Dimers found in DNA chains damaged by ULTRAVIOLET RAYS. They consist of two adjacent PYRIMIDINE NUCLEOTIDES, usually THYMINE nucleotides, in which the pyrimidine residues are covalently joined by a cyclobutane ring. These dimers block DNA REPLICATION.
Agencies of the FEDERAL GOVERNMENT of the United States.
A 34-amino acid polypeptide antibiotic produced by Streptococcus lactis. It has been used as a food preservative in canned fruits and vegetables, and cheese.
The process of discovering or asserting an objective or intrinsic relation between two objects or concepts; a faculty or power that enables a person to make judgments; the process of bringing to light and asserting the implicit meaning of a concept; a critical evaluation of a person or situation.
A basis of value established for the measure of quantity, weight, extent or quality, e.g. weight standards, standard solutions, methods, techniques, and procedures used in diagnosis and therapy.
An operating division of the US Department of Health and Human Services. It is concerned with the overall planning, promoting, and administering of programs pertaining to health and medical research. Until 1995, it was an agency of the United States PUBLIC HEALTH SERVICE.
An enzyme that catalyzes the reactivation by light of UV-irradiated DNA. It breaks two carbon-carbon bonds in PYRIMIDINE DIMERS in DNA.
The collective designation of three organizations with common membership: the European Economic Community (Common Market), the European Coal and Steel Community, and the European Atomic Energy Community (Euratom). It was known as the European Community until 1994. It is primarily an economic union with the principal objectives of free movement of goods, capital, and labor. Professional services, social, medical and paramedical, are subsumed under labor. The constituent countries are Austria, Belgium, Denmark, Finland, France, Germany, Greece, Ireland, Italy, Luxembourg, Netherlands, Portugal, Spain, Sweden, and the United Kingdom. (The World Almanac and Book of Facts 1997, p842)
Any enterprise centered on the processing, assembly, production, or marketing of a line of products, services, commodities, or merchandise, in a particular field often named after its principal product. Examples include the automobile, fishing, music, publishing, insurance, and textile industries.
Customer satisfaction or dissatisfaction with a benefit or service received.
The continuous sequence of changes undergone by living organisms during the post-embryonic developmental process, such as metamorphosis in insects and amphibians. This includes the developmental stages of apicomplexans such as the malarial parasite, PLASMODIUM FALCIPARUM.
A highly toxic gas that has been used as a chemical warfare agent. It is an insidious poison as it is not irritating immediately, even when fatal concentrations are inhaled. (From The Merck Index, 11th ed, p7304)
The terms, expressions, designations, or symbols used in a particular science, discipline, or specialized subject area.
Freedom from exposure to danger and protection from the occurrence or risk of injury or loss. It suggests optimal precautions in the workplace, on the street, in the home, etc., and includes personal safety as well as the safety of property.
Inorganic compounds derived from hydrochloric acid that contain the Cl- ion.
Unforeseen occurrences, especially injuries in the course of work-related activities.
Databases devoted to knowledge about specific chemicals.
Exclusive legal rights or privileges applied to inventions, plants, etc.
That portion of the electromagnetic spectrum immediately below the visible range and extending into the x-ray frequencies. The longer wavelengths (near-UV or biotic or vital rays) are necessary for the endogenous synthesis of vitamin D and are also called antirachitic rays; the shorter, ionizing wavelengths (far-UV or abiotic or extravital rays) are viricidal, bactericidal, mutagenic, and carcinogenic and are used as disinfectants.
The reconstruction of a continuous two-stranded DNA molecule without mismatch from a molecule which contained damaged regions. The major repair mechanisms are excision repair, in which defective regions in one strand are excised and resynthesized using the complementary base pairing information in the intact strand; photoreactivation repair, in which the lethal and mutagenic effects of ultraviolet light are eliminated; and post-replication repair, in which the primary lesions are not repaired, but the gaps in one daughter duplex are filled in by incorporation of portions of the other (undamaged) daughter duplex. Excision repair and post-replication repair are sometimes referred to as "dark repair" because they do not require light.
Injuries to DNA that introduce deviations from its normal, intact structure and which may, if left unrepaired, result in a MUTATION or a block of DNA REPLICATION. These deviations may be caused by physical or chemical agents and occur by natural or unnatural, introduced circumstances. They include the introduction of illegitimate bases during replication or by deamination or other modification of bases; the loss of a base from the DNA backbone leaving an abasic site; single-strand breaks; double strand breaks; and intrastrand (PYRIMIDINE DIMERS) or interstrand crosslinking. Damage can often be repaired (DNA REPAIR). If the damage is extensive, it can induce APOPTOSIS.
A rare, pigmentary, and atrophic autosomal recessive disease. It is manifested as an extreme photosensitivity to ULTRAVIOLET RAYS as the result of a deficiency in the enzyme that permits excisional repair of ultraviolet-damaged DNA.
An enzyme which catalyzes an endonucleolytic cleavage near PYRIMIDINE DIMERS to produce a 5'-phosphate product. The enzyme acts on the damaged DNA strand, from the 5' side of the damaged site.
A syndrome characterized by multiple system abnormalities including DWARFISM; PHOTOSENSITIVITY DISORDERS; PREMATURE AGING; and HEARING LOSS. It is caused by mutations of a number of autosomal recessive genes encoding proteins that involve transcriptional-coupled DNA REPAIR processes. Cockayne syndrome is classified by the severity and age of onset. Type I (classical; CSA) is early childhood onset in the second year of life; type II (congenital; CSB) is early onset at birth with severe symptoms; type III (xeroderma pigmentosum; XP) is late childhood onset with mild symptoms.
A trace element that constitutes about 27.6% of the earth's crust in the form of SILICON DIOXIDE. It does not occur free in nature. Silicon has the atomic symbol Si, atomic number 14, and atomic weight [28.084; 28.086].
Enzymes that are involved in the reconstruction of a continuous two-stranded DNA molecule without mismatch from a molecule, which contained damaged regions.
Nanometer-sized particles that are nanoscale in three dimensions. They include nanocrystaline materials; NANOCAPSULES; METAL NANOPARTICLES; DENDRIMERS, and QUANTUM DOTS. The uses of nanoparticles include DRUG DELIVERY SYSTEMS and cancer targeting and imaging.
Compounds possessing both a hydroxyl (-OH) and an amino group (-NH2).
Organic compounds containing the carboxy group (-COOH). This group of compounds includes amino acids and fatty acids. Carboxylic acids can be saturated, unsaturated, or aromatic.
A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.
Unstable isotopes of phosphorus that decay or disintegrate emitting radiation. P atoms with atomic weights 28-34 except 31 are radioactive phosphorus isotopes.
Inorganic salts of phosphoric acid.
A class of amino acids characterized by a closed ring structure.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.

