, or low blood pressure. It is important to take dipyridamole exactly as directed by your healthcare provider and to report any unusual symptoms or side effects promptly.

Purine nucleosides are fundamental components of nucleic acids, which are the genetic materials found in all living organisms. A purine nucleoside is composed of a purine base (either adenine or guanine) linked to a sugar molecule, specifically ribose in the case of purine nucleosides.

The purine base and sugar moiety are joined together through a glycosidic bond at the 1' position of the sugar. These nucleosides play crucial roles in various biological processes, including energy transfer, signal transduction, and as precursors for the biosynthesis of DNA and RNA.

In the human body, purine nucleosides can be derived from the breakdown of endogenous nucleic acids or through the dietary intake of nucleoproteins. They are further metabolized to form uric acid, which is eventually excreted in the urine. Elevated levels of uric acid in the body can lead to the formation of uric acid crystals and contribute to the development of gout or kidney stones.

Inosine is not a medical condition but a naturally occurring compound called a nucleoside, which is formed from the combination of hypoxanthine and ribose. It is an intermediate in the metabolic pathways of purine nucleotides, which are essential components of DNA and RNA. Inosine has been studied for its potential therapeutic benefits in various medical conditions, including neurodegenerative disorders, cardiovascular diseases, and cancer. However, more research is needed to fully understand its mechanisms and clinical applications.

Membrane transport proteins are specialized biological molecules, specifically integral membrane proteins, that facilitate the movement of various substances across the lipid bilayer of cell membranes. They are responsible for the selective and regulated transport of ions, sugars, amino acids, nucleotides, and other molecules into and out of cells, as well as within different cellular compartments. These proteins can be categorized into two main types: channels and carriers (or pumps). Channels provide a passive transport mechanism, allowing ions or small molecules to move down their electrochemical gradient, while carriers actively transport substances against their concentration gradient, requiring energy usually in the form of ATP. Membrane transport proteins play a crucial role in maintaining cell homeostasis, signaling processes, and many other physiological functions.

Nucleobase transport proteins are a type of membrane transport protein that facilitate the passive or active transport of nucleobases across biological membranes. Nucleobases, which include adenine, guanine, cytosine, thymine, and uracil, are fundamental components of nucleic acids (DNA and RNA) and are essential for genetic information storage, replication, and expression.

These transport proteins play a crucial role in maintaining the intracellular concentration of nucleobases by enabling their movement between intracellular and extracellular compartments or between cellular organelles. They can be specific to certain nucleobases or operate as broad-specificity transporters, depending on the protein's structure and function.

The transport process may involve uniport (transport of a single type of molecule), symport (coupled transport of multiple types of molecules in the same direction), or antiport (coupled transport of multiple types of molecules in opposite directions). The precise mechanisms governing nucleobase transport protein function are still under investigation, and further research is required to fully understand their regulation and significance in various physiological and pathophysiological contexts.

Biological transport refers to the movement of molecules, ions, or solutes across biological membranes or through cells in living organisms. This process is essential for maintaining homeostasis, regulating cellular functions, and enabling communication between cells. There are two main types of biological transport: passive transport and active transport.

Passive transport does not require the input of energy and includes:

1. Diffusion: The random movement of molecules from an area of high concentration to an area of low concentration until equilibrium is reached.
2. Osmosis: The diffusion of solvent molecules (usually water) across a semi-permeable membrane from an area of lower solute concentration to an area of higher solute concentration.
3. Facilitated diffusion: The assisted passage of polar or charged substances through protein channels or carriers in the cell membrane, which increases the rate of diffusion without consuming energy.

Active transport requires the input of energy (in the form of ATP) and includes:

1. Primary active transport: The direct use of ATP to move molecules against their concentration gradient, often driven by specific transport proteins called pumps.
2. Secondary active transport: The coupling of the movement of one substance down its electrochemical gradient with the uphill transport of another substance, mediated by a shared transport protein. This process is also known as co-transport or counter-transport.

Guanosine is a nucleoside that consists of a guanine base linked to a ribose sugar molecule through a beta-N9-glycosidic bond. It plays a crucial role in various biological processes, such as serving as a building block for DNA and RNA during replication and transcription. Guanosine triphosphate (GTP) and guanosine diphosphate (GDP) are important energy carriers and signaling molecules involved in intracellular regulation. Additionally, guanosine has been studied for its potential role as a neuroprotective agent and possible contribution to cell-to-cell communication.

Membrane transport modulators refer to a class of molecules that affect the movement of ions, nutrients, and other substances across cell membranes by interacting with membrane transport proteins. These proteins, also known as transporters or carriers, facilitate the passive or active transport of molecules in and out of cells.

Membrane transport modulators can either inhibit or enhance the activity of these transport proteins. They play a crucial role in pharmacology and therapeutics, as they can influence drug absorption, distribution, metabolism, and excretion (ADME). Examples of membrane transport modulators include ion channel blockers, inhibitors of efflux pumps like P-glycoprotein, and enhancers of nutrient uptake transporters.

It is important to note that the term "membrane transport modulator" can encompass a wide range of molecules with varying mechanisms and specificities, so further characterization is often necessary for a more precise understanding of their effects.

Hypoxanthine is a purine derivative and an intermediate in the metabolic pathways of nucleotide degradation, specifically adenosine to uric acid in humans. It is formed from the oxidation of xanthine by the enzyme xanthine oxidase. In the body, hypoxanthine is converted to xanthine and then to uric acid, which is excreted in the urine. Increased levels of hypoxanthine in the body can be indicative of various pathological conditions, including tissue hypoxia, ischemia, and necrosis.

Deoxycytidine kinase (dCK) is an enzyme that plays a crucial role in the phosphorylation of deoxycytidine and its analogs, which are important components in the intracellular metabolism of DNA precursors. The enzyme catalyzes the transfer of a phosphate group from adenosine triphosphate (ATP) to the hydroxyl group at the 5' carbon atom of deoxycytidine, forming deoxycytidine monophosphate (dCMP).

Deoxycytidine kinase is a key enzyme in the salvage pathway of pyrimidine nucleotide synthesis and is also involved in the activation of many antiviral and anticancer drugs that are analogs of deoxycytidine. The activity of dCK is tightly regulated, and its expression levels can vary depending on the cell type and physiological conditions.

In addition to its role in nucleotide metabolism, dCK has been implicated in various biological processes, including DNA damage response, cell cycle regulation, and apoptosis. Abnormalities in dCK activity or expression have been associated with several human diseases, including cancer and viral infections. Therefore, modulation of dCK activity has emerged as a potential therapeutic strategy for the treatment of these conditions.

Arabinofuranosyluracil (AraU) is a nucleoside analogue, which means it is a synthetic compound similar to the building blocks of DNA and RNA. AraU is formed by combining the sugar arabinose with the nucleobase uracil. Nucleoside analogues like AraU are often used in cancer chemotherapy and antiviral therapy because they can interfere with the replication of DNA and RNA, disrupting the growth or replication of cancer cells or viruses.

In the context of medical research and treatment, AraU has been studied for its potential use as an anticancer and antiviral agent. However, it is not currently approved for use as a medication in humans. Like many nucleoside analogues, AraU can have toxic effects on normal cells as well as cancerous or virus-infected cells, which limits its usefulness as a therapeutic agent.

Carrier proteins, also known as transport proteins, are a type of protein that facilitates the movement of molecules across cell membranes. They are responsible for the selective and active transport of ions, sugars, amino acids, and other molecules from one side of the membrane to the other, against their concentration gradient. This process requires energy, usually in the form of ATP (adenosine triphosphate).

Carrier proteins have a specific binding site for the molecule they transport, and undergo conformational changes upon binding, which allows them to move the molecule across the membrane. Once the molecule has been transported, the carrier protein returns to its original conformation, ready to bind and transport another molecule.

Carrier proteins play a crucial role in maintaining the balance of ions and other molecules inside and outside of cells, and are essential for many physiological processes, including nerve impulse transmission, muscle contraction, and nutrient uptake.

Deoxycytidine is a chemical compound that is a component of DNA, one of the nucleic acids in living organisms. It is a nucleoside, consisting of the sugar deoxyribose and the base cytosine. Deoxycytidine pairs with guanine via hydrogen bonds to form base pairs in the double helix structure of DNA.

In biochemistry, deoxycytidine can also exist as a free nucleoside, not bound to other molecules. It is involved in various cellular processes related to DNA metabolism and replication. Deoxycytidine can be phosphorylated to form deoxycytidine monophosphate (dCMP), which is an important intermediate in the synthesis of DNA.

