A paralytic condition of the legs caused by ingestion of lathyrogens, especially BETA-AMINOPROPIONITRILE or beta-N-oxalyl amino-L-alanine, which are found in the seeds of plants of the genus LATHYRUS.
Cyanomethylamine.
A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms.
Compounds consisting of benzene rings linked to each other in either ortho, meta or para positions. Permitted are any substitutions, but ring fusion to any of the benzene rings is not allowed.
Inorganic and organic derivatives of sulfuric acid (H2SO4). The salts and esters of sulfuric acid are known as SULFATES and SULFURIC ACID ESTERS respectively.
Oxy acids of sulfur with the general formula RSOH, where R is an alkyl or aryl group such as CH3. They are often encountered as esters and halides. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.
A clear, odorless, tasteless liquid that is essential for most animal and plant life and is an excellent solvent for many substances. The chemical formula is hydrogen oxide (H2O). (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A compound used as an x-ray contrast medium that occurs in nature as the mineral barite. It is also used in various manufacturing applications and mixed into heavy concrete to serve as a radiation shield.
Agents destructive to parasitic worms. They are used therapeutically in the treatment of HELMINTHIASIS in man and animal.
A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.
A benzimidazole broad-spectrum anthelmintic structurally related to MEBENDAZOLE that is effective against many diseases. (From Martindale, The Extra Pharmacopoeia, 30th ed, p38)
Commonly known as parasitic worms, this group includes the ACANTHOCEPHALA; NEMATODA; and PLATYHELMINTHS. Some authors consider certain species of LEECHES that can become temporarily parasitic as helminths.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
Infections or infestations with parasitic organisms. The infestation may be experimental or veterinary.
Infestation with parasitic worms of the helminth class.
Spectrophotometry in the infrared region, usually for the purpose of chemical analysis through measurement of absorption spectra associated with rotational and vibrational energy levels of molecules. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A plant family of the order Bromeliales, subclass Zingiberidae, class Liliopsida (monocotyledons).
The theory that the radiation and absorption of energy take place in definite quantities called quanta (E) which vary in size and are defined by the equation E=hv in which h is Planck's constant and v is the frequency of the radiation.
A spectroscopic technique in which a range of wavelengths is presented simultaneously with an interferometer and the spectrum is mathematically derived from the pattern thus obtained.
Prepared food that is ready to eat or partially prepared food that has a final preparation time of a few minutes or less.
Theoretical representations that simulate the behavior or activity of chemical processes or phenomena; includes the use of mathematical equations, computers, and other electronic equipment.
A genus of parasitic nematode worms which infest the duodenum and stomach of domestic and wild herbivores, which ingest it with the grasses (POACEAE) they eat. Infestation of man is accidental.
Infection with nematodes of the genus HAEMONCHUS, characterized by digestive abnormalities and anemia similar to that from hookworm infestation.
An order of nematodes of the subclass SECERNENTEA. Characteristics include an H-shaped excretory system with two subventral glands.
Diseases of domestic and mountain sheep of the genus Ovis.
Substances used in the treatment or control of nematode infestations. They are used also in veterinary practice.
The relationship between an invertebrate and another organism (the host), one of which lives at the expense of the other. Traditionally excluded from definition of parasites are pathogenic BACTERIA; FUNGI; VIRUSES; and PLANTS; though they may live parasitically.

Synergistic induction of apoptosis in human leukemia cells (U937) exposed to bryostatin 1 and the proteasome inhibitor lactacystin involves dysregulation of the PKC/MAPK cascade. (1/44)