Synthesis and evaluation of [18F]1-amino-3-fluorocyclobutane-1-carboxylic acid to image brain tumors. (1/266)

We have developed a new tumor-avid amino acid, 1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC), labeled with 18F for nuclear medicine imaging. METHODS: [18F]FACBC was prepared with high specific activity (no carrier added [NCA]) and was evaluated for its potential in tumor localization. A comparative study was performed for [18F]FACBC and [18F]2-fluorodeoxyglucose (FDG) in which the uptake of each agent in 9L gliosarcoma (implanted intracerebrally in Fisher 344 rats) was measured. In addition, the first human PET study of [18F]FACBC was performed on a patient with residual glioblastoma multiforme. Quantitative brain images of the patient were obtained by using a Siemens 921 47-slice PET imaging system. RESULTS: In the rat brain, the initial level of radioactivity accumulation after injection of [18F]FACBC was low (0.11 percentage injected dose per gram [%ID/g]) at 5 min and increased slightly to 0.26 %ID/g at 60 min. The tumor uptake exhibited a maximum at 60 min (1.72 %ID/g), resulting in a tumor-to-brain ratio increase of 5.58 at 5 min to 6.61 at 60 min. In the patient, the uptake of [18F]FACBC in the tumor exhibited a maximum concentration of 146 nCi/mL at 35 min after injection. The uptake of radioactivity in the normal brain tissue was low, 21 nCi/mL at 15 min after injection, and gradually increased to 29 nCi/mL at 60 min after injection. The ratio of tumor to normal tissue was 6 at 20 min after injection. The [18F]FACBC PET scan showed intense uptake in the left frontal region of the brain. CONCLUSION: The amino acid FACBC can be radiofluorinated for clinical use. [18F]FACBC is a potential PET tracer for tumor imaging.  (+info)

Thermogenic effects of sibutramine and its metabolites. (2/266)

1. The thermogenic activity of the serotonin and noradrenaline reuptake inhibitor sibutramine (BTS 54524; Reductil) was investigated by measuring oxygen consumption (VO2) in rats treated with sibutramine or its two pharmacologically-active metabolites. 2. Sibutramine caused a dose-dependent rise in VO2, with a dose of 10 mg kg(-1) of sibutramine or its metabolites producing increases of up to 30% that were sustained for at least 6 h, and accompanied by significant increases (0.5-1.0 degrees C) in body temperature. 3. Based on the accumulation in vivo of radiolabelled 2-deoxy-[3H]-glucose, sibutramine had little or no effect on glucose utilization in most tissues, but caused an 18 fold increase in brown adipose tissue (BAT). 4. Combined high, non-selective doses (20 mg kg(-1)) of the beta-adrenoceptor antagonists, atenolol and ICI 118551, inhibited completely the VO2 response to sibutramine, but the response was unaffected by low, beta1-adrenoceptor-selective (atenolol) or beta2-adrenoceptor-selective (ICI 118551) doses (1 mg kg(-1)). 5. The ganglionic blocking agent, chlorisondamine (15 mg kg(-1)), inhibited completely the VO2 response to the metabolites of sibutramine, but had no effect on the thermogenic response to the beta3-adrenoceptor-selective agonist BRL 35135. 6. Similar thermogenic responses were produced by simultaneous injection of nisoxetine and fluoxetine at doses (30 mg kg(-1)) that had no effect on VO2 when injected individually. 7. It is concluded that stimulation of thermogenesis by sibutramine requires central reuptake inhibition of both serotonin and noradrenaline, resulting in increased efferent sympathetic activation of BAT thermogenesis via beta3-adrenoceptor, and that this contributes to the compound's activity as an anti-obesity agent.  (+info)

Structural consequences of anesthetic and nonimmobilizer interaction with gramicidin A channels. (3/266)

Although interactions of general anesthetics with soluble proteins have been studied, the specific interactions with membrane bound-proteins that characterize general anesthesia are largely unknown. The structural modulations of anesthetic interactions with synaptic ion channels have not been elucidated. Using gramicidin A as a simplified model for transmembrane ion channels, we have recently demonstrated that a pair of structurally similar volatile anesthetic and nonimmobilizer, 1-chloro-1,2,2-trifluorocyclobutane (F3) and 1,2-dichlorohexafluorocyclobutane (F6), respectively, have distinctly different effects on the channel function. Using high-resolution NMR structural analysis, we show here that neither F3 nor F6 at pharmacologically relevant concentrations can significantly affect the secondary structure of the gramicidin A channel. Although both the anesthetic F3 and the nonimmobilizer F6 can perturb residues at the middle section of the channel deep inside the hydrophobic region in the sodium dodecyl sulfate micelles, only F3, but not F6, can significantly alter the chemical shifts of the tryptophan indole N-H protons near the channel entrances. The results are consistent with the notion that anesthetics cause functional change of the channel by interacting with the amphipathic domains at the peptide-lipid-water interface.  (+info)

Comparison of the potassium channel openers, WAY-133537, ZD6169, and celikalim on isolated bladder tissue and In vivo bladder instability in rat. (4/266)

The effects of the ATP-dependent potassium channel agonists ZD6169, celikalim, and WAY-133537 on bladder contractile function were examined in vitro on isolated bladder strips and in vivo on spontaneous bladder contractions. All three compounds produced a concentration-dependent relaxation of isolated rat detrusor strips (IC50 values = 0.93, 0.03, and 0.09 microM, respectively for ZD6169, celikalim, and WAY-133537. Contractile inhibition by all three compounds was fully reversed by 6 microM glyburide. These compounds also effectively inhibited spontaneous bladder contractions in the rat hypertrophied bladder model of detrusor instability. We also examined the electrophysiological properties of WAY-133537 on isolated rat bladder detrusor myocytes. Myocytes had an average resting membrane potential of -40 mV. Under patch current-clamp conditions, WAY-133537 (0.3 and 1.0 microM, n = 4-5) produced a significant hyperpolarization of 21 and 26 mV, respectively. Hyperpolarization was reversed by the addition of 5 microM glyburide. In patch voltage-clamp studies, WAY-133537 (0.3 microM, n = 3) significantly increased outward current in response to both voltage step and ramp protocols consistent with activation of the ATP-dependent potassium channel. In the detrusor instability model, WAY-133537 and celikalim had similar oral potencies (ED50 = 0.13 and 0.3 mg/kg, respectively), whereas ZD6169 was less potent (ED50 = 2.4 mg/kg). The antihypertensive agent celikalim exerted effects on the bladder at doses that significantly reduced systemic blood pressure. In contrast, both WAY-133537 and ZD6169 inhibited bladder hyperactivity at doses that produced minimal changes in both mean arterial blood pressure and heart rate. These data suggest that both WAY-133537 and ZD6169 may be useful in the treatment of bladder instability at doses associated with minimal hemodynamic side effects.  (+info)

Successful treatment of alopecia areata-like hair loss with the contact sensitizer squaric acid dibutylester (SADBE) in C3H/HeJ mice. (5/266)

A type of hair loss closely resembling human alopecia areata has been described in C3H/HeJ mice. In order to test the assumed analogy with human alopecia areata, we investigated the efficacy of treatment with the contact allergen squaric acid dibutylester. In 12 C3H/HeJ mice with alopecia areata an allergic contact dermatitis was induced and elicited weekly on one side of the back by topical applications of squaric acid dibutylester. Overt hair regrowth was observed only on the treated side of the back in nine of 12 mice. Histopathologic examination revealed a change in the distribution of the inflammatory infiltrate from a dense perifollicular lymphocytic infiltrate around the mid and lower regions of hair follicles in untreated skin to a uniform presence in the upper dermis in treated skin. Immunohistomorphometric studies revealed that treatment with squaric acid dibutylester increased the CD4+/CD8+ ratio from approximately 1:2 in untreated alopecia areata to 1:1 in treated alopecia areata. Additional immunohistochemical investigations showed an aberrant expression of major histocompatibility complex class I, major histocompatibility complex class II and intercellular adhesion molecule 1 on keratinocytes of the mid and lower parts of hair follicles in untreated alopecia areata. In successfully treated skin ectopic major histocompatibility complex class I and II expression was clearly reduced, whereas intercellular adhesion molecule 1 expression showed only minor changes. In conclusion, alopecia areata-like hair loss in C3H/HeJ mice responded to treatment with the contact sensitizer squaric acid dibutylester analogous to human alopecia areata. Moreover, successful treatment changes the aberrant expression of major histocompatibility complex class I and II in a way similar to that observed in human alopecia areata. These observations support the concept that alopecia areata-like hair loss in C3H/HeJ mice can be utilized as an appropriate model for the study of human alopecia areata.  (+info)