It's worth noting that while deoxycytidine is a component of DNA, its counterpart in RNA is cytidine, which contains ribose instead of deoxyribose as the sugar component.

Affinity labels are chemical probes or reagents that can selectively and covalently bind to a specific protein or biomolecule based on its biological function or activity. These labels contain a functional group that interacts with the target molecule, often through non-covalent interactions such as hydrogen bonding, van der Waals forces, or ionic bonds. Once bound, the label then forms a covalent bond with the target molecule, allowing for its isolation and further study.

Affinity labels are commonly used in biochemistry and molecular biology research to identify and characterize specific proteins, enzymes, or receptors. They can be designed to bind to specific active sites, binding pockets, or other functional regions of a protein, allowing researchers to study the structure-function relationships of these molecules.

One example of an affinity label is a substrate analogue that contains a chemically reactive group. This type of affinity label can be used to identify and characterize enzymes by binding to their active sites and forming a covalent bond with the enzyme. The labeled enzyme can then be purified and analyzed to determine its structure, function, and mechanism of action.

Overall, affinity labels are valuable tools for studying the properties and functions of biological molecules in vitro and in vivo.

Purines are heterocyclic aromatic organic compounds that consist of a pyrimidine ring fused to an imidazole ring. They are fundamental components of nucleotides, which are the building blocks of DNA and RNA. In the body, purines can be synthesized endogenously or obtained through dietary sources such as meat, seafood, and certain vegetables.

Once purines are metabolized, they are broken down into uric acid, which is excreted by the kidneys. Elevated levels of uric acid in the body can lead to the formation of uric acid crystals, resulting in conditions such as gout or kidney stones. Therefore, maintaining a balanced intake of purine-rich foods and ensuring proper kidney function are essential for overall health.

Antimetabolites are a class of antineoplastic (chemotherapy) drugs that interfere with the metabolism of cancer cells and inhibit their growth and proliferation. These agents are structurally similar to naturally occurring metabolites, such as amino acids, nucleotides, and folic acid, which are essential for cellular replication and growth. Antimetabolites act as false analogs and get incorporated into the growing cells' DNA or RNA, causing disruption of the normal synthesis process, leading to cell cycle arrest and apoptosis (programmed cell death).

Examples of antimetabolite drugs include:

1. Folate antagonists: Methotrexate, Pemetrexed
2. Purine analogs: Mercaptopurine, Thioguanine, Fludarabine, Cladribine
3. Pyrimidine analogs: 5-Fluorouracil (5-FU), Capecitabine, Cytarabine, Gemcitabine

These drugs are used to treat various types of cancers, such as leukemias, lymphomas, breast, ovarian, and gastrointestinal cancers. Due to their mechanism of action, antimetabolites can also affect normal, rapidly dividing cells in the body, leading to side effects like myelosuppression (decreased production of blood cells), mucositis (inflammation and ulceration of the gastrointestinal tract), and alopecia (hair loss).

Purinergic P1 receptors are a type of G-protein coupled receptor that bind to nucleotides such as adenosine. These receptors are involved in a variety of physiological processes, including modulation of neurotransmitter release, cardiovascular function, and immune response. There are four subtypes of P1 receptors (A1, A2A, A2B, and A3) that have different signaling pathways and functions. Activation of these receptors can lead to a variety of cellular responses, including inhibition or stimulation of adenylyl cyclase activity, changes in intracellular calcium levels, and activation of various protein kinases. They play important roles in the central nervous system, cardiovascular system, respiratory system, gastrointestinal system, and immune system.

In the context of medicine and pharmacology, "kinetics" refers to the study of how a drug moves throughout the body, including its absorption, distribution, metabolism, and excretion (often abbreviated as ADME). This field is called "pharmacokinetics."

1. Absorption: This is the process of a drug moving from its site of administration into the bloodstream. Factors such as the route of administration (e.g., oral, intravenous, etc.), formulation, and individual physiological differences can affect absorption.

2. Distribution: Once a drug is in the bloodstream, it gets distributed throughout the body to various tissues and organs. This process is influenced by factors like blood flow, protein binding, and lipid solubility of the drug.

3. Metabolism: Drugs are often chemically modified in the body, typically in the liver, through processes known as metabolism. These changes can lead to the formation of active or inactive metabolites, which may then be further distributed, excreted, or undergo additional metabolic transformations.

4. Excretion: This is the process by which drugs and their metabolites are eliminated from the body, primarily through the kidneys (urine) and the liver (bile).

Understanding the kinetics of a drug is crucial for determining its optimal dosing regimen, potential interactions with other medications or foods, and any necessary adjustments for special populations like pediatric or geriatric patients, or those with impaired renal or hepatic function.

Pyrimidine nucleosides are organic compounds that consist of a pyrimidine base (a heterocyclic aromatic ring containing two nitrogen atoms and four carbon atoms) linked to a sugar molecule, specifically ribose or deoxyribose, via a β-glycosidic bond. The pyrimidine bases found in nucleosides can be cytosine (C), thymine (T), or uracil (U). When the sugar component is ribose, it is called a pyrimidine nucleoside, and when it is linked to deoxyribose, it is referred to as a deoxy-pyrimidine nucleoside. These molecules play crucial roles in various biological processes, particularly in the structure and function of nucleic acids such as DNA and RNA.

An oocyte, also known as an egg cell or female gamete, is a large specialized cell found in the ovary of female organisms. It contains half the number of chromosomes as a normal diploid cell, as it is the product of meiotic division. Oocytes are surrounded by follicle cells and are responsible for the production of female offspring upon fertilization with sperm. The term "oocyte" specifically refers to the immature egg cell before it reaches full maturity and is ready for fertilization, at which point it is referred to as an ovum or egg.

Molecular sequence data refers to the specific arrangement of molecules, most commonly nucleotides in DNA or RNA, or amino acids in proteins, that make up a biological macromolecule. This data is generated through laboratory techniques such as sequencing, and provides information about the exact order of the constituent molecules. This data is crucial in various fields of biology, including genetics, evolution, and molecular biology, allowing for comparisons between different organisms, identification of genetic variations, and studies of gene function and regulation.

"Xenopus laevis" is not a medical term itself, but it refers to a specific species of African clawed frog that is often used in scientific research, including biomedical and developmental studies. Therefore, its relevance to medicine comes from its role as a model organism in laboratories.

In a broader sense, Xenopus laevis has contributed significantly to various medical discoveries, such as the understanding of embryonic development, cell cycle regulation, and genetic research. For instance, the Nobel Prize in Physiology or Medicine was awarded in 1963 to John R. B. Gurdon and Sir Michael J. Bishop for their discoveries concerning the genetic mechanisms of organism development using Xenopus laevis as a model system.

Benzothiepins are a class of heterocyclic compounds that contain a benzene fused to a thiepin ring. They do not have a specific medical definition, as they are not a type of drug or medication. However, some benzothiepin derivatives have been synthesized and studied for their potential pharmacological activity, particularly as anti-inflammatory and analgesic agents.

One example of a benzothiepin derivative is benzothiophene, which has been investigated for its anti-inflammatory properties. However, it is not widely used in clinical practice due to its potential toxicity. Therefore, the term 'benzothiepins' does not have a well-established medical meaning and is primarily used in the context of chemistry and pharmacology research.

An amino acid sequence is the specific order of amino acids in a protein or peptide molecule, formed by the linking of the amino group (-NH2) of one amino acid to the carboxyl group (-COOH) of another amino acid through a peptide bond. The sequence is determined by the genetic code and is unique to each type of protein or peptide. It plays a crucial role in determining the three-dimensional structure and function of proteins.

2-Chloroadenosine is a synthetic, chlorinated analog of adenosine, which is a naturally occurring purine nucleoside. It acts as an antagonist at adenosine receptors and has been studied for its potential effects on the cardiovascular system, including its ability to reduce heart rate and blood pressure. It may also have anti-cancer properties and has been investigated as a potential therapeutic agent in cancer treatment. However, further research is needed to establish its safety and efficacy in clinical settings.

Ribonucleoside Diphosphate Reductase (RNR) is an enzyme that plays a crucial role in the regulation of DNA synthesis and repair. It catalyzes the conversion of ribonucleoside diphosphates (NDPs) to deoxyribonucleoside diphosphates (dNDPs), which are the building blocks of DNA. This reaction is essential for the synthesis of new DNA strands during replication and repair processes. The enzyme's activity is tightly regulated, as it must be carefully controlled to prevent errors in DNA synthesis that could lead to mutations and genomic instability. RNR is a target for chemotherapeutic agents due to its essential role in DNA synthesis.