Cotreatment with a minimally toxic concentration of the protein kinase C (PKC) activator (and down-regulator) bryostatin 1 (BRY) induced a marked increase in mitochondrial dysfunction and apoptosis in U937 monocytic leukemia cells exposed to the proteasome inhibitor lactacystin (LC). This effect was blocked by cycloheximide, but not by alpha-amanitin or actinomycin D. Qualitatively similar interactions were observed with other PKC activators (eg, phorbol 12-myristate 13-acetate and mezerein), but not phospholipase C, which does not down-regulate the enzyme. These events were examined in relationship to functional alterations in stress (eg, SAPK, JNK) and survival (eg, MAPK, ERK) signaling pathways. The observations that LC/BRY treatment failed to trigger JNK activation and that cell death was unaffected by a dominant-interfering form of c-JUN (TAM67) or by pretreatment with either curcumin or the p38/RK inhibitor, SB203580, suggested that the SAPK pathway was not involved in potentiation of apoptosis. In marked contrast, perturbations in the PKC/Raf/MAPK pathway played an integral role in LC/BRY-mediated cell death based on evidence that pretreatment of cells with bisindolylmaleimide I, a selective PKC inhibitor, or geldanamycin, a benzoquinone ansamycin, which destabilizes and depletes Raf-1, markedly suppressed apoptosis. Furthermore, ERK phosphorylation was substantially prolonged in LC/BRY-treated cells compared to those exposed to BRY alone, and pretreatment with the highly specific MEK inhibitors, PD98059, U0126, and SL327, opposed ERK activation while protecting cells from LC/BRY-induced lethality. Together, these findings suggest a role for activation and/or dysregulation of the PKC/MAPK cascade in modulation of leukemic cell apoptosis following exposure to the proteasome inhibitor LC. (Blood. 2001;97:2105-2114)  (+info)

Alcohol-induced c-Fos expression in the Edinger-Westphal nucleus: pharmacological and signal transduction mechanisms. (2/44)

Mapping inducible transcription factors has shown that the Edinger-Westphal nucleus is preferentially sensitive to alcohol intoxication. Herein, we characterize the pharmacological and signal transduction mechanisms related to alcohol-induced c-Fos expression in Edinger-Westphal neurons. Using immunohistochemistry, we show that pretreatment with gamma-aminobutyric acid (GABA)-ergic antagonists (4 mg/kg bicuculline and 45 mg/kg pentylenetetrazole) attenuates induction of c-Fos expression by alcohol (2.4 g/kg, intraperitoneal). In addition, 10 mg/kg 2-(2,3-dihydro-2-methoxy-1,4-benzodioxin-2-yl)4,5-dihydro-1H-imidazole (RX 821002), an alpha(2A/D)-adrenoceptor antagonist, and 20 mg/kg haloperidol, a dopamine antagonist, also block alcohol-induced c-Fos expression in Edinger-Westphal neurons. No effects were seen in alcohol-induced c-Fos after the pretreatment of 20 mg/kg propranolol (beta-adrenoceptor antagonist), 10 mg/kg 2-(2-(4-(2-methoxyphenyl)piperazin-1-yl) ethy)-4,4-dimethyl-1,3-(2H,4H)-isoquinolindione dihydrochloride (ARC 239) (alpha(2B/C)-adrenoceptor antagonist), or 30 mg/kg naltrexone (opioid antagonist). Although positive modulators for the GABA(A) receptor (20 mg/kg 3alpha-hydroxy-5alpha-pregnan-20-one and 10-30 mg/kg chlordiazepoxide) and opioid receptor (10 mg/kg morphine) produced significant elevations, agonists for alpha(2)-adrenoceptors (clonidine) and dopamine receptors (apomorphine) had no effect on Edinger-Westphal c-Fos expression. These findings suggest that alcohol-induced c-Fos expression in Edinger-Westphal results from direct interactions with GABA(A) receptors, which are modified by alpha(2A/D)-adrenoceptors and dopamine receptors. Also using immunohistochemistry to identify potential intracellular mechanisms associated with alcohol-induced c-Fos expression in Edinger-Westphal, we show time-dependent increases in serine 727 phospho-signal transducer and activator of transcription 3 (Stat3) but no changes in phospho-cAMP response element-binding protein and phospho-Elk1. Time-dependent increases in phospho-extracellular signal-regulated kinase (ERK) 1/2 were found to occur simultaneously with increases in serine 727 phospho-Stat3. Finally, blockade of ERK 1/2 phosphorylation with the mitogen-activated protein kinase (MEK) 1/2 inhibitor SL327 blocked alcohol-induced c-Fos expression, suggesting that alcohol induces c-Fos in Edinger-Westphal neurons through activation of the MEK1/2-ERK1/2-Stat3 pathway.  (+info)