Distinctly different interactions of anesthetic and nonimmobilizer with transmembrane channel peptides. (6/266)

Although it plays no clinical role in general anesthesia, gramicidin A, a transmembrane channel peptide, provides an excellent model for studying the specific interaction between volatile anesthetics and membrane proteins at the molecular level. We show here that a pair of structurally similar volatile anesthetic and nonimmobilizer (nonanesthetic), 1-chloro-1,2,2-trifluorocyclobutane (F3) and 1, 2-dichlorohexafluorocyclobutane (F6), respectively, interacts differently with the transmembrane peptide. With 400 microM gramicidin A in a vesicle suspension of 60 mM phosphatidylcholine-phosphatidylglycerol (PC/PG), the intermolecular cross-relaxation rate constants between (19)F of F3 and (1)H in the chemical shift regions for the indole and backbone amide protons were 0.0106 +/- 0.0007 (n = 12) and 0.0105 +/- 0.0014 (n = 8) s(-1), respectively. No cross-relaxation was measurable between (19)F of F6 and protons in these regions. Sodium transport study showed that with 75 microM gramicidin A in a vesicle suspension of 66 mM PC/PG, F3 increased the (23)Na apparent efflux rate constant from 149.7 +/- 7.2 of control (n = 3) to 191.7 +/- 12.2 s(-1) (n = 3), and the apparent influx rate constant from 182.1 +/- 15.4 to 222.8 +/- 21.7 s(-1) (n = 3). In contrast, F6 had no effects on either influx or efflux rate. It is concluded that the ability of general anesthetics to interact with amphipathic residues near the peptide-lipid-water interface and the inability of nonimmobilizer to do the same may represent some characteristics of anesthetic-protein interaction that are of importance to general anesthesia.  (+info)

Studies on the role of serotonin receptor subtypes in the effect of sibutramine in various feeding paradigms in rats. (7/266)

The effect of the 5-hydroxytryptamine (5-HT) and noradrenaline (NA) reuptake inhibitor sibutramine was studied in food deprived, neuropeptide Y (NPY)- or muscimol-injected rats. Sibutramine dose-dependently reduced feeding caused by food-deprivation (ED50 = 5.1+/-0.8 mg kg(-1)) or by NPY injection into the paraventricular nucleus of the hypothalamus (ED50 = 6.0+/-0.5 mg kg(-1)). The increase in food intake caused by muscimol injected into the dorsal raphe was not modified by sibutramine (1-10 mg kg(-1)). The hypophagic effect of 5.1 mg kg(-1) sibutramine in food-deprived rats was studied in rats pretreated with different serotonin receptor antagonists. Metergoline (non-selective, 0.3 and 1.0 mg kg(-1)), ritanserin (5-HT2A/2C, 0.5 and 1.0 mg kg(-1)) and GR127935 (5-HT1B/1D), 0.5 and 1.0 mg kg(-1)) did not modify the hypophagic effect of sibutramine, while SB206553 (5-HT2B/2C, 5 and 10 mg kg(-1)) slightly but significantly reduced it (Fint(2.53) = 3.4; P<0.05). The reduction in food intake caused by 6.0 mg kg(-1) sibutramine in NPY-injected rats was not modified by GR127935 (1.0 mg kg(-1)). The results suggest that, with the possible exception of a partial involvement of 5-HT2B/2C receptors in sibutramine's hypophagia in food-deprived rats, 5-HT1 and 5-HT2 receptor subtypes do not play an important role in the hypophagic effect of sibutramine, at least in the first 2 h after injection.  (+info)

Subtype-selective inhibition of [methyl-3H]-N-methylscopolamine binding to muscarinic receptors by alpha-truxillic acid esters. (8/266)

Seven esters of alpha-truxillic acid have been synthesized: bis-3-piperidylpropyl ester and its quaternary bis-N-ethyl derivative, bis-N-diethylaminopropyl ester and its quaternary bis-N-methyl derivative, and bis-4-piperidylbutyl ester and its quaternary bis-N-methyl and bis-N-ethyl derivatives. All esters inhibited the specific binding of muscarinic receptor antagonist [methyl-3H]-N-methylscopolamine ([3H]-NMS) to muscarinic receptors in membranes of CHO cell lines stably expressing the human gene for the M1, M2, M3 or M4 subtype of muscarinic receptors. All esters displayed the highest potency at the M2 and the lowest potency at the M3 receptor subtype. In experiments performed on the M2 muscarinic receptor subtype, the affinity between the receptors and the esters was greatly increased when the concentration of ions was diminished. The highest affinities were found for the tertiary bis-3-piperidylpropyl and bis-4-piperidylbutyl aminoesters (equilibrium dissociation constants of 52 and 179 pM, respectively, in the low ionic strength medium). All investigated esters slowed down the dissociation of [3H]-NMS from the M2 muscarinic receptor subtype. [3H]-NMS dissociation from the M1, M3 and M4 muscarinic receptor subtypes was investigated in experiments with the bis-4-piperidylbutyl aminoester and also found to be decelerated. It is concluded that the esters of alpha-truxillic acid act as M2-selective allosteric modulators of muscarinic receptors and that, by their potency, the tertiary bis-3-piperidylpropyl and bis-4-piperidylbutyl aminoesters surpass the other known allosteric modulators of these receptors.  (+info)