Membrane proteins are a type of protein that are embedded in the lipid bilayer of biological membranes, such as the plasma membrane of cells or the inner membrane of mitochondria. These proteins play crucial roles in various cellular processes, including:

1. Cell-cell recognition and signaling
2. Transport of molecules across the membrane (selective permeability)
3. Enzymatic reactions at the membrane surface
4. Energy transduction and conversion
5. Mechanosensation and signal transduction

Membrane proteins can be classified into two main categories: integral membrane proteins, which are permanently associated with the lipid bilayer, and peripheral membrane proteins, which are temporarily or loosely attached to the membrane surface. Integral membrane proteins can further be divided into three subcategories based on their topology:

1. Transmembrane proteins, which span the entire width of the lipid bilayer with one or more alpha-helices or beta-barrels.
2. Lipid-anchored proteins, which are covalently attached to lipids in the membrane via a glycosylphosphatidylinositol (GPI) anchor or other lipid modifications.
3. Monotopic proteins, which are partially embedded in the membrane and have one or more domains exposed to either side of the bilayer.

Membrane proteins are essential for maintaining cellular homeostasis and are targets for various therapeutic interventions, including drug development and gene therapy. However, their structural complexity and hydrophobicity make them challenging to study using traditional biochemical methods, requiring specialized techniques such as X-ray crystallography, nuclear magnetic resonance (NMR) spectroscopy, and single-particle cryo-electron microscopy (cryo-EM).

Histiocytosis is a term used to describe a group of rare disorders characterized by an abnormal increase in the number of histiocytes, which are a type of white blood cell that helps fight infection and helps in healing processes. These disorders can affect various organs and tissues in the body, leading to different symptoms and severity.

There are several types of histiocytosis, including Langerhans cell histiocytosis (LCH), Erdheim-Chester disease (ECD), and hemophagocytic lymphohistiocytosis (HLH). Each type has its own specific features and diagnostic criteria.

For example, LCH is characterized by the abnormal accumulation of Langerhans cells, a type of histiocyte found in the skin and mucous membranes. These cells can form tumors or lesions in various organs, such as the bones, lungs, liver, and skin.

HLH, on the other hand, is a life-threatening condition that occurs when there is an overactive immune response leading to excessive activation of histiocytes and other immune cells. This can result in fever, enlargement of the liver and spleen, and decreased blood cell counts.

The exact cause of histiocytosis is not fully understood, but it is believed to involve genetic mutations that lead to uncontrolled proliferation and accumulation of histiocytes. Treatment for histiocytosis depends on the type and severity of the disorder and may include chemotherapy, radiation therapy, immunosuppressive drugs, or stem cell transplantation.

"Xenopus" is not a medical term, but it is a genus of highly invasive aquatic frogs native to sub-Saharan Africa. They are often used in scientific research, particularly in developmental biology and genetics. The most commonly studied species is Xenopus laevis, also known as the African clawed frog.

In a medical context, Xenopus might be mentioned when discussing their use in research or as a model organism to study various biological processes or diseases.

A cell line is a culture of cells that are grown in a laboratory for use in research. These cells are usually taken from a single cell or group of cells, and they are able to divide and grow continuously in the lab. Cell lines can come from many different sources, including animals, plants, and humans. They are often used in scientific research to study cellular processes, disease mechanisms, and to test new drugs or treatments. Some common types of human cell lines include HeLa cells (which come from a cancer patient named Henrietta Lacks), HEK293 cells (which come from embryonic kidney cells), and HUVEC cells (which come from umbilical vein endothelial cells). It is important to note that cell lines are not the same as primary cells, which are cells that are taken directly from a living organism and have not been grown in the lab.

I'm sorry for any confusion, but "Protozoan Proteins" is not a specific medical or scientific term. Protozoa are single-celled eukaryotic organisms, and proteins are large biological molecules consisting of one or more chains of amino acid residues. Therefore, "Protozoan Proteins" generally refers to the various types of proteins found in protozoa.

However, if you're looking for information about proteins specific to certain protozoan parasites with medical relevance (such as Plasmodium falciparum, which causes malaria), I would be happy to help! Please provide more context or specify the particular protozoan of interest.

Sequence homology, amino acid, refers to the similarity in the order of amino acids in a protein or a portion of a protein between two or more species. This similarity can be used to infer evolutionary relationships and functional similarities between proteins. The higher the degree of sequence homology, the more likely it is that the proteins are related and have similar functions. Sequence homology can be determined through various methods such as pairwise alignment or multiple sequence alignment, which compare the sequences and calculate a score based on the number and type of matching amino acids.

Messenger RNA (mRNA) is a type of RNA (ribonucleic acid) that carries genetic information copied from DNA in the form of a series of three-base code "words," each of which specifies a particular amino acid. This information is used by the cell's machinery to construct proteins, a process known as translation. After being transcribed from DNA, mRNA travels out of the nucleus to the ribosomes in the cytoplasm where protein synthesis occurs. Once the protein has been synthesized, the mRNA may be degraded and recycled. Post-transcriptional modifications can also occur to mRNA, such as alternative splicing and addition of a 5' cap and a poly(A) tail, which can affect its stability, localization, and translation efficiency.

A cell membrane, also known as the plasma membrane, is a thin semi-permeable phospholipid bilayer that surrounds all cells in animals, plants, and microorganisms. It functions as a barrier to control the movement of substances in and out of the cell, allowing necessary molecules such as nutrients, oxygen, and signaling molecules to enter while keeping out harmful substances and waste products. The cell membrane is composed mainly of phospholipids, which have hydrophilic (water-loving) heads and hydrophobic (water-fearing) tails. This unique structure allows the membrane to be flexible and fluid, yet selectively permeable. Additionally, various proteins are embedded in the membrane that serve as channels, pumps, receptors, and enzymes, contributing to the cell's overall functionality and communication with its environment.