Significant neuroprotection against ischemic brain injury by inhibition of the MEK1 protein kinase in mice: exploration of potential mechanism associated with apoptosis. (3/44)

MEK1/2 is a serine/threonine protein kinase that phosphorylates and activates extracellular signal-responsive kinase (ERK)1/2. In the present study we explored the role of MEK1/2 in ischemic brain injury using a selective MEK1/2 inhibitor, SL327, in mice. C57BL/6 mice were subjected to a 30-min occlusion of the middle cerebral artery (MCAO) followed by reperfusion. Western blot analysis demonstrated the immediate activation of MEK/ERK after reperfusion (within the first 10 min) in the ischemic brain; this activation was dose dependently blocked by SL327 (10-100 mg/kg, i.p.). A single dose of SL327 (100 mg/kg) administered 15 min before or 25 min after the onset of ischemia resulted in 63.6% (n = 18, p < 0.001) and 50.7% (n = 18, p < 0.01) reduction in infarct size, respectively, compared with vehicle-treated mice. Similarly, SL327 significantly reduced neurological deficits 1 to 3 days after reperfusion (n = 12, p < 0.01). The salutary effect of SL327-induced neuroprotection was independent of mitochondrial cytochrome c release or caspase-8-mediated apoptosis; however, SL327 markedly suppressed the levels of active caspase-3 and DNA fragmentation (as a measure of apoptosis) after ischemia/reperfusion. Our data suggest that the inhibition of MEK1/2 results in neuroprotection from reperfusion injury and that this protection may be associated with the reduction in apoptosis.  (+info)

A role for ERK MAP kinase in physiologic temporal integration in hippocampal area CA1. (4/44)

Recent studies demonstrate a requirement for the Extracellular signal Regulated Kinase (ERK) mitogen-activated protein kinase (MAPK) cascade in both the induction of long-lasting forms of hippocampal synaptic plasticity and in hippocampus-dependent associative and spatial learning. In the present studies, we investigated mechanisms by which ERK might contribute to synaptic plasticity at Schaffer collateral synapses in hippocampal slices. We found that long-term potentiation (LTP) induced with a pair of 100-Hz tetani does not require ERK activation in mice whereas it does in rats. However, in mice, inhibition of ERK activation blocked LTP induced by two LTP induction paradigms that mimicked the endogenous theta rhythm. In an additional series of studies, we found that mice specifically deficient in the ERK1 isoform of MAPK showed no impairments in tests of hippocampal physiology. To investigate ERK-dependent mechanisms operating during LTP-inducing stimulation paradigms, we monitored spike production in the cell body layer of the hippocampus during the period of theta-like LTP-inducing stimulation. Theta-burst stimulation (TBS) produced a significant amount of postsynaptic spiking, and the likelihood of spike production increased progressively over the course of the three trains of TBS independent of any apparent increase in Excitatory Post-Synaptic Potential (EPSP) magnitude. Inhibition of ERK activation dampened this TBS-associated increase in spiking. These data indicate that, for specific patterns of stimulation, ERK may function in the regulation of neuronal excitability in hippocampal area CA1. Overall, our data indicate that the progressive increase in spiking observed during TBS represents a form of physiologic temporal integration that is dependent on ERK MAPK activity.  (+info)

Preparation of (cyanomethylene)trimethylphosphorane as a new Mitsunobu-type reagent. (5/44)

(Cyanomethylene)trimethylphosphorane (CMMP) mediates Mitsunobu-type reactions, which are a versatile method for the alkylation of various nucleophiles (HA) with alcohols (ROH) to give RA. CMMP is quite effective for the reaction of carbon nucleophiles whose pK(a) value are higher than 13. CMMP, which is very sensitive to air and moisture, was synthesized in two steps starting from chloroacetonitrile.  (+info)

The role of the extracellular signal-regulated kinase signaling pathway in mood modulation. (6/44)