Buy Sibutramine hydrochloride (CAS 84485-00-7), a water soluble serotonin, noradrenaline and dopamine reuptake inhibitor. Join researchers using high quality…
After the screening period, patients eligible for inclusion/exclusion criteria would administer Sibutramine placebo and Orlistat placebo during 2 weeks of the run-in period, Subsequently, subjects are randomized to 2 groups of the Sibutramine monotherapy group and the Orlistat and Sibutramine combination group. Sibutramine monotherapy group would receive Sibutramine 10mg once daily and Orlistat placebo three times daily for 12 weeks; the Orlistat and Sibutramine combination group would receive Sibutramine 10mg once daily and Orlistat 120mg three times daily for 12 weeks. After completing the dosing period, the occurrence of adverse events would be checked for 4 weeks and the study would be completed.. Body weight, abdominal CT(Computed Tomography)(visceral fat examination), body fat analysis, etc. would be measured before the study initiation and after 14 weeks of treatment, and comparatively analyzed. A two sample t-test is conducted for the inter-group comparison and a paired t-rest is ...
Moniliformin is a mycotoxin produced by certain fungi pathogenic to maize. It is capable of causing disease in domestic animals, possibly through inhibition of pyruvate dehydrogenase. Testing for MON commonly involves extraction of maize, isolation of moniliformin using solid-phase extraction columns and detection with high-performance liquid chromatography (HPLC) or gas chromatography. A capillary zone electrophoresisdiode array detection (CZE-DAD) method for determination of moniliformin in maize is reported. The extraction and isolation procedures are similar to those of a commonly used HPLC method, while the detection step requires only 10 min. Sixty-three samples of maize were tested by an established HPLC method using absorbance at 229 nm (HPLC-ultraviolet light) and by the CZE-DAD method. The limit of detection of the CZE-DAD method was 0.1 μg MON g-1 maize compared with 0.05 μg g-1 for the HPLC-ultraviolet light method. The CZE-DAD method gave good agreement with the HPLC-ultraviolet light
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EuroBolic.com: Sibutramine (trade name Meridia, Ectiva and Reductil), usually as sibutramine hydrochloride monohydrate, is an orally administered agent for the treatment of obesity, as an appetite suppressant. Meridia is a centrally-acting serotonin-norepinephrine reuptake inhibitor structurally related to amphetamines, although its mechanism of action is distinct.
Prof. Echavarrens group presents the first general enantioselective synthesis of cyclobutenes by intermolecular [2+2] cycloadditions. Digold complexes catalyse the reaction between terminal alkynes and alkenes leading to chiral cyclobutenes, useful in organic chemistry because they can be hydrogenated into functionalised cyclobutanes, which are motifs present in a variety of natural products and pharmaceuticals.. Previous attempts to achieve this transformation required activated alkynes or strained alkenes. The new strategy developed at ICIQ works for an enormous variety of terminal alkynes and a myriad of both disubstituted and trisubstituted alkenes. In total, this gold-catalysed reaction was used to synthesize a scope of over 40 different products, all with good yields and excellent enantiomeric ratios.. Due to the linear geometry of gold(I) complexes, chiral ligands are usually far away from the reaction centre. Hence, finding the gold catalysts that yield enantioselective transformations ...
Another strained ring system that we were interested in functionalizing was [1.1.0]Bicyclobutane for the synthesis of cyclobutylated amines. After attempts to functionalize bicyclobutane failed, we realized that we would need an anchoring group that was attached directly to bicyclobutane to make this reaction feasible. A reaxys search revealed that substituted phenylsulfonylbicyclobutanes could be aminated under high temperature in a neat mixture. Since we believed that a method to directly append cyclobutanes onto amines would be of value, we sought out to explore ways to make this reaction broadly applicable. We started by reasoning that placement of EWGs on the phenyl ring would increase the reactivity of the central bond which could allow for milder conditions which would hopefully lead to a broad substrate scope. After synthesizing a range of substituted phenylsulfonylbicyclobutanes, we chose to move forward with the 3,5-difluoro derivative because it offered a nice balance between ...
Another strained ring system that we were interested in functionalizing was [1.1.0]Bicyclobutane for the synthesis of cyclobutylated amines. After attempts to functionalize bicyclobutane failed, we realized that we would need an anchoring group that was attached directly to bicyclobutane to make this reaction feasible. A reaxys search revealed that substituted phenylsulfonylbicyclobutanes could be aminated under high temperature in a neat mixture. Since we believed that a method to directly append cyclobutanes onto amines would be of value, we sought out to explore ways to make this reaction broadly applicable. We started by reasoning that placement of EWGs on the phenyl ring would increase the reactivity of the central bond which could allow for milder conditions which would hopefully lead to a broad substrate scope. After synthesizing a range of substituted phenylsulfonylbicyclobutanes, we chose to move forward with the 3,5-difluoro derivative because it offered a nice balance between ...
This information should not be used to decide whether or not to take sibutramine or any other medicine. Only your health care provider has the knowledge and training to decide which medicines are right for you. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about sibutramine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to sibutramine. This information is not specific medical advice and does not replace information you receive from your health care provider. You must talk with your healthcare provider for complete information about the risks and benefits of using sibutramine.. ...
This trial will compare the efficacy and tolerability of induction chemotherapy with 5-fluorouracil and lobaplatin versus cisplatin followed by concurrent
Methods of making and using racemic and optically pure metabolites of sibutramine, and pharmaceutically acceptable salts, solvates, and clathrates thereof, are disclosed. Pharmaceutical compositions and dosage forms are also disclosed which comprise a dopamine reuptake inhibitor, such as a racemic or optically pure sibutramine metabolite, and optionally an additional pharmacologically active compound.
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Exposure–response model for sibutramine and placebo: suggestion for application to long-term weight-control drug development Seunghoon Han,1,2 Sangil Jeon,1,2 Taegon Hong,1,2 Jongtae Lee,1,2 Soo Hyeon Bae,1,2 Wan-su Park,1,2 Gab-jin Park,1,2 Sunil Youn,1,2 Doo Yeon Jang,1,2 Kyung-Soo Kim,3 Dong-Seok Yim1,2 1Department of Pharmacology, College of Medicine, The Catholic University of Korea, 2Pharmacometrics Institute for Practical Education and Training, 3Department of Family Medicine, Seoul St Mary’s Hospital, Seochogu, Seoul, Republic of KoreaAbstract: No wholly successful weight-control drugs have been developed to date, despite the tremendous demand. We present an exposure–response model of sibutramine mesylate that can be applied during clinical development of other weight-control drugs. Additionally, we provide a model-based evaluation of sibutramine efficacy. Data from a double-blind, randomized, placebo-controlled, multicenter study were used (N=120). Subjects in the treatment