Solute carrier family Equilibrative nucleoside transporters Nucleoside transporters GRCh38: Ensembl release 89: ENSG00000174669 ... Equilibrative nucleoside transporter 2 (ENT2) is a protein that in humans is encoded by the SLC29A2 gene. ... 2004). "The equilibrative nucleoside transporter family, SLC29". Pflügers Arch. 447 (5): 735-43. doi:10.1007/s00424-003-1103-2 ... Mangravite LM, Xiao G, Giacomini KM (2003). "Localization of human equilibrative nucleoside transporters, hENT1 and hENT2, in ...
Solute carrier family Equilibrative nucleoside transporters Nucleoside transporters Augustine blood group system GRCh38: ... "A single glycine mutation in the equilibrative nucleoside transporter gene, hENT1, alters nucleoside transport activity and ... Equilibrative nucleoside transporter 1 (ENT1) is a protein that in humans is encoded by the SLC29A1 gene. Multiple ... This gene is a member of the equilibrative nucleoside transporter family. The gene encodes a transmembrane glycoprotein that ...
There are two known types of nucleoside transporters, concentrative nucleoside transporters (CNTs; SLC28) and equilibrative ... Baldwin SA, Beal PR, Yao SY, King AE, Cass CE, Young JD (February 2004). "The equilibrative nucleoside transporter family, ... Nucleoside transporters (NTs) are a group of membrane transport proteins which transport nucleoside substrates like adenosine ... "Physiological and pharmacological roles of nucleoside transporter proteins". Nucleosides, Nucleotides & Nucleic Acids. 27 (6): ...
It is known alternatively as the human equilibrative nucleoside transporter-4 (hENT4). Unlike other members of the ENT family, ... Baldwin SA, Beal PR, Yao SY, King AE, Cass CE, Young JD (February 2004). "The equilibrative nucleoside transporter family, ... equilibrative nucleoside transporters). No highly selective PMAT inhibitors are yet available, but a number of existing ... The plasma membrane monoamine transporter (PMAT) is a low-affinity monoamine transporter protein which in humans is encoded by ...
"Human equilibrative nucleoside transporter (ENT) family of nucleoside and nucleobase transporter proteins". Xenobiotica. 38 (7- ... Nucleoside (in) Concentrative nucleoside transporter Nucleoside transporter Molina-Arcas M, Trigueros-Motos L, Casado FJ, ... Members of the Equilibrative Nucleoside Transporter (ENT) Family (TC# 2.A.57) are transport proteins that are specific to ... Baldwin SA, Beal PR, Yao SY, King AE, Cass CE, Young JD (Feb 2004). "The equilibrative nucleoside transporter family, SLC29". ...
In these, trifluridine used the concentrative nucleoside transporter 1 (CNT1) and equilibrative nucleoside transporters 1 (ENT1 ... It is a nucleoside analogue, a modified form of deoxyuridine, similar enough to be incorporated into viral DNA replication, but ... Drugs that interact with these transporters could influence blood plasma concentrations of trifluridine. Being a thymidine ... 24 (2): 122-124. PMID 9571274. O'Brien WJ, Taylor JL (August 1991). "Therapeutic response of herpes simplex virus-induced ...
Adenosine transporters, including: Equilibrative nucleoside transporter 1 (ENT1) Equilibrative nucleoside transporter 2 (ENT2) ... Equilibrative nucleoside transporter 3 (ENT3) Equilibrative nucleoside transporter 4 (ENT4) Vesicular acetylcholine transporter ... Vesicular glutamate transporter 3 (VGLUT3) GABA transporters, including: GABA transporter type 1 (GAT1) GABA transporter type 2 ... GAT2) GABA transporter type 3 (GAT3) Betaine transporter (BGT1) Vesicular GABA transporter (VGAT) Glycine transporters, ...
... equilibrative nucleoside transporter 1 MeSH D12.776.157.530.625.750.500.750 - equilibrative-nucleoside transporter 2 MeSH ... nucleoside transport proteins MeSH D12.776.157.530.625.750.500 - equilibrative nucleoside transport proteins MeSH D12.776. ... cationic amino acid transporter 1 MeSH D12.776.157.530.200.374.600.300 - cationic amino acid transporter 2 MeSH D12.776.157.530 ... glucose transporter type 4 MeSH D12.776.157.530.500.500.968 - glucose transporter type 5 MeSH D12.776.157.530.500.750 - sodium- ...
... equilibrative nucleoside transporter 1 MeSH D12.776.543.585.625.750.500.750 - equilibrative-nucleoside transporter 2 MeSH ... nucleoside transport proteins MeSH D12.776.543.585.625.750.500 - equilibrative nucleoside transport proteins MeSH D12.776. ... cationic amino acid transporter 1 MeSH D12.776.543.585.200.374.600.300 - cationic amino acid transporter 2 MeSH D12.776.543.585 ... glucose transporter type 4 MeSH D12.776.543.585.500.500.968 - glucose transporter type 5 MeSH D12.776.543.585.500.750 - sodium- ...
Baldwin SA, Beal PR, Yao SY, King AE, Cass CE, Young JD (February 2004). "The equilibrative nucleoside transporter family, ... Na+-coupled nucleoside transport (SLC28A1, SLC28A2, SLC28A3) facilitative nucleoside transporter (SLC29A1, SLC29A2, SLC29A3, ... copper transporter (SLC31A1, SLC31A2) vesicular inhibitory amino acid transporter (SLC32A1) Acetyl-CoA transporter (SLC33A1) ... basolateral iron transporter (SLC40A1) MgtE-like magnesium transporter (SLC41A1, SLC41A2, SLC41A3) Ammonia transporter (RHAG( ...
The protein which acts as the Augustine antigens is equilibrative nucleoside transporter 1, a transmembrane glycoprotein that ... Individuals with the null phenotype, lacking any form of the transporter protein, have mineralization around the joints, ... 35 (1): 1-2. doi:10.21307/immunohematology-2020-001. ISSN 0894-203X. PMID 30908068. S2CID 85514375. Archived (PDF) from the ... mediates cellular uptake of nucleosides. This protein is abundant in erythroid progenitor cells and in mature red blood cells. ...
... family 1.B.10 Nucleoside-specific channel-forming outer membrane porin (Tsx) family 1.B.11 Outer membrane fimbrial usher porin ... Transporter Classification Database List at qmul.ac.uk Saier MH, Tran CV, Barabote RD (January 2006). "TCDB: the Transporter ... mediated Active Transport 3.A.1 ABC transporters including BtuCD, molybdate uptake transporter, Cystic fibrosis transmembrane ... The Transporter Classification Database (or TCDB) is an International Union of Biochemistry and Molecular Biology (IUBMB)- ...
... which encodes for the equilibrative nucleoside transporter 3 (ENT3), a nucleoside transporter that is present in membranes of ... November 2012). "Whole-exome sequencing identifies mutations in the nucleoside transporter gene SLC29A3 in dysosteosclerosis, a ... ENT3 is responsible for the trafficking of nucleoside, free purines and pyrimidines into the mitochondria and out of lysosomes ... Mutation leads to impaired ENT3 transportation activity, accumulation of nucleotides and nucleoside in lysosomes. As ...
"Glycine 154 of the equilibrative nucleoside transporter, hENT1, is important for nucleoside transport and for conferring ... nucleoside and neurotransmitter adenosine by blocking the action of one or more of the equilibrative nucleoside transporters ( ... and dilazep for the human equilibrative nucleoside transporter, hENT1". Biochem J. 380 (1): 131-137. doi:10.1042/BJ20031880. ... Chaudary N, Naydenova Z, Shuralyova I, Coe IR (2004). "The adenosine transporter, mENT1, is a target for adenosine receptor ...
Current research interests include understanding the underlying structure of Equilibrative nucleoside transporters (ENTs) and ... function and regulation of nucleoside transporters. In 2005 she was the first woman to chair the Department of Biology, and ... working as a postdoctoral fellow working on the role of adenosine transporter (membrane transport proteins) with Adrienne Grant ... Archived from the original on 2 June 2018. Retrieved 19 February 2018. "381: Dr. Imogen Coe: Studying Drug Transport Proteins ...
Concentrative nucleoside transporters (CNTs): Na+-dependent symporters Equilibrative nucleoside transporters (ENTs): Na+- ... Nucleoside transporters (NTs) are a group of membrane transport proteins which transport nucleoside substrates including ... Dos Santos-Rodrigues A, Grañé-Boladeras N, Bicket A, Coe IR (July 2014). "Nucleoside transporters in the purinome". ... In any case, the final product of the hydrolysis cascade is the nucleoside. The Pannexin-1 channel (PANX1) is an integral ...
Solute carrier family Equilibrative nucleoside transporters Nucleoside transporters GRCh38: Ensembl release 89: ENSG00000174669 ... Equilibrative nucleoside transporter 2 (ENT2) is a protein that in humans is encoded by the SLC29A2 gene. ... 2004). "The equilibrative nucleoside transporter family, SLC29". Pflügers Arch. 447 (5): 735-43. doi:10.1007/s00424-003-1103-2 ... Mangravite LM, Xiao G, Giacomini KM (2003). "Localization of human equilibrative nucleoside transporters, hENT1 and hENT2, in ...