The neurobiological underpinnings of mood modulation, molecular pathophysiology of manic-depressive illness, and therapeutic mechanism of mood stabilizers are largely unknown. The extracellular signal-regulated kinase (ERK) pathway is activated by neurotrophins and other neuroactive chemicals to produce their effects on neuronal differentiation, survival, regeneration, and structural and functional plasticity. We found that lithium and valproate, commonly used mood stabilizers for the treatment of manic-depressive illness, stimulated the ERK pathway in the rat hippocampus and frontal cortex. Both drugs increased the levels of activated phospho-ERK44/42, activated phospho-ribosomal protein S6 kinase-1 (RSK1) (a substrate of ERK), phospho-CREB (cAMP response element-binding protein) and phospho-B cell lymphoma protein-2 antagonist of cell death (substrates of RSK), and BDNF. Inhibiting the ERK pathway with the blood-brain barrier-penetrating mitogen-activated protein kinase (MAP kinase)/ERK kinase (MEK) kinase inhibitor SL327, but not with the nonblood-brain barrier-penetrating MEK inhibitor U0126, decreased immobility time and increased swimming time of rats in the forced-swim test. SL327, but not U0126, also increased locomotion time and distance traveled in a large open field. The behavioral changes in the open field were prevented with chronic lithium pretreatment. SL327-induced behavioral changes are qualitatively similar to the changes induced by amphetamine, a compound that induces relapse in remitted manic patients and mood elevation in normal subjects. These data suggest that the ERK pathway may mediate the antimanic effects of mood stabilizers.  (+info)

Sustained extracellular signal-regulated kinase 1/2 phosphorylation in neonate 6-hydroxydopamine-lesioned rats after repeated D1-dopamine receptor agonist administration: implications for NMDA receptor involvement. (7/44)

Extracellular signal-regulated kinase (ERK) 1/2, a well known regulator of gene expression, is likely to contribute to signaling events underlying enduring neural adaptations. Phosphorylated (phospho)-ERK was examined immunohistochemically after both single and repeated (i.e., sensitizing) doses of the partial D1-dopamine (DA) receptor agonist SKF-38393 (2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benazepine HCl) to adult rats lesioned as neonates (neonate lesioned) with 6-hydroxydopamine. Remarkably, prolonged phospho-ERK accumulated primarily in layers II-III of medial prefrontal cortex (MPC), where it declined gradually yet remained significantly elevated for at least 36 d after repeated doses of SKF-38393. Sustained (> or =7 d) phospho-ERK was observed for shorter periods in various other cortical regions but was not detectable in striatum or nucleus accumbens. At 36 d, an additional injection of SKF-38393 to sensitized rats restored phospho-ERK to maximal levels only in MPC when examined 7 d later. Phosphorylated cAMP response element-binding protein (CREB), examined 7 d after the sensitizing regimen, was observed exclusively in MPC, where it was abundant throughout all layers. Systemic injections of SL327 (alpha-[amino[(4-aminophenyl)thio]methylene]-2-(trifluoromethyl)benzeneacetonitri le), an inhibitor of the upstream ERK activator mitogen ERK kinase, attenuated both ERK and CREB phosphorylation in layers II-III of MPC. Pretreatment with the D1 antagonist SCH-23390 ((R)-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-OL maleate) inhibited the prolonged increase in MPC phospho-ERK, whereas the 5-HT2 receptor antagonist ketanserin (3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2,4(1H,3H)-quinazolinedione tartrate) was ineffective. Competitive and noncompetitive NMDA receptor antagonists also blocked sustained ERK phosphorylation. Collectively, the present results demonstrate coupling of D1 and NMDA receptor function reflected in sustained activation of the ERK signaling pathway in MPC of SKF-38393-sensitized neonate-lesioned rats. Ultimately, long-lasting phosphorylation of ERK and CREB in MPC may play a pivotal role in any permanent adaptive change(s) in these animals.  (+info)

ERK kinase inhibition stabilizes the aryl hydrocarbon receptor: implications for transcriptional activation and protein degradation. (8/44)