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The study consisted of 4 periods: 1) a Screening Period of approximately 2 weeks; 2) a 6-week Lead-in Period, during which subjects received single-blind sibutramine and country-specific standard of care for weight management. Subjects who discontinued study drug treatment during the Lead-in Period were not randomized and did not participate in the double-blind Treatment Period or the Follow-up Period; 3) a double-blind Treatment Period in which subjects were randomized to 1 of the 2 treatment groups and were followed until the study ended; and 4) a double-blind Follow-up Period, during which randomized subjects who discontinued study drug were followed until the study ended. The Randomization Phase consisted of the double-blind Treatment Period and the double-blind Follow-up Period. Subjects received country-specific standard of care for weight management during the Randomization Phase.. An independent events adjudication committee evaluated all potential cardiovascular outcome events and ...
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Theoretical work in the field of unimolecular reactions raises some doubt whether or not high pressure limits to unimolecular rates do exist. The objective of the work was to study the unimolecular decomposition of some alkyl-substituted cyclobutanes at pressures as high as two hundred atmospheres, using nitrogen as a diluent gas, in an attempt to determine if the proposed limits actually exist. Small partial pressures (twenty to fifty mm Hg) of ethylcyclobutane were mixed from one hundred to four thousand psi of oxygen-free nitrogen and pyrolyzed at approximately four hundred ten degrees centigrade. Analyses were done on a Varian Aerograph six hundred D chromatograph with flame ionization detection. Despite serious experimental problems the search was successful and the predicted decrease of the rate constant was observed and verified. Measurements of this sort can provide kineticists with a new type of information about the nature of the transition state in unimolecular gas reactions. (Author)(
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Based on the concept of covalent capture of supramolecular assemblies, the idea of mechanical encapsulation is exploited for the protection and delivery of peptidebased molecules. This thesis aims to establish a general method for the encapsulation of peptides within a rotaxane structure, as well as studying their mode of release under specific stimuli. The synthesis of such structures, relying on the elongation of short peptido[2]rotaxanes, is applied to the design of rotaxane peptide carriers whose function is to protect against biological degradation and release peptides under a biological stimulus. These molecules are composed of a rotaxane-encapsulated peptide bearing a biodegradable stopper, the enzyme-specific cleavage of which triggers peptide release, via dethreading. The synthesis and in vitro assessment of rotaxane carriers as agents for anti-cancer therapy will be described in detail. The future challenges and potential applications of the proposed systems will be addressed ...
TY - JOUR. T1 - Synthesis and two-photon spectrum of a bis(porphyrin)-substituted squaraine. AU - Odom, Susan A.. AU - Webster, Scott. AU - Padilha, Lazaro A.. AU - Peceli, Davorin. AU - Hu, Honghua. AU - Nootz, Gero. AU - Chung, Sung Jae. AU - Ohira, Shino. AU - Matichak, Jonathan D.. AU - Przhonska, Olga V.. AU - Kachkovski, Alexei D.. AU - Barlow, Stephen. AU - Brédas, Jean Luc. AU - Anderson, Harry L.. AU - Hagan, David J.. AU - Van Stryland, Eric W.. AU - Marder, Seth R.. PY - 2009/6/10. Y1 - 2009/6/10. N2 - (Figure Presented) A chromophore in which zinc porphyrin donors are linked through their meso positions by ethynyl bridges to a bis(indolinylidenemethyl) squaraine core has been synthesized using Sonogashira coupling. The chromophore exhibits a two-photon absorption spectrum characterized by a peak cross section of 11000 GM and, more unusually, also exhibits a large cross section of ,780 GM over a photon-wavelength window 750 nm in width.. AB - (Figure Presented) A chromophore in which ...
Mechanically interlocked molecules (MIMs) have been attracting increasing interest since their emergence in the 1960s. The development of passive template and active template synthetic approaches facilitated the rapid growth in synthesis of various functionalised mechanically interlocked molecules (MIMs), allowing for a wide range of applications. In this thesis, Chapter 1 will discuss the synthetic methodologies from earliest statistical methods to passive templates and the latest active templates. Amongst the active template methodologies, the Cu catalysed alkyne azide cycloaddition (AT-CuAAC), together with its introduction, mechanistic studies as well as its application in syntheses of various functionalised rotaxanes will be presented. Chapter 2 will illustrate the discovery of an unexpected dinuclear Cu(I) complex during the investigation of an AT-CuAAC reaction and its selective demetallation. Chapter 3 highlights the important role of the mechanical geometry on stabilising a Pt(II) ...
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Squaric Acid Ester Amido Polyethylene Glycols are a novel class of reactive and chemoselective PEGylation reagents. The squaric acid PEG´s are chemoselective towards the amino groups of Lysin in protein PEGylation whereas the guanidine function of Arginine, the hydroxyl group of Serine and the imidazole function of Histidine are not affected. Literature: L 59 ...
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Asymmetric Synthesis of Cyclobutanones: Synthesis of Cyclobut-G Benjamin Darses, Andrew E. Greene & Jean-François Poisson* J. Org. Chem., 2012, 77 (4), 1710; DOI: 10.1021/jo202261z A synopsis by Peddabuddi Gopal Cycloalkanes are less stable than simple (acyclic) alkanes because of bond angle strain, which increases as the number of carbons in a ring decreases. Cyclopropanes (bond strain…
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"Fluorinated Cyclobutanes and Their Derivatives". In Zvi Rappoport; Joel F. Liebman (eds.). The Chemistry of Cyclobutanes. ...
Rappoport, Zvi; Liebman, Joel F. (2005). The Chemistry of Cyclobutanes. John Wiley & Sons. ISBN 9780470864012. Oda, Masaji; ...
Cyclobutane Cyclobutadiene Cyclobutyne Squaric acid J. Salaün; A. Fadel (1986). "Cyclobutene". Org. Synth. 64: 50. doi:10.15227 ... David M. Lemal; Xudong Chen (2005). "Fluorinated Cyclobutanes and Their Derivatives". In Zvi Rappoport; Joel F. Liebman (eds ... The Chemistry of Cyclobutanes. PATAI'S Chemistry of Functional Groups. doi:10.1002/0470864028.ch21. v t e. ...
Cava, M. P.; Deana, A. A.; Muth, K. (1959). "Condensed Cyclobutane Aromatic Compounds. VIII. The Mechanism of Formation of 1,2- ...
M. P. Cava, J. P. VanMeter (1969). "Condensed cyclobutane aromatic compounds. XXX. Synthesis of some unusual 2,3- ...
Setlow, R. B. (1966). "Cyclobutane-type pyrimidine dimers in polynucleotides". Science. 153 (734): 379-386. Bibcode:1966Sci... ...
Lindner, Patrick E.; Correa, Ricardo A.; Gino, James; Lemal, David M. (1996-01-01). "Novel Keto−Enol Systems: Cyclobutane ...
In his early pre-ETH period, his work included structure studies of cyclobutane, of ferrocene with the first description of its ... Dunitz, J. D.; Schomaker, V. (1952). "The Molecular Structure of Cyclobutane" (PDF). The Journal of Chemical Physics. 20 (11): ...
A cyclobutane pyrimidine dimer (CPD) contains a four membered ring arising from the coupling of the two double-bonded carbons ... Two common UV products are cyclobutane pyrimidine dimers (CPDs) and 6-4 photoproducts. These premutagenic lesions alter the ... Vink Arie A.; Roza Len (2001). "Biological consequences of cyclobutane pyrimidine dimers". Journal of Photochemistry and ... R. B. Setlow (1966). "Cyclobutane-Type Pyrimidine Dimers in Polynucleotides". Science. 153 (3734): 379-386. Bibcode:1966Sci... ...
This species is electronically related to cyclobutane. Theory suggest that the diatomic aluminium monobromide condenses to a ...
Cyclopropenes, aziridines and cyclobutanes may be formed in a similar manner. Carbon acids which can be deprotonated by sodium ...
1240-1241, doi:10.1021/ja01101a503 M.P. Cava, J.P. VanMeter (1969), "Condensed cyclobutane aromatic compounds. XXX. Synthesis ... "Condensed cyclobutane aromatic compounds. XIII. An attempted synthesis of 1,2-diphenylbenzocyclobutene", J. Org. Chem., 25 (9 ...