Since the equilibrative nucleoside transporter-2 (Ent2) is important in regulating brain adenosine homeostasis, the present ... The Critical Role of Equilibrative Nucleoside Transporter-2 in Modulating Cerebral Damage and Vascular Dysfunction in Mice with ...
Deletion of equilibrative nucleoside transporter-2 protects against lipopolysaccharide-induced neuroinflammation and blood- ... https://www.scopus.com/inward/record.uri?eid=2-s2.0-85076202140&doi=10.1016%2fj.bbi.2019.11.008&partnerID=40&md5= ...
Residue 33 of Human Equilibrative Nucleoside Transporter 2 Is a Functionally Important Component of Both the Dipyridamole and ... Molecular Determinants of Substrate/Inhibitor Binding to the Human and Rabbit Renal Organic Cation Transporters hOCT2 and ... Nucleoside Binding Sites Frank Visser, Jing Zhang, R. Taylor Raborn, Stephen A. Baldwin, James D. Young and Carol E. Cass ... β-Arrestin 2-Dependent Angiotensin II Type 1A Receptor-Mediated Pathway of Chemotaxis Dacia L. Hunton, William G. Barnes, Jihee ...
Human equilibrative nucleoside transporter-3 (hENT3) spectrum disorder mutations impair nucleoside transport, protein ... Mutations in SLC29A3, encoding an equilibrative nucleoside transporter ENT3, cause a familial histiocytosis syndrome ( ... which provides instructions for making a protein called equilibrative nucleoside transporter 3 (ENT3). ENT3 belongs to a family ... A lack of ENT3 activity may also lead to a reduction in the amount of nucleosides in mitochondria. This nucleoside shortage ...
Predicting drug interactions with human equilibrative nucleoside transporters 1 and 2 using functional knockout cell lines and ... Purine Nucleoside-dependent inhibition of cellular proliferation in 1321N1 human astrocytoma cells. Islinger, F., Gekle, M. & ... Physiological Characterization of the Transporter-Mediated Uptake of the Reversible Male Contraceptive H2-Gamendazole across ... Weyand, N. J., Calton, C. M., Higashi, D. L., Kanack, K. J. & So, M., Jan 15 2010, In: Journal of Immunology. 184, 2, p. 694- ...
3E10 gains entry to the cells via the equilibrative nucleoside transporter 2 (ENT2; SLC29A2), a receptor found in many cell ... Aim 2) in vivo characterization of VAL-0914 effects on heart function and misfolded protein clearance in a mouse model of ...
Equilibrative nucleoside transporter 1. ... mercaptopurine riboside] and dilazep for the human equilibrative nucleoside ... Anticancer nucleobase analogues 6-mercaptopurine and 6-thioguanine are novel substrates for equilibrative nucleoside.... ... nucleobase analogues 6-mercaptopurine and 6-thioguanine are novel substrates for equilibrative nucleoside transporter 2. ( ... 6-thioguanine nucleosides (6-TGNs), 6-methylmercaptopurine, and 6-methylmercaptopurine nucleosides (6-MMPNs). (nih.gov) ...
Deletion of equilibrative nucleoside transporter-2 protects against lipopolysaccharide-induced neuroinflammation and blood- ... Amelioration of lipopolysaccharide-induced memory impairment in equilibrative nucleoside transporter-2 knockout mice is ...
Deletion of equilibrative nucleoside transporter-2 protects against lipopolysaccharide-induced neuroinflammation and blood- ...
Type 1 equilibrative nucleoside transporter (ENT1) is responsible for the majority of adenosine transport across the plasma ... Type 1 equilibrative nucleoside transporter (ENT1) is responsible for the majority of adenosine transport across the plasma ... Type 1 equilibrative nucleoside transporter (ENT1) is responsible for the majority of adenosine transport across the plasma ... Type 1 equilibrative nucleoside transporter (ENT1) is responsible for the majority of adenosine transport across the plasma ...
The Trypanosoma brucei genome project has identified 12 members of the equilibrative nucleoside transporter family, most of ... The Trypanosoma brucei genome project has identified 12 members of the equilibrative nucleoside transporter family, most of ... The Trypanosoma brucei genome project has identified 12 members of the equilibrative nucleoside transporter family, most of ... The Trypanosoma brucei genome project has identified 12 members of the equilibrative nucleoside transporter family, most of ...
Equilibrative nucleoside transporter 1 (ENT1) and excitatory amino acid transporter 2 (EAAT2) are predominantly expressed in ... Studies performed in cell cultures suggest that ethanol inhibits equilibrative nucleoside transporter 1 to block the reuptake ... The purine nucleoside, adenosine, is responsible for mediating many neuronal and behavioral responses to ethanol. ... Experiments 1 and 2 demonstrated a direct relationship between β-E levels and immobility. There were also sex differences in ...
Carrier, E.J.; Auchampach, J.A.; Hillard, C.J. Inhibition of an equilibrative nucleoside transporter by cannabidiol: A ... by binding to equilibrative nucleoside transporter-1); inhibition ofG-protein coupled receptor 55 (GPR55); and the stimulation ... showed that CBD acts as a inhibitor of adenosine and thiamine uptake by inhibiting the equilibrative nucleoside transporter-1 ( ... the purine nucleoside, adenosine, is secreted by cancer and immune cells under metabolic stress and hypoxia [130]. Adenosine ...
An analysis of human equilibrative nucleoside transporter-1, ribonucleoside reductase subunit m1, ribonucleoside reductase ... Capecitabine was dosed at 1,600 mg/m2/day in two divided doses per day (median dose=1,600 mg/m2/day) based on our phase I study ... 2Hofstra North Shore LIJ School of Medicine, North Shore LIJ Health System, New Hyde Park, New York, NY, U.S.A. ... This was combined with either 4 months of gemcitabine at 1,000 mg/m2 weekly for 3 out of 4 weeks or capecitabine at 2,000 mg/m2 ...
3the human being equilibrative nucleoside transporter 1 (hENT1), and it is eventually phosphorylated to cytarabine-triphosphate ... The cytotoxicity of Ara-C in the Mnk1&2 KD cells was improved by 10-fold in comparison to WT cells (Desk ?(Desk2).2). Also, the ... Alternatively, Ara-C activates the MAPK-Mnk-eIF4E pathway by causing the phosphorylation of Erk1/2, p38 and eIF4E, leading to a ... MNKI-8e is normally a powerful and selective Mnk inhibitor in comparison to known Mnk inhibitors, phosphorylation of Erk1/2, ...
Equilibrative NBMPR-insensitive nucleoside transporter,Hydrophobic nucleolar protein, 36 kDa,Nucleoside transporter, ei-type, ... Alias: Equilibrative nucleoside transporter 2,36 kDa nucleolar protein HNP36,Delayed-early response protein 12,Equilibrative ... Background: Mediates equilibrative transport of purine, pyrimidine nucleosides and the purine base hypoxanthine. Very less ...
Inhibition of an equilibrative nucleoside transporter by cannabidiol: a mechanism of cannabinoid immunosuppression. Proc Natl ... 1998;280(2):147-151.. *Smith BH, Elliott AM, Chambers WA, et al. The impact of chronic pain in the community. Fam Pract. 2001; ... 2009;30(2):79-84.. *Klein TW, Newton C, Larsen K, et al. The cannabinoid system and immune modulation. J Leukoc Biol. 2003;74(4 ... 2002;241(2):329-339.. *Lodzki M, Godin B, Rakou L, et al. Cannabidiol-transdermal delivery and anti-inflammatory effect in a ...
Equilibrative nucleoside transporter 1. MTTSHQPQDRYKAVWLIFFMLGLGTLLPWNFFMTATQYFTNRLDMSQNVS.... unknown. inhibitor. P- ... InChI=1S/C21H30O2/c1-5-6-7-8-16-12-19(22)21(20(23)13-16)18-11-15(4)9-10-17(18)14(2)3/h11-13,17-18,22-23H,2,5-10H2,1,3-4H3/t17-, ... 2-[(1~{R},6~{R})-3-methyl-6-prop-1-en-2-yl-cyclohex-2-en-1-yl]-5-pentyl-benzene-1,3-diol. ... Indoleamine 2,3-dioxygenase 1. MAHAMENSWTISKEYHIDEEVGFALPNPQENLPDFYNDWMFIAKHLPDLI.... unknown. inhibitor. Cytochrome P450 1B1. ...
Equilibrative Nucleoside Transporters *ER *ErbB *ERK *ERR *Esterases *Estrogen (GPR30) Receptors *Estrogen Receptors ... Dipeptidyl peptidase-4 inhibitors (DPP-4I) and sodium-glucose co-transporter-2 inhibitors (SGLT-2I) are various other exciting ... The gradual drop in -cell function is inevitable in type 2. * Post author By exposed ... The gradual drop in -cell function is inevitable in type 2 diabetes mellitus and for that reason, substantial proportions of ...
Human Equilibrative nucleoside transporter 1 ELISA Kit Biotechnolabs Elisa Kit, Molecular Biology, Plant and Animal Antibodies ... equilibrative nucleoside transporter 1; Equilibrative nucleoside transporter 1; equilibrative nucleoside transporter 1; solute ... equilibrative nucleoside transporter), member 1; Equilibrative nitrobenzylmercaptopurine riboside-sensitive Gene Name. [SLC29A1 ... Human Equilibrative nucleoside transporter 1 ELISA Kit. Synonym. [Equilibrative nucleoside transporter 1]. ...