The ultimate carcinogen and metabolite of benzo-[a]pyrene-7,8-dihydrodiol, benzo[a]pyrene-r-7,t-8-dihydrodiol-t-9,10-epoxide (+/-), stimulates apoptosis, and this process can be blocked by extracellular signal-regulated kinase (Erk) kinase inhibitors. However, we show here that Erk kinase inhibitors were unable to prevent B[a]P-7,8-dihydrodiol-induced apoptosis, leading us to speculate that Erk kinases are linked to regulation of the aryl hydrocarbon (Ah) receptor. Cotreatment of hepa1c1c7 cells with 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and Erk kinase inhibitor PD98059, U0126, or SL327 led to enhanced nuclear accumulation of Ah receptor but with a reduced capacity to complement TCDD induction of Cyp1a1. This is explained in part by the ability of Erk kinase inhibitors to alter the steady-state levels of cellular Ah receptor, a result that leads to a dramatic induction in detectable receptor levels. These changes in cellular Ah receptor levels are associated with delayed degradation of the Ah receptor because TCDD-initiated degradation is reversed when cells are co-treated with TCDD and Erk kinase inhibitors. Erk kinase is linked to Ah receptor expression, as demonstrated by reductions in total Ah receptor levels after overexpression of constitutively active MEK1. In addition, Erk kinase activity modulates the transcriptional response because MEK1 overexpression enhances TCDD-initiated transactivation potential of the receptor. Thus, Erk kinase activity facilitates ligand-initiated transcriptional activation while targeting the Ah receptor for degradation. Immunoprecipitation experiments of the Ah receptor indicate that Erk kinase activity is associated with the receptor. It is interesting that the carboxyl region of the Ah receptor is associated with the transactivation region as well as the site for ubiquitination, indicating that Erk kinase-dependent phosphorylation targets the carboxyl region of the receptor.  (+info)