For simple non-planar cyclobutanes, dihedral angles range from 19 to 31°. CBDO's cis isomer crystallizes as two conformers with ... 1867-1870.doi:10.1107/S0567740876006559 Margulis, T.R. "Planar Cyclobutanes: Structure of 2,2,4,4-Tetramethylcyclobutane-trans- ...
Sinninghe, Damste (2002). "Linearly concatenated cyclobutane lipids form a dense bacterial membrane". Nature. 419 (6908): 708- ... which contain a series of cyclobutane ring structures. However, all other membranes within anammox bacteria are similar to ...
The final cyclobutane is formed by a Wolff rearrangement, and the alkyl chain is installed by a Wittig olefination. In 2016, ... UV irradiation of the solid produces the targeted [n]ladderane, with the C=C bonds reacting to form the fused cyclobutane ... In chemistry, a ladderane is an organic molecule containing two or more fused cyclobutane rings. The name arises from the ... Ladderanes with lengths up to 13 cyclobutane rings have been synthesized by Mehta and coworkers. This process involves the in ...
Structurally, the molecule consists of cyclopropane fused to cyclobutane. The synthesis of molecules containing multiple ...
Scheerer P, Zhang F, Kalms J, von Stetten D, Krauß N, Oberpichler I, Lamparter T (May 2015). "The class III cyclobutane ... Thiagarajan V, Byrdin M, Eker AP, Müller P, Brettel K (June 2011). "Kinetics of cyclobutane thymine dimer splitting by DNA ... The more common covalent linkage involves the formation of a cyclobutane bridge. Photolyases have a high affinity for these ... Teranishi, M., Nakamura, K., Morioka, H.,Yamamoto, K. and Hidema, J. (2008). "The native cyclobutane pyrimidine dimer ...
For large base-sizes, some of the cyclobutanes can be fused anti to each other, giving a non-convex polygon base. These are ... Chemically, it is a series of fused cyclobutane rings (a ladderane, with all-cis/all-syn geometry) that wraps around to join ... Their chemical formula is (C2H2)n, where n is the number of cyclobutane sides (the size of the cycloalkane base), and that ... For example, the structure of [12]prismane would have the cyclobutane chain twisted, with the dodecagonal bases non-planar and ...
Cyclobutane is a larger ring, but still has bent bonds. In this molecule, the carbon bond angles are 90° for the planar ... In terms of reactivity, cyclobutane is relatively inert and behaves like ordinary alkanes. An alternative model utilizes semi- ...
... formation of the equivalent cyclobutane derivative of acrylonitrile is "sluggish". Intramolecular [2+2] cyclizations have also ...
Steric interactions encourage the placement of large substituents on opposite sides of the new cyclobutane ring. If the enone ... Spin inversion to the singlet diradical allows closure to the cyclobutane. As an alternative a pericyclic reaction mechanism is ... which then recombine to the cyclobutane. Enone-alkene cycloadditions can produce two isomers, depending on the orientation of ...
cyclobutane, C4H8 - if it was completely square planar its bond angles would be 90° whereas tetrahedral 109.5° bond angles are ... The high strain energy of cyclobutane is primarily from angle strain. cyclopentane, C5H10 - if it was a completely regular ... The simplest examples of angle strain are small cycloalkanes such as cyclopropane and cyclobutane. In alkanes, optimum overlap ... Strain is most commonly discussed for small rings such as cyclopropanes and cyclobutanes, whose internal angles are ...
The compound is a diketone of cyclobutane, bearing four methyl groups. It is a white solid that is used as a precursor to ...
... (BCB) is a benzene ring fused to a cyclobutane ring. It has chemical formula C8H8. BCB is frequently used to ...
The neighboring pyrimidines form a cyclobutane pyrimidine dimer in a CPD lesion. DNA absorption of UV radiation can also lead ...
Cite journal requires ,journal= (help) Pradhan, Padmanava; Banerji, Asoke (1998). "Novel cyclobutane fused furochromone ...
Gordon, LK; Haseltine WA (1981). "Early Steps of Excision Repair of Cyclobutane Pyrimidine Dimers by the Micrococcus Luteus ... Brash, DE; Franklin WA; Sancar GB; Sancar A; Haseltine WA (1985). "E. coli DNA Photolyase Reverses Cyclobutane Pyrimidine ... Gordon, LK; Haseltine WA (1982). "Quantitation of Cyclobutane Pyrimidine Dimer Formation in Double and Single Stranded DNA ... Chan, GL; Doetsch PW; Haseltine WA (1985). "Cyclobutane Pyrimidine Dimers (6-4) Photo Product Block Polymerization by DNA ...
... cyclobutane pyrimidine dimers). Other Web sites state correctly that: "Coumarins produce photosensitivity therefore advise the ...
In these cations the electron deficiency is spread over the central cyclobutane ring. These dications were the first examples ...
Riener, Michelle; Nicewicz, David A. (2013). "Synthesis of cyclobutane lignans via an organic single electron oxidant-electron ...
Derivatives of cyclobutane are called cyclobutanes. Cyclobutane itself is of no commercial or biological significance, but more ... As such, cyclobutane is unstable above about 500 °C. The four carbon atoms in cyclobutane are not coplanar; instead the ring ... Cyclobutane is a cycloalkane and organic compound with the formula (CH2)4. Cyclobutane is a colourless gas and commercially ... 1,4-Dihalobutanes convert to cyclobutanes upon dehalogenation with reducing metals. Cyclobutane was first synthesized in 1907 ...
Quick, L.M.; Knecht, D.A.; Back, M.H., Kinetics of the formation of cyclobutane from ethylene, Int. J. Chem. Kinet., 1972, 4, ... Rathjens, G.W., Jr.; Gwinn, W.D., Heat capacities and entropy of cyclobutane, J. Am. Chem. Soc., 1953, 75, 5629-5633. [all data ... Coops, J.; Kaarsemaker, SJ., Heat of combustion of cyclobutane, Recl. Trav. Chim. Pays-Bas, 1950, 69, 1364. [all data] ... Rathjens G.W., Jr., Infrared absorption spectra, structure and thermodynamic properties of cyclobutane, J. Am. Chem. Soc., 1953 ...
Rathjens, G.W., Jr.; Gwinn, W.D., Heat capacities and entropy of cyclobutane, J. Am. Chem. Soc., 1953, 75, 5629-5633. [all data ... Coops, J.; Kaarsemaker, SJ., Heat of combustion of cyclobutane, Recl. Trav. Chim. Pays-Bas, 1950, 69, 1364. [all data] ...
Bromomethyl)cyclobutane. Regulatory process names 1 CAS names 1 IUPAC names 2 Trade names 1 Other identifiers 1 ...
This page contains information on the chemical Cyclobutane including: 3 synonyms/identifiers; U.S. Code of Federal Regulations ... Cyclobutane. Identifications. *Synonyms/Related:*Cyclobutane*Cyclobutane [UN2601] [Flammable gas]*Tetramethylene. Health & ... Cyclobutane (EnvironmentalChemistry.com),/a,- This page contains information on the chemical Cyclobutane including: 3 synonyms/ ... Cyclobutane. No. No. Related Resources. *USDOT Hazardous Materials Table 49 CFR 172.101. An online version of the USDOTs ...
Organo- and biocatalyzed eco-friendly approaches to cyclobutane-containing molecules have been developed with interesting ... In the last decade a certain number of new cyclobutane and cyclobutanone synthesis and functionalization protocols have been ... we report a critical survey on the literature concerning the enantiocontrolled synthesis and functionalization of cyclobutane ...
Purinyl and pyrimidinyl cyclobutanes and their use as antiviral agents. 1990-04-17. Zahler et al.. 514/262. ... Synthesis of SQ 33,054, A Novel Cyclobutane Nucleoside with Potent Antiviral Activity; Tetrahedron Letters, vol. 30, p. 6453 ( ...
... enzyme inhibition was due to the presence of cyclobutane pyrimidine dimers in the DNA. When 10-20 cyclobutane dimers were ... Inhibition of eukaryotic topoisomerase II by ultraviolet-induced cyclobutane pyrimidine dimers J Biol Chem. 1991 Oct 15;266(29 ... Results of the present study demonstrate that the repair of cyclobutane pyrimidine dimers is important for the efficient ...
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... cyclobutane-1-carboxylic acid; CAS Number: 35120-20-8; find Enamine-ENA429359342 MSDS, related peer-reviewed papers, technical ...