Equilibrative Nucleoside Transporter 1 D12.776.157.530.937.532.500 D12.776.543.585.937.563.500 Equilibrative-Nucleoside ... Equilibrative Nucleoside Transport Proteins D12.776.157.530.937.532 D12.776.543.585.937.563 ... Cationic Amino Acid Transporter 1 D12.776.157.530.937.375.200 D12.776.543.585.937.375.200 Cationic Amino Acid Transporter 2 ... Glucose Transporter Type 1 D12.776.157.530.937.563.500 D12.776.543.585.937.625.500 Glucose Transporter Type 2 D12.776.157.530. ...
Equilibrative Nucleoside Transporter 1 D12.776.157.530.937.532.500 D12.776.543.585.937.563.500 Equilibrative-Nucleoside ... Equilibrative Nucleoside Transport Proteins D12.776.157.530.937.532 D12.776.543.585.937.563 ... Cationic Amino Acid Transporter 1 D12.776.157.530.937.375.200 D12.776.543.585.937.375.200 Cationic Amino Acid Transporter 2 ... Glucose Transporter Type 1 D12.776.157.530.937.563.500 D12.776.543.585.937.625.500 Glucose Transporter Type 2 D12.776.157.530. ...
Equilibrative Nucleoside Transporter 1 D12.776.157.530.937.532.500 D12.776.543.585.937.563.500 Equilibrative-Nucleoside ... Equilibrative Nucleoside Transport Proteins D12.776.157.530.937.532 D12.776.543.585.937.563 ... Cationic Amino Acid Transporter 1 D12.776.157.530.937.375.200 D12.776.543.585.937.375.200 Cationic Amino Acid Transporter 2 ... Glucose Transporter Type 1 D12.776.157.530.937.563.500 D12.776.543.585.937.625.500 Glucose Transporter Type 2 D12.776.157.530. ...
Equilibrative Nucleoside Transporter 1 D12.776.157.530.937.532.500 D12.776.543.585.937.563.500 Equilibrative-Nucleoside ... Equilibrative Nucleoside Transport Proteins D12.776.157.530.937.532 D12.776.543.585.937.563 ... Cationic Amino Acid Transporter 1 D12.776.157.530.937.375.200 D12.776.543.585.937.375.200 Cationic Amino Acid Transporter 2 ... Glucose Transporter Type 1 D12.776.157.530.937.563.500 D12.776.543.585.937.625.500 Glucose Transporter Type 2 D12.776.157.530. ...
Equilibrative Nucleoside Transporter 1 D12.776.157.530.937.532.500 D12.776.543.585.937.563.500 Equilibrative-Nucleoside ... Equilibrative Nucleoside Transport Proteins D12.776.157.530.937.532 D12.776.543.585.937.563 ... Cationic Amino Acid Transporter 1 D12.776.157.530.937.375.200 D12.776.543.585.937.375.200 Cationic Amino Acid Transporter 2 ... Glucose Transporter Type 1 D12.776.157.530.937.563.500 D12.776.543.585.937.625.500 Glucose Transporter Type 2 D12.776.157.530. ...
Equilibrative nucleoside transporter 1 (ENT1) regulates postischemic blood flow during acute kidney injury in mice. Grenz1, ... Consistent with the notion that equilibrative nucleoside transporters (ENTs) terminate adenosine signaling, we observed that ... 2) a design exercise with VR professionals to explore possible notification methods; and 3) an empirical study on the ... 2, 3). Particularly for surgical patients, AKI represents a significant threat. For example, surgical procedures requiring ...
"Equilibrative nucleoside transporter 3","protein_coding" "Sro1204_g252200.1","Contig1757.g15595","Seminavis robusta","PI-PLC X ... "Equilibrative nucleoside transporter [Interproscan].","protein_coding" "SymbC1.scaffold3742.4","3742.4","Cladocopium sp. clade ... ","ABC transporter-like; ABC-transporter extension domain [Interproscan].","protein_coding" "SymbC1.scaffold8376.4","8376.4"," ... ","ABC transporter-like; ABC-transporter extension domain [Interproscan].","protein_coding" "TP13G01420.1","No alias"," ...
Equilibrative nucleoside transporter 1; Equilibrative nucleoside transporter 2; Equilibrative nucleoside transporter 3; Sodium/ ... Equilibrative nucleoside transporter 1; Equilibrative nucleoside transporter 2; Equilibrative nucleoside transporter 3 ... Equilibrative nucleoside transporter 1; Equilibrative nucleoside transporter 2; Sodium/nucleoside cotransporter 2 ... Equilibrative nucleoside transporter 1; Equilibrative nucleoside transporter 2; Equilibrative nucleoside transporter 3; Plasma ...
Carrier, E. J., Auchampach, J. A., & Hillard, C. J. (2006). Inhibition of an equilibrative nucleoside transporter by ... 2. Inhibits Brain Inflammation. One of the ways marijuana was used in the past to treat headaches, was by wrapping its wet ... Phase 2: Aura Phase. During the aura phase, people experience strange changes in their vision and/or perception. It can change ... 2. Inflammation (Sensitization). We need inflammation to stay healthy.. Its our bodies way to trap and destroy invading ...
  • The study used three-dimensional pharmacophores for ENT1 and ENT2 substrates and inhibitors and Bayesian machine learning models to identify potential interactions with these transporters. (nih.gov)
  • We tested this possibility employing dilazep, a potent inhibitor of each equilibrative nucleoside transporter 1 (ENT1) and ENT2, and NBTI, a distinct inhibitor of ENT1 (33, 42, 43). (idhinhibitor.com)
  • RO7117997, is an IND-ready Equilibrative Nucleoside Transporter 1 (ENT1) inhibitor discovered in partnership with Roche using the PsychoGenics' AI-enabled phenotypic screening platforms. (butwhatdoweknow.com)
  • This is known as the equilibrative nucleoside transporter 1 (ENT1) and meant that sleep disturbances could occur a result. (belgraviacentre.com)
  • As its pharmacokinetics depend on facilitated transmembrane transport, we assessed whether variants in genes that code for concentrative (concentrative nucleoside transporters 2 and 3 coded by SLC28A2 and SLC28A3, respectively) and equilibrative nucleoside transporters (equilibrative nucleoside transporters 1 and 2 coded by SLC29A1 and SLC29A2, respectively) are associated with the therapy response and side effects. (nih.gov)
  • To date, no practical assay exists to identify patients likely to derive benefit from F-ara-A. We previously reported that high mRNA levels encoding human concentrative nucleoside transporter 3 (hCNT3) protein in CLL correlated with clinical resistance to F-ara-A. This study explores the value of immunohistochemistry (IHC) for hCNT3 as a marker of F-ara-A resistance in CLL. (medscape.com)
  • In humans, these transporters include two members of the equilibrative nucleoside transporter (ENT) family (hENT1/2), and three members of the concentrative nucleoside transporter (CNT) family (hCNT1/2/3). (medscape.com)
  • Human concentrative nucleoside transporter-3 (hCNT3) is a sodium-coupled nucleoside transporter that exhibits high affinity and broad substrate selectivity, making it the most suitable candidate for mediating the uptake and cytotoxic action of most nucleoside-derived drugs. (aianmodena.org)
  • The uptake of nucleosides by transporters, such as SLC29A2, is essential for nucleotide synthesis by salvage pathways in cells that lack de novo biosynthetic pathways. (nih.gov)
  • CBD inhibited adenosine uptake via equilibrative nucleoside transporter 1 and synergistically enhanced adenosine's TNF-α suppression upon LPS treatment. (thecannabisadvisory.com)
  • A good correlation was found for the inhibitory effects of nucleoside analogs to adenosine uptake between in situ and in vitro studies. (elsevierpure.com)
  • In addition to very simple passive diffusion, bendamustine uptake may be facilitated by means of nucleoside transportersFigure 6. (idhinhibitor.com)
  • Bendamustine enhances the uptake of Ara-C and subsequent increase in Ara-CTP in HBL-2 cells. (idhinhibitor.com)
  • ENT3 belongs to a family of proteins that transport molecules called nucleosides in cells. (medlineplus.gov)
  • A subtype of equilibrative nucleoside transporter proteins that is insensitive to inhibition by 4-nitrobenzylthioinosine. (nih.gov)
  • A subtype of equilibrative nucleoside transporter proteins that is sensitive to inhibition by 4-nitrobenzylthioinosine. (lookformedical.com)
  • Proteins involved in the transport of NUCLEOSIDES across cellular membranes. (lookformedical.com)
  • The Transporter Classification Database (or TCDB ) is an International Union of Biochemistry and Molecular Biology (IUBMB)-approved classification system for membrane transport proteins , including ion channels . (wikipedia.org)
  • This graph shows the total number of publications written about "Nucleoside Transport Proteins" by people in this website by year, and whether "Nucleoside Transport Proteins" was a major or minor topic of these publications. (musc.edu)
  • Below are the most recent publications written about "Nucleoside Transport Proteins" by people in Profiles. (musc.edu)
  • Equilibrative nucleoside transporters (ENTs) are present at the blood-testis barrier (BTB), where they can facilitate antiviral drug disposition to eliminate a sanctuary site for viruses detectable in semen. (nih.gov)