... SOUTH SAN FRANCISCO Calif. May 6 /- CatalystBiosci...CB 813 is designed to substantially enhance clot-generating activity a... Patients receiving factor VIIa therapy typically require multipledos... The selection of this development candidate is an exciting milestone...,Catalyst,Biosciences,Selects,Drug,Development,Candidate,in,Factor,VIIa,Program,for,Hemophilia,medicine,advanced medical technology,medical laboratory technology,medical device technology,latest medical technology,Health
SOUTH SAN FRANCISCO, Calif., Aug. 23, 2021 (GLOBE NEWSWIRE) -- NGM Biopharmaceuticals, Inc. (NGM) (Nasdaq: NGM), a biotechnology company focused on discovering and developing transformative therapeutics for patients, today disclosed its fourth oncology development candidate, NGM831, an antagonist antibody designed to block the interaction of ILT3 with fibronectin, as well as with other ligands. The announcement coincides with a publication in Cancer Immunology Research, a journal of the American Association for Cancer Research,1 describing NGMs discovery of ILT3s functional ligand, fibronectin, an extracellular matrix protein that forms a fibrillar network within the tumor stroma. This discovery enabled the development of NGM831, which joins NGMs growing portfolio of wholly owned oncology antibody programs, including NGM120 (anti-GFRAL), NGM707 (anti-ILT2/ILT4) and NGM438 (anti-LAIR1).. NGM is a leader in research elucidating the central role that myeloid cells play in creating a suppressive ...
Vir Biotechnology, Inc. (Nasdaq: VIR) and Alnylam Pharmaceuticals, Inc. (Nasdaq: ALNY) today announced the selection of a development candidate (DC) f
When contemplating how best to cripple this pathway, several key proteins are reasonable candidates for consideration. Most efforts to design small-molecule inhibitors of RAS-MAPK signaling have focused on the major protein players (i.e., RAS, RAF, MEK, and ERK). We may see more attention devoted in the future, however, to several scaffolding proteins and endogenous inhibitors that also come into play with respect to pathway dynamics (5). Recent advances in the development of genome-wide RNA interference libraries have enabled screening that may potentially identify other novel regulators of MAP signaling amenable to pharmacologic intervention (6, 7).. Is RAS druggable? Attempts to target RAS by perturbing its interaction with either SOS or GRB2 have not yielded viable drug development candidates largely because of the inherent difficulties of disrupting protein-protein interactions with drug-like molecules. Several drug discovery programs have also been devoted to finding inhibitors of ...
VX 954 was selected in October 2000 as a drug development candidate from Vertex Pharmaceuticals p38 mitogen-activated protein (MAP) kinase research programme.
In molecular biology and pharmacology, a small molecule is a low molecular weight (,900 Daltons[1]) organic compound that may help regulate a biological process, with a size on the order of 10−9 m. Most drugs are small molecules.. The upper molecular weight limit for a small molecule is approximately 900 Daltons, which allows for the possibility to rapidly diffuse across cell membranes so that they can reach intracellular sites of action.[1][2] In addition, this molecular weight cutoff is a necessary but insufficient condition for oral bioavailability. Finally, a lower molecular weight cutoff of 500 Daltons (as part of the «rule of five») has been recommended for small molecule drug development candidates based on the observation that clinical attrition rates are significantly reduced if the molecular weight is kept below this 500 Dalton limit.[3][4]. Pharmacology usually restricts the term to a molecule that binds to a specific biopolymer-such as protein or nucleic acid-and acts as an ...
NewLink Genetics Corporation (NASDAQ NLNK) today announced that indoximod, its leading drug development candidate, was granted orphan-drug designation by the U.
... - RDEA594 Data to Be Presented at the 2008 Annual European Congress... 2008 - ...SAN DIEGO May 19 /- Ardea Biosciences Inc.(N...Based on extensive in vitro and in vivo experiments the Companybelie...,Ardea,Biosciences,Identifies,Lead,Development,Candidate,for,Gout,,RDEA594,medicine,advanced medical technology,medical laboratory technology,medical device technology,latest medical technology,Health
-IND filing expected by end of 2007- EDMONTON, April 16, 2007 PRNewswire-FirstCall - Biomira Inc. today announced that it has selected PX-866 as its next clinic
Array Receives $1,000,000 Milestone Payment from AstraZeneca -. BOULDER, Colo., Jan. 24 /PRNewswire-FirstCall/ -- Array BioPharma Inc. (Nasdaq: ARRY) and AstraZeneca PLC selected an additional clinical candidate for their small molecule anti-cancer program, triggering a $1 million milestone payment from AstraZeneca to Array. In December 2003, Array partnered the oncology portion of its MEK program, including its lead compound, ARRY-142886 (AZD6244), for co-development and commercialization with AstraZeneca. At that time, Array and AstraZeneca established a collaboration for research and development of additional clinical candidates.. We are pleased that our collaboration with AstraZeneca has yielded an additional high quality development candidate, said Kevin Koch, Ph.D., President and Chief Scientific Officer, Array BioPharma. Our first proprietary compound, ARRY-142886, continues to make good progress in Phase Ib. We believe the data generated in this study will support more advanced ...