... the cyclobutane ring was able to tolerate acid and base treatments showing good chemical stability. A series of cyclobutane- ... cyclobutane-1,3-diacid (CBDA), is introduced to materials synthesis due to its great potentials. As an example of CBDA, α- ... the cyclobutane ring was able to tolerate acid and base treatments showing good chemical stability. A series of cyclobutane- ... Despite the prevalence of the cyclobutane unit in many natural products19,20,21,22,23,24,25 and synthetic drugs26,27,28,29,30, ...
... photoproducts and cyclobutane pyrimidine dimers have been measured in the UV-sensitive mutants of Saccharomyces cerevisiae: ... Repair of 6-4 photoproducts and cyclobutane pyrimidine dimers in rad mutants of Saccharomyces cerevisiae Mutat Res. 1994 Nov; ... Repair rates of both pyrimidine-pyrimidone (6-4) photoproducts and cyclobutane pyrimidine dimers have been measured in the UV- ... 5) No mutant repairs cyclobutane dimers more rapidly than 6-4 photoproducts. ...
Here, we demonstrate UV dose- and time-dependent induction of DNA damage in the form of cyclobutane pyrimidine dimers (CPD) in ... Kinetics of UV light-induced cyclobutane pyrimidine dimers in human skin in vivo: an immunohistochemical analysis of both ...
... cyclobutane-1-carboxylic acid , C14H14O2 , CID 70519439 - structure, chemical names, physical and chemical properties, ...
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The Native Cyclobutane Pyrimidine Dimer Photolyase of Rice Is Phosphorylated. Mika Teranishi, Kentaro Nakamura, Hiroshi Morioka ... The Native Cyclobutane Pyrimidine Dimer Photolyase of Rice Is Phosphorylated. Mika Teranishi, Kentaro Nakamura, Hiroshi Morioka ... The Native Cyclobutane Pyrimidine Dimer Photolyase of Rice Is Phosphorylated Message Subject (Your Name) has sent you a message ... The Native Cyclobutane Pyrimidine Dimer Photolyase of Rice Is Phosphorylated. Mika Teranishi, Kentaro Nakamura, Hiroshi Morioka ...
Solution-state structure of a DNA dodecamer duplex containing a Cis-syn thymine cyclobutane dimer, the major UV photoproduct of ... SOLUTION-STATE STRUCTURE OF A DNA DODECAMER DUPLEX CONTAINING A CIS-SYN THYMINE CYCLOBUTANE DIMER.. ...
The Roles of Several Residues of Escherichia coli DNA Photolyase in the Highly Efficient Photo-Repair of Cyclobutane Pyrimidine ... "The Roles of Several Residues of Escherichia coli DNA Photolyase in the Highly Efficient Photo-Repair of Cyclobutane Pyrimidine ...
... cyclobutane]-4-one; CAS Number: 1272756-10-1; Linear Formula: C11H11N3O3; find Accela ChemBio Inc.-AC5372910953 MSDS, related ...
Cyclobutane Pyrimidine Dimers are the Main Mutagenic DNA Photoproducts in DNA Repair-deficient Trichothiodystrophy Cells. ... Cyclobutane Pyrimidine Dimers are the Main Mutagenic DNA Photoproducts in DNA Repair-deficient Trichothiodystrophy Cells ... Cyclobutane Pyrimidine Dimers are the Main Mutagenic DNA Photoproducts in DNA Repair-deficient Trichothiodystrophy Cells ... Cyclobutane Pyrimidine Dimers are the Main Mutagenic DNA Photoproducts in DNA Repair-deficient Trichothiodystrophy Cells ...
3 Time-dependent formation of the cyclobutane thymine dimer in the 5S rRNA gene. Total incorporation of cyclobutane dimers (T^T ... 2 Formation of the cyclobutane thymine dimer within the 5S rRNA gene (X. borealis). Yields and distribution of the cyclobutane ... Accumulation of the cyclobutane thymine dimer in defined sequences of free and nucleosomal DNA†. Amethist S. Finch‡ a, William ... V. Lyamichev, Unusual conformation of (dA)n·(dT)n-tracts as revealed by cyclobutane thymine-thymine dimer formation, Nucleic ...
... pyrimidine cis-syn cyclobutane dimer. Such single-stranded moieties are useful models for the in uiuo situation because single ... DNA Backbone Conformation in Cis-Syn Pyrimidine[ ]Pyrimidine Cyclobutane Dimers. Broyde, Suse B.; Stellman, Steven D.; Hingerty ... pyrimidine cis-syn cyclobutane dimer. Such single-stranded moieties are useful models for the in uiuo situation because single ...
Cyclobutane pyrimidine dimers (CPDs) constitute a majority of DNA lesions caused by ultraviolet-B (UVB). CPD photolyase, which ... Cyclobutane pyrimidine dimers (CPDs) constitute a majority of DNA lesions caused by ultraviolet-B (UVB). CPD photolyase, which ... Hada M, Iida Y, Takeuchi Y (2000) Action spectra of DNA photolyases for photorepair of cyclobutane pyrimidine dimers in sorghum ... Pang Q, Hays JB (1991) UV-B inducible and temperature-sensitive photoreactivation of cyclobutane pyrimidine dimers in ...
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Cyclobutane dimer formation has been used to probe conformation of (dA)n.(dT)n-tracts cloned in plasmid DNA. The observed dimer ... Accumulation of the cyclobutane thymine dimer in defined sequences of free and nucleosomal DNA.. Amethist Shajary Finch, W. ... Cyclobutane dimer formation has been used to probe conformation of (dA)n.(dT)n-tracts cloned in plasmid DNA. The observed dimer ... Modulation of cyclobutane thymine photodimer formation in T11-tracts in rotationally phased nucleosome core particles and DNA ...
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UVA1 induces cyclobutane pyrimidine dimers but not 6-4 photoproducts in human skin in vivo. Abstract ... p53 mutant human glioma cells are sensitive to UV-C-induced apoptosis due to impaired cyclobutane pyrimidine dimer removal. ...
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  • The major UVB-induced lesions are cyclobutane pyrimidine dimers (CPDs) and pyrimidine-pyrimidone (6-4) photoproducts, which are formed between adjacent pyrimidines on the same strand ( Britt, 1996 ). (plantphysiol.org)
  • We have used the replicating shuttle vector pR2 to determine the role of ultraviolet C (UVC)-induced cyclobutane pyrimidine dimers (CPDs) and nondimer photoproducts in mutagenesis in human trichothiodystrophy (TTD) cells and in their repair-proficient counterparts obtained after complementation with the wild-type XPD/ERCC2 repair gene (TTD + ERCC2 cells). (aacrjournals.org)
  • Cyclobutane pyrimidine dimers (CPDs) constitute a majority of DNA lesions caused by ultraviolet-B (UVB). (springer.com)
  • The results show high levels and accumulation of UV-induced DNA lesions (strand breaks and cyclobutane pyrimidine dimers, CPDs) in different cells with RhoA loss of function ( LoF ), either by stable overexpression of negative dominant RhoA (RhoA-N19 mutant), by inhibition with C3 toxin or by transient silencing with siRNA. (frontiersin.org)
  • Two common UV products are cyclobutane pyrimidine dimers (CPDs) and 6-4 photoproducts . (wikipedia.org)
  • Mutations in sunlight-induced melanoma arise from cyclobutane pyrimidine dimers (CPDs), DNA photoproducts that are typically created picoseconds after an ultraviolet (UV) photon is absorbed at thymine or cytosine. (sciencemag.org)
  • Escherichia coli DNA photolyase is a DNA-repair enzyme that repairs cyclobutane pyrimidine dimers (CPDs) that are formed on DNA upon exposure of cells to ultraviolet light. (montclair.edu)
  • UV-B radiation damages nuclear, chloroplast and mitochondrial DNA by the formation of cyclobutane pyrimidine dimers (CPDs), which are the primary UV-B-induced DNA lesions, and are a principal cause of UV-B-induced growth inhibition in plants. (elsevier.com)
  • The present study is extended from mouse model to human system in vivo to determine the effect of topical application of GTP to human individuals against UV light-induced DNA damage in the form of cyclobutane pyrimidine dimers (CPDs) in the skin. (aacrjournals.org)
  • As determined by DNA photolyase-catalyzed photoreactivation experiments, enzyme inhibition was due to the presence of cyclobutane pyrimidine dimers in the DNA. (nih.gov)
  • Results of the present study demonstrate that the repair of cyclobutane pyrimidine dimers is important for the efficient catalytic function of topoisomerase II. (nih.gov)
  • Repair rates of both pyrimidine-pyrimidone (6-4) photoproducts and cyclobutane pyrimidine dimers have been measured in the UV-sensitive mutants of Saccharomyces cerevisiae: rad1 to rad12 and rad14 to rad24. (nih.gov)
  • A dot blot immunoassay for UV photoproducts was used which measures lesions in the genome as a whole and which distinguishes 6-4 photoproducts from cyclobutane dimers. (nih.gov)
  • The principal findings are: (1) Wild-type yeast cells, like normal mammalian cells, repair 6-4 photoproducts more rapidly than cyclobutane dimers. (nih.gov)