  • ENT3 is unique as the only intracellular nucleoside transporter in the family with putative localization in late endosomes, lysosomes, and mitochondria (other human ENTs (hENTs) primarily function at the cell surface) 19 , 20 . (nature.com)
  • The purpose of this study was to investigate ENT-drug interactions with three nucleoside analogs, remdesivir, molnupiravir, and molnupiravir's active metabolite, β-d-N4-hydroxycytidine (EIDD-1931), and four non-nucleoside molecules repurposed as antivirals for coronavirus disease 2019 (COVID-19). (nih.gov)
  • Equilibrative nucleoside transporter 2 (ENT2) is a protein that in humans is encoded by the SLC29A2 gene. (wikipedia.org)
  • The SLC29A3 gene provides instructions for making a protein called equilibrative nucleoside transporter 3 (ENT3). (medlineplus.gov)
  • Protein expression was evaluated by western blot and immunocytochemistry and cytotoxicity by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. (nih.gov)
  • Although CLL cells lack hCNT3 activity, they do express this transporter protein, which is located mostly in the cytosol. (aianmodena.org)
  • TGF-beta1 acts through activation of ERK1/2 and the small GTPase RhoA to promote plasma membrane trafficking of the hCNT3 protein. (aianmodena.org)
  • No Cad-specific changes were identified, but a detailed erythroid Cad glycoprotein profile was obtained, especially for glycophorin-A (GLPA) O-glycosylation, equilibrative nucleoside transporter 1 (S29A1) O-glycosylation, and band 3 anion transport protein (B3AT) N-glycosylation. (scilifelab.se)
  • Mutations exclusively in equilibrative nucleoside transporter 3 (ENT3), the only intracellular nucleoside transporter within the solute carrier 29 ( SLC29 ) gene family, cause an expanding spectrum of human genetic disorders (e.g. (nature.com)
  • In this type of malignancy, the gemcitabine resistance is associated with a decreased level of human equilibrative nucleoside transporter 1 (hENT1) and acquisition of epithelial-to-mesenchymal transition (EMT) - like phenotype. (biomedcentral.com)
  • The most active single agent in CLL is the purine nucleoside analog fludarabine (9- β -D-arabinofuranosyl-2-fluoroadenine, or F-ara-A). Clinical studies of F-ara-A monotherapy in CLL have demonstrated it to be at least as effective as alkylator agent therapies, yielding responses in 63-79% of untreated patients and 32-48% of pretreated patients. (medscape.com)
  • Nelarabine is a purine nucleoside analog and antineoplastic agent used for the treatment of with acute T-cell lymphoblastic leukemia and T-cell lymphoblastic lymphoma with inadequate clinical response to prior chemotherapeutic treatments. (drugbank.com)
  • Nelarabine is a purine nucleoside analog converted to its corresponding arabinosylguanine nucleotide triphosphate (araGTP), resulting in the inhibition of DNA synthesis and cytotoxicity. (drugbank.com)
  • SGLT-2 inhibitors are became significantly connected with fat loss and reduced amount of blood circulation pressure by a comparatively large numbers of research. (exposed-skin-care.net)
  • An impact of upsurge in glucagon secretion by SGLT-2 inhibitors on metabolic risk elements remains unknown. (exposed-skin-care.net)
  • Right here we reviewed released content about the feasible anti-atherosclerotic results beyond blood sugar lowering from the SGLT-2 inhibitors. (exposed-skin-care.net)
  • The Search Technique for Released Content About the Anti-Atherosclerotic Results Beyond Glucose Reducing from the SGLT-2 Inhibitors We researched through the use of Pubmed (Desk 1), and discovered 770 released content about SGLT-2 inhibitors. (exposed-skin-care.net)
  • Ten types of SGLT-2 inhibitors had been discovered, and we researched the released content about each SGLT-2 inhibitor. (exposed-skin-care.net)
  • The amount of released content about dapagliflozin was the best among SGLT-2 inhibitors. (exposed-skin-care.net)
  • Since SGLT-2 inhibitors possess similar chemical buildings, we concentrated over the released content about dapagliflozin. (exposed-skin-care.net)
  • Decrease of bodyweight and blood circulation pressure by SGLT-2 inhibitors can be induced by osmotic diuretics [11]. (exposed-skin-care.net)
  • This was phenocopied by raising intracellular adenosine levels with a combination of inhibitors of adenosine kinase, adenosine deaminase, and the equilibrative nucleoside transporter: mature receptors with complex glycosylation accumulated at the cell surface and bound to an A 1 -selective antagonist with an affinity indistinguishable from the wild-type A 1 receptor. (aspetjournals.org)
  • solid course="kwd-title" Keywords: Type 2 diabetes mellitus, Sodium-glucose cotransporter 2 inhibitor, Center failure, Diuretic impact Intro Sodium-glucose cotransporter 2 (SGLT2) inhibitors certainly are a fresh class of dental hypoglycemic medicines that inhibit SGLT2 in the proximal tubules from the kidneys and decrease the blood sugar level by raising urinary blood sugar excretion. (cancerhugs.com)
  • Nevertheless, there's a significant difference in the hemodynamics ramifications of SGLT2 inhibitors and thiazide diuretics, which relates to a differing effect on the heartrate (HR). Aftereffect of SGLT2 Inhibitors for the HR A built-in evaluation of Japanese double-blind managed studies of luseogliflozin was performed [2-4]. (cancerhugs.com)
  • In a variety of animal types of nondiabetic kidney disease, metformin, GLP-1R agonists, DPP-4 inhibitors, and SGLT-2 inhibitors had been favorable to kidney function and morphology. (exposed-skin-care.net)
  • Considering the paucity of new brokers to treat kidney disease and the minimal adverse effects of metformin, GLP-1R agonists, DPP-4 inhibitors, and SGLT-2 inhibitors, these Ketanserin (Vulketan Gel) anti-diabetic brokers could be used in patients with non-diabetic kidney disease. (exposed-skin-care.net)
  • Equilibrative nucleoside transporter 2 (ENT2) was previously reported to have the dual ability of transporting both nucleosides and nucleobases. (bvsalud.org)
  • Drug Transporters at the Human Blood-Testis Barrier. (nih.gov)
  • Ribavirin (1- β -D-ribofuranosyl-1,2,4-triazole-3-carboxamide) is a nucleotide analogue of guanosine and a broad-spectrum direct antiviral agent (DAA). (hindawi.com)
  • Functional characterization of novel human and mouse equilibrative nucleoside transporters (hENT3 and mENT3) located in intracellular membranes. (medlineplus.gov)
  • B) HBL-2 cells had been pretreated with the vehicle alone (ara-C), F-Ara-A (F-ara-A+ara-C) or bendamustine (Bendamustine+ara-C), followed by the incubation with Ara-C. Intracellular Ara-CTP levels have been determined employing HPLC as described in Materials and Strategies. (idhinhibitor.com)
  • Patients (n=169) chronically infected with the hepatitis C virus genotype 1, treated with standard doses of pegylated interferon-α and weight-based doses of ribavirin for up to 48 weeks, were genotyped for 21 variants in nucleoside transporter genes SLC28A2, SLC28A3, SLC29A1, and SLC29A2, selected to include reported functional variants and to span the complete gene loci. (nih.gov)
  • Researchers believe that ENT3 transports nucleosides generated by the breakdown of DNA and RNA out of lysosomes into the cell so they can be reused. (medlineplus.gov)
  • A lack of ENT3 activity can also lead to a reduction in the amount of nucleosides in mitochondria. (medlineplus.gov)
  • As anticipated, each dilazep and NBTI just about totally abrogated the cytotoxic impact of cytosine arabinoside against HBL-2 and Namalwa cells, whereas they did. (idhinhibitor.com)
  • Mediates equilibrative transport of purine, pyrimidine nucleosides and the purine base hypoxanthine. (nih.gov)
  • 2002). "Functional and molecular characterization of nucleobase transport by recombinant human and rat equilibrative nucleoside transporters 1 and 2. (wikipedia.org)
  • Remdesivir and EIDD-1931 Interact with Human Equilibrative Nucleoside Transporters 1 and 2: Implications for Reaching SARS-CoV-2 Viral Sanctuary Sites. (nih.gov)
  • Facilitated mitochondrial import of antiviral and anticancer nucleoside drugs by human equilibrative nucleoside transporter-3. (medlineplus.gov)
  • In particular, expression levels of human equilibrative nucleoside transporter-1 and thymydilate synthase were significantly related to gemcitabine and 5-fluorouracil cytotoxicity. (nih.gov)
  • The drug of this class most commonly used in the treatment of chronic lymphocytic leukemia (CLL) is the pro-apoptotic nucleoside analog fludarabine (Flu), which enters CLL cells primarily through human equilibrative nucleoside transporters (hENTs). (aianmodena.org)