BA DPhil CChem FRSC. I took early retirement from GSK in 2019 and set up Blue Burgundy Ltd. My 30+ years of drug discovery experience provide expertise in identifying issues and opportunities in discovery programmes, which enable my imaginative and innovative thinking to address the unique needs of every programme.. I joined Wellcome in 1990, following BA/DPhil at the University of Oxford and Post Doc at Ben May Institute, University of Chicago. Subsequent career navigated changes, mergers, and acquisitions, charting significant contributions to six development candidates in antivirals (HIV/HBV/Herpes), iNOS and Factor Xa. Moved to early stage discovery in 2006, contributing to and leading numerous successful H2L programs (HTS/Fragments/ELT). Amongst many fruitful partnerships in international collaborations (France, Italy, Japan, Korea, USA), productive links with GSK Diseases of the Developing World group in Spain were a highlight (influential leadership in several programmes and served on SAB ...
Basel (Switzerland) and Mannheim (Germany), January 18, 2018 - VAXIMM AG, a Swiss/German biotech company focused on developing oral T-cell immunotherapies, today announced that the Company will participate in several upcoming events in the first quarter of 2018.. ASCO-SITC Clinical Immuno-Oncology Symposium January 25-27, 2018 San Francisco, CA, USA. The ASCO-SITC Clinical Immuno-Oncology Symposium is focused on clinical and translational research in immuno-oncology and the implications for clinical care. VAXIMM will present preclinical data with its oral T‑cell immunotherapy development candidate VXM10. The poster, Live attenuated oral Salmonella platform for effective T- and B-cell targeting of PD‑L1, summarizes the immunogenicity and anti-leukemia activity of VXM10 in an animal model, transformed with a eukaryotic expression plasmid encoding different variants of the murine PD‑L1 protein.. The poster will be presented during Poster Session A on Thursday, January 25th at 11:30 AM - ...
At Vernalis, we develop and apply fragment and structure-based methods to solve problems in drug discovery and generate development candidates against targets in oncology, neurodegeneration, anti-infectives and inflammation. We have a full-time lab-based opportunity for a Scientist to join our Oncology & Cell Biology team, located at our Cambridge Research site.
Worldwide the incidence for NAFLD is rising dramatically and is highly correlated to the Metabolic Syndrome. Activation of the FXR recep¬tor through a drug combats the underlying causes of NAFLD by lowering liver lipids and improving hepatic insulin sensitivity, combined with a liver specific anti-fibrotic and anti-inflammatory effect. A first human clinical trial with Phenex´ proprietary FXR development candidate PX-102 is scheduled for spring 2011. Phenex intends to outlicense this program after first human proof of concept data ...
We develop and apply fragment and structure-based methods to solve problems in drug discovery, and have generated cell active lead compounds and development candidates against targets in oncology, neurodegeneration, anti-infectives and inflammation.. ...
Continued Productivity in Research. Vertex continues to focus its research efforts in the areas of infectious diseases, including viral infections - such as influenza - and bacterial infections, inflammatory diseases, cancer and neurological disorders, including pain. Vertex expects additional development candidates for the treatment of one or more of these diseases to emerge from research in 2012. The company will report full-year 2011 financial results and financial guidance on February 2, 2012 . Webcast. Vertex Pharmaceuticals will webcast its corporate presentation at the 30th Annual J.P. Morgan Healthcare Conference on January 9, 2012 at 11:00 a.m. PT ( 2:00 p.m. ET ). A link to the live webcast will be available via Vertexs website, www.vrtx.com, in the Events & Presentations section. An archived webcast of the presentation will be available on Vertexs website through January 23, 2012 . About Vertex. Vertex creates new possibilities in medicine. Our team discovers, develops and ...
is advancing messenger RNA (mRNA) science to create a new class of transformative medicines for patients. mRNA medicines are designed to direct the bodys cells to produce intracellular, membrane or secreted proteins that can have a therapeutic or preventive benefit and have the potential to address a broad spectrum of diseases. Modernas platform builds on continuous advances in basic and applied mRNA science, delivery technology and manufacturing, providing the Company the capability to pursue in parallel a robust pipeline of new development candidates ...
1HV7: The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate
Max and Dev have developed a powerful platform for fine-tuning the tumor microenvironment to enhance the immune systems response against cancer, said Steven James, Pionyrs executive chairman and interim CEO. We are building on these capabilities to develop antibody-based therapeutics with novel antigen targets and mechanisms of action. We expect to choose development candidates and drive them to IND in the near future.. Pionyr Immunotherapeutics is led by industry veterans with deep management and immuno-oncology expertise. Mr. James, former CEO of Labrys Biologics (acquired by TEVA) and KAI Pharmaceuticals (acquired by Amgen), is joined on the leadership team by Michel Streuli, Ph.D., senior vice president of research, who previously led immuno-oncology efforts at Gilead, Merck (as early development chair for Keytruda), Schering-Plough and Organon. On the board of directors, in addition to Mr. James and Dr. Krummel, are Michael Ross, Ph.D., and Joshua Resnick, M.D., both partners at SV ...
Infinity Pharmaceuticals, Inc. (NASDAQ: INFI) today announced initial clinical and new preclinical data for IPI-549, an orally administered immuno-oncology development candidate
WASHINGTON, April 1, 2017 /PRNewswire/ -- Infinity Pharmaceuticals, Inc. (NASDAQ: INFI) today reported updated Phase 1 clinical data for IPI-549, an orally administered immuno-oncology development candidate ...
The drug, monepantel - sold under the trade name Zolvix - was reclassified from POM-V to POM-VPS in 2017, despite the BVAs concern it was
Imidazo[4,5-c]quinoline derivatives have been discovered and developed as potent and effective modulators of the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) pathway to lead to clinical development candidates. The SAR data of representative examples of this compound class and their bi …
Macrophage Pharma is developing a highly novel class of small molecule therapeutics which modulate immune responses to combat cancer based on its proprietary Esterase Motif Technology™ (ESM™) platform. ESM molecules deliver small molecule inhibitors of key intracellular targets in a highly selective manner to macrophages, monocytes and monocyte-derived dendritic cells. Macrophage Pharma is rapidly progressing its lead molecules to the clinic utilising ESM to deliver inhibitors to tumour associated macrophages and tolerogenic dendritic cells in the tumour microenvironment.. The Company was founded by the CRT Pioneer Fund and recently announced a £9 million financing round. The round was led by CPF who were joined by two specialist investors, Novo A/S and Aglaia Biomedical Ventures BV. The proceeds of the financing round will enable the Company to complete the pre-clinical development of its lead development candidate, a p38 MAP kinase inhibitor, and advance two additional discovery ...
About Crinetics Pharmaceuticals Crinetics Pharmaceuticals is a clinical stage pharmaceutical company focused on the discovery, development, and commercialization of novel therapeutics for rare endocrine diseases and endocrine-related tumors. The companys lead product candidate, CRN00808, is an oral selective nonpeptide somatostatin receptor type 2 biased agonist undergoing two Phase 2 clinical trials for the treatment of acromegaly, an orphan disease affecting more than 25,000 people in the United States. Crinetics second oral product development candidate, CRN01941, has entered the clinic for the treatment of neuroendocrine tumors. The company is also developing oral nonpeptide somatostatin agonists for hyperinsulinism, as well as oral nonpeptide ACTH antagonists for the treatment of Cushings disease. All of the companys drug candidates are new chemical entities resulting from in-house drug discovery efforts. For more information, please visit www.crinetics.com. Forward-Looking Statements ...
Brown Rudnicks client Eliem Therapeutics Inc. recently closed on a $60-million Series B financing. Brown Rudnick has advised and continues to advise the company on intellectual property and advised on the IP aspects of the transaction.. Eliem is a clinical-stage biotechnology company focused on developing novel therapies for neuronal excitability disorders to address unmet needs in disorders of the peripheral and central nervous systems. The financing round was led by Intermediate Capital Group and RA Capital Management and included participation from Access Biotechnology, Samlyn Capital, Acorn Bioventures, and LifeArc. Eliem plans to use the proceeds to advance its two lead clinical-stage product candidates, ETX-810 and ETX-155, through topline data across four different indications in patients with chronic pain, depressive disorders, and epilepsy, as well as to advance its two preclinical-stage programs to selection of clinical development candidates.. The Brown Rudnick deal team included ...
Pegoraro S, Duffey M, Otto TD, Wang Y, Rosemann R, Baumgartner R, Fehler SK, Lucantoni L, Avery VM, Moreno-Sabater A, Mazier D, Vial HJ, Strobl S, Sanchez CP, Lanzer M (2017). SC83288 is a clinical development candidate for the treatment of severe malaria. Nat Commun. 8:14193. Cyrklaff M, Srismith S, Nyboer B, Burda K, Hoffmann A, Lasitschka F, Adjalley S, Bisseye C, Simpore J, Mueller AK, Sanchez CP, Frischknecht F, Lanzer M (2016). Oxidative insult can induce malaria-protective trait of sickle and fetal erythrocytes. Nat Commun. 7:13401. Rieger H, Yoshikawa HY, Quadt K, Nielsen MA, Sanchez CP, Salanti A, Tanaka M, Lanzer M (2015). Cytoadhesion of Plasmodium falciparum-infected erythrocytes to chondroitin-4-sulfate is cooperative and shear enhanced. Blood 125:383-391. Sanchez CP, Liu CH, Mayer S, Nurhasanah A, Cyrklaff M, Mu J, Ferdig MT, Stein WD, Lanzer M (2014). A HECT ubiquitin-protein ligase as a novel candidate gene for altered quinine and quinidine responses in Plasmodium falciparum. ...
NovaDigm is developing innovative immunotherapeutics and preventative vaccines