  • 5) No mutant repairs cyclobutane dimers more rapidly than 6-4 photoproducts. (nih.gov)
  • Kinetics of UV light-induced cyclobutane pyrimidine dimers in human skin in vivo: an immunohistochemical analysis of both epidermis and dermis. (nih.gov)
  • Here, we demonstrate UV dose- and time-dependent induction of DNA damage in the form of cyclobutane pyrimidine dimers (CPD) in skin cells following a single exposure of human skin to UV radiation. (nih.gov)
  • Lei Xu and Guoping Zhu, "The Roles of Several Residues of Escherichia coli DNA Photolyase in the Highly Efficient Photo-Repair of Cyclobutane Pyrimidine Dimers," Journal of Nucleic Acids , vol. 2010, Article ID 794782, 7 pages, 2010. (hindawi.com)
  • Both the distribution of cyclobutane thymine dimers and the genetic changes caused by irradiation are heterogeneous within cellular DNA. (rsc.org)
  • 14-17 Single-stranded DNA also generates more cyclobutane thymine dimers than double-stranded DNA of equivalent sequence, 18 and triplex formation further suppresses thymine dimerization in a helix. (rsc.org)
  • 22-24 A similar distribution of cyclobutane dimers is not evident after irradiation of the same DNA in the absence of NCP. (rsc.org)
  • The detection of cyclobutane thymine dimers, (6-4) photolesions and the Dewar photoisomers in sections of UV-irradiated human skin using specific antibodies, and the demonstration of depth penetration effects. (openrepository.com)
  • Establishment of a monoclonal antibody recognizing cyclobutane-type thymine dimers in DNA: a comparative study with 64M-1 antibody specific for (6-4)photoproducts. (openrepository.com)
  • In human cells, it is primarily responsible for repair of UV-induced cyclobutane pyrimidine dimers (CPD) and (6-4) photoproducts. (pnas.org)
  • Results for Reference: Human mitochondrial DNA polymerase γ exhibits potential for bypass and mutagenesis at UV-induced cyclobutane thymine dimers. (neb.com)
  • We also observed that the removal of cyclobutane pyrimidine dimers from the dihydrofolate reductase and c-MYC genes in mitotic cells was very slow. (elsevier.com)
  • This suggests that transcription-coupled repair of cyclobutane pyrimidine dimers is compromised or non-functional during mitosis, which is probably the consequence of mitotic transcriptional repression. (elsevier.com)
  • Monoclonal antibody to cyclobutane thymine dimers (clone KTM53, IgG1) was purchased from Kamiya Biomedical Company (Seattle, WA). (aacrjournals.org)
  • These UV rays cause kinks in the DNA of cells called cyclobutane pyrimidine dimers. (newscientist.com)
  • Cyclobutane pyrimidine dimers (CPD) and 6-4 photoproducts are precursors to the C/T and CC/TT transitions that are the classic "UV signature" mutations. (bmj.com)
  • Derivatives of cyclobutane are called cyclobutanes. (wikipedia.org)
  • Cyclobutane itself is of no commercial or biological significance, but more complex derivatives are important in biology and biotechnology. (wikipedia.org)
  • 2.3 Cyclobutanes and their derivatives. (wiley.com)
  • and highly unsaturated cyclobutane derivatives. (thefreedictionary.com)
  • In an attempt to locate possible characteristic frequencies of the C_4-ring, the infrared spectra of 191 cyclobutane derivatives have been examined. (caltech.edu)
  • When cis-syn cyclobutane pyrimidine dimer was used as substrate, the Michaelis constant (K m ) value for the photolyase activity was 100nM. (elsevier.com)
  • Ultraviolet (UV) radiation has dangerous effects on the skin that may cause multiple clinical and cellular effects, which will produce DNA damage characterized by formation of photoproducts such as cyclobutane pyrimidine dimer (CPD), and acute inflammation characterized by neutrophil infiltration in the skin tissues. (sciencepublishinggroup.com)
  • The infrared spectra of cyclobutane compounds. (caltech.edu)
  • The most useful correlations appear to be a band near 1235 cm.^(-1) for cyclobutane compounds with at least one ring methylene group, and a band near 915 cm.^(-1) for mono- and 1,1-disubstituted cyclobutanes. (caltech.edu)
  • A previously overlooked building block, cyclobutane-1,3-diacid (CBDA), is introduced to materials synthesis due to its great potentials. (nature.com)
  • The synthesis of a 5,10-seco steroid containing two double bonds in a AB-macrocycle as well as the preparation of a steroidal skeleton with a cyclobutane fragment is described. (wur.nl)
  • Photostationary levels of the cyclobutane thymine dimer have now been quantified in homogenous samples of DNA reconstituted into nucleosome core particles to examine the basis for previous observations that such structures could induce a periodicity in dimer yield when libraries of heterogeneous sequences were used. (rsc.org)
  • Scheme 1 Formation and repair of the cyclobutane thymine dimer. (rsc.org)
  • Unusual conformation of (dA)n.(dT)n-tracts as revealed by cyclobutane thymine-thymine dimer formation. (semanticscholar.org)
  • Accumulation of the cyclobutane thymine dimer in defined sequences of free and nucleosomal DNA / Amethist S. Finch, William B. Davis, and Steven E. Rokita. (exlibrisgroup.com)
  • The ring strain energy of cyclobutane is about 20.1 and 26.2 kcal/mol higher than that of cyclopentane and cylcohexane, respectively 37 . (nature.com)
  • DNA dynamics, conformation and flexibility have all been implicated in the yield of cyclobutane thymine dimerization. (rsc.org)
  • A theoretical calculation involving minimization of energy functions was made to determine the conformation of a deoxydinucleoside monophosphate pyrimidine[ ]pyrimidine cis-syn cyclobutane dimer. (columbia.edu)
  • Cyclobutane dimer formation has been used to probe conformation of (dA)n.(dT)n-tracts cloned in plasmid DNA. (semanticscholar.org)
  • Photochemical cyclobutane dimerization of adjacent thymines generates the major lesion in DNA caused by exposure to sunlight. (rsc.org)
  • Cyclobutane is a cycloalkane and organic compound with the formula (CH2)4. (wikipedia.org)
  • Simultaneous establishment of monoclonal antibodies specific for either cyclobutane pyrimidine dimer or (6-4)photoproduct from the same mouse immunized with ultraviolet-irradiated DNA. (openrepository.com)
  • citation needed] Cyclobutane photodimers (CPD) are formed by photochemical reactions that result in the coupling of the C=C double bonds of pyrimidines. (wikipedia.org)
  • One unusual example is pentacycloanammoxic acid, which is a ladderane composed of 5 fused cyclobutane units. (wikipedia.org)
  • Carboplatin is a popular anticancer drug that is derived from cyclobutane-1,1-dicarboxylic acid. (wikipedia.org)
  • While its two carboxylic acid groups can be readily utilized in connecting with other molecules to form new materials, the cyclobutane ring was able to tolerate acid and base treatments showing good chemical stability. (nature.com)
  • 1 The resulting thymine -thymine cyclobutane dimer product was soon identified as the major DNA lesion formed by UV irradiation of cells and was associated with the mutagenic and carcinogenic effects of solar irradiation. (rsc.org)
  • n-, iso- and cyclo-alk en es and -alk yn es (unsaturated hydrocarbons). (wikipedia.org)
  • Initial rate studies did not reveal a similar periodicity when a homogenous core particle was analyzed, but this approach examined only formation of this photochemically reversible cyclobutane dimer. (rsc.org)
  • Utin Variantini, Safruddin Amin, Anni Adriani, Idham Jaya Ganda, Gemini Alam, M. Husni Cangara, The Protection Effect of Topical Cocoa Extract on Cyclobutane Pyrimidine Dimer (CPD) Formation and Tissue Neutrophil in Mice Induced by Ultraviolet B, American Journal of Clinical and Experimental Medicine . (sciencepublishinggroup.com)
  • Therefore, we hypothesized that cyclobutane has sufficient thermal and sunlight stability for many potential applications in materials. (nature.com)
  • The cyclobutane pyrimidine dimer (CPD) is a major type of DNA damage induced by ultraviolet B (UVB) radiation. (plantphysiol.org)
  • 1. The exact structure of the cyclobutane is not known. (orgsyn.org)