  • The effect of the inhibitor combination was specific, because it did not result in enhanced surface levels of two folding-defective human V 2 -vasopressin receptor mutants, which were susceptible to pharmacochaperoning by their cognate antagonist. (aspetjournals.org)
  • Anticancer nucleobase analogues 6-mercaptopurine and 6-thioguanine are novel substrates for equilibrative nucleoside transporter 2. (bvsalud.org)
  • Administration of the antiviral agents in combination with the anticancer drugs is known for positively influencing the effectiveness of the treatment [ 2 ]. (biomedcentral.com)
  • solid course="kwd-title" Keywords: Atherosclerosis, Blood circulation pressure, Bodyweight, Glucagon, Sodium-glucose cotransporter 2 inhibitor Launch Sodium-glucose cotransporter 2 (SGLT-2) mediates around 90% of energetic renal blood sugar reabsorption in the proximal tubule from the kidney [1]. (exposed-skin-care.net)
  • In the lab of Lori Sussel, Ph.D., she worked to model type 2 diabetes and analyze alternative splicing events in associated genes. (nih.gov)
  • Sulfhydryl analog of INOSINE that inhibits nucleoside transport across erythrocyte plasma membranes, and has immunosuppressive properties. (lookformedical.com)
  • Ribavirin is assimilated at 90% with a N1 nucleoside-transporter active mechanism in the proximal small intestine. (hindawi.com)
  • Adjuvant antiviral therapy also has a reported antiproliferative effect in some types of cancer [ 2 ]. (biomedcentral.com)
  • Mutations in codons 12 and 13 of K-ras exon 2 in colorectal tumors of Saudi Arabian patients: frequency, clincopathological associations, and clinical outcomes. (geneticsmr.com)
  • The aim of this study was (1) to address the genetic profile relevant to drug activity and (2) to evaluate differences between microdissected and non-microdissected tumors, normal tissues, and primary cell cultures. (nih.gov)
  • With chemical modification, nucleosides become the building blocks of DNA, its chemical cousin RNA, and molecules such as ATP and GTP, which serve as energy sources in the cell. (medlineplus.gov)
  • Molecules derived from nucleosides play an important role in many functions throughout the body. (medlineplus.gov)
  • CONCORD, Mass., July 11, 2017-Valerion Therapeutics, a clinical-stage biotechnology company that specializes in the development of therapies for orphan genetic diseases, today announced that it has initiated dosing in a Phase 1/2 clinical trial evaluating VAL-1221 in patients with late-onset Pompe disease. (amda-pompe.org)
  • The Company expects to report top-line data from the Phase 1/2 study in the fourth quarter of 2017. (amda-pompe.org)
  • In spontaneously hypertensive rats, metformin reduced proteinuria and increased the production of vascular endothelial growth factor (VEGF)-A in rat kidneys, probably by hypoxia-inducible factor (HIF)-2 activation [41]. (exposed-skin-care.net)
  • Raising cellular adenosine levels by subjecting cells to hypoxia (5% O 2 ) reproduced chaperoning by the inhibitor combination and enhanced surface expression of A 1 -receptor-Y 288 A within 1 hour. (aspetjournals.org)
  • RT-PCR revealed the expression of RNA of mouse equilibrative nucleoside transporter (mENT1) in mouse brain capillary and MBEC4 cells. (elsevierpure.com)
  • 18. Juuti A, Louhimo J, Nordling S, Ristimaki A, Haglund C.: Cyclooxygenase-2 expression correlates with poor prognosis in pancreatic cancer. (gastro-update.hu)
  • The brand new drug for type 2 diabetes, the sodium-glucose cotransporter 2 (SGLT-2) inhibitor, is reversible inhibitor of SGLT-2, resulting in reduced amount of renal glucose reabsorption and loss of plasma glucose, within an insulin-independent manner. (exposed-skin-care.net)
  • The SGLT-2 inhibitor is normally reversible inhibitor of SGLT-2, resulting in reduced amount of renal blood sugar reabsorption and loss of plasma blood sugar, within an insulin-independent way [2]. (exposed-skin-care.net)
  • Sotagliflozin3 Open up in another window Glucose, BODYWEIGHT and BLOOD CIRCULATION PRESSURE Lowering Ramifications of Dapagliflozin Dapagliflozin also reduces renal glucose reabsorption and loss of plasma glucose, within an insulin-independent manner [2], which induces reduced amount of bodyweight and blood circulation pressure. (exposed-skin-care.net)
  • Jabbour SA, Whaley JM, Tirmenstein M, Poucher SM, Reilly TP, Boulton DW, Saye J, List JF, Parikh S. Targeting renal glucose reabsorption for the treatment of type 2 diabetes mellitus using the SGLT2 inhibitor dapagliflozin. (jefferson.edu)
  • They speculate that the resulting impairment of nucleoside transport leads to a buildup of nucleosides in lysosomes and possibly in other cellular structures. (medlineplus.gov)
  • Nucleoside transport also plays a key role in the regulation of many physiologic processes through its effect on adenosine concentration at the cell surface (Griffiths et al. (nih.gov)
  • A sodium-glucose transporter that is expressed in the luminal membrane of the PROXIMAL KIDNEY TUBULES. (jefferson.edu)
  • The endogenous levels of the purine nucleoside, adenosine, increase significantly following cardiovascular events. (frontiersin.org)
  • As a nucleoside analog, Ara-GTP competes with endogenous deoxyGTP (dGTP) for incorporation into DNA. (drugbank.com)
  • 2. testicular disposition of clofarabine in rats is dependent on equilibrative nucleoside transporters. (nih.gov)
  • Southwest Oncology Group Study S0530: a phase 2 trial of clofarabine and cytarabine for relapsed or refractory acute lymphocytic leukaemia. (musc.edu)
  • Only in 1972, Geoff Burnstock (born: May 10, 1929, died: June 2, 2020) coined the term purinergic signalling referring to the extracellular effects of adenosine 5′-triphosphate (ATP). (frontiersin.org)
  • Mutations in codons 12/13 of K-ras exon 2 are associated with reduced benefit from anti-epidermal growth factor receptor antibody treatment for metastatic colorectal cancer (CRC). (geneticsmr.com)
  • Lately, the new medication for type 2 diabetes, the SGLT-2 inhibitor originated. (exposed-skin-care.net)
  • Matthaei et al examined ramifications of dapagliflozin 10 mg/time or placebo for 52 weeks on metabolic variables in sufferers with type 2 diabetes using sulphonylurea and metformin [12], HbA1c and fasting plasma sugar levels demonstrated better improvement from baseline with dapagliflozin (-0.8% and -1.5 mmol/L) than with placebo. (exposed-skin-care.net)
  • It really is widely accepted that weight problems and type 2 diabetes mellitus (T2DM) raise the risk of center failing (HF) independently of underlying coronary artery disease. (cancerhugs.com)
  • P 0.0001) in comparison to individuals treated with other classes of antidiabetic medicines (Empagliflozin, Cardiovascular Outcomes, and Mortality in Type 2 Diabetes (EMPA-REG OUTCOME) trial) [1]. (cancerhugs.com)
  • 2013. A randomized crossover study to assess the effect of an oat-rich diet on glycaemic control, plasma lipids and postprandial glycaemia, inflammation and oxidative stress in Type 2 diabetes . (hutton.ac.uk)
  • Pfizer Inc. (NYSE: PFE) today announced topline data from the Phase 2b clinical trial (NCT04707313) investigating its oral Glucagon-like peptide-1 receptor agonist (GLP-1RA) candidate, danuglipron (PF-06882961), in adults with obesity and without type 2 diabetes. (butwhatdoweknow.com)
  • To corroborate this assumption, we performed wash-out experiments and DAPK custom synthesis identified that only 3-hour exposure was adequate for bendamustine to elicit complete cytotoxic activity in HBL-2 cells (Figure 4D, left panel), whereas 4-OHCY expected a minimum of 12-hour exposure (Figure 4D, ideal panel). (idhinhibitor.com)
  • 2 Due to the rarity of these T-cell malignancies, nelarabine was first granted orphan drug status and a fast-track designation by the FDA to address the unmet therapeutic needs of these cancers. (drugbank.com)
  • 2. Boeck S, Stieber P, Holdenrieder S, Wilkowski R, Heinemann V.: Prognostic and therapeutic significance of carbohydrate antigen 19-9 as tumor marker in patients with pancreatic cancer. (gastro-update.hu)
  • Mesh term #2: (spine) OR (central nervous system). (biomedcentral.com)
  • Sodium-Glucose Transporter 2" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (jefferson.edu)
  • [ 2 ] Although different chemotherapeutic agents are used in the treatment of this indolent lymphoid malignancy, none have been shown to be superior in terms of survival advantage. (medscape.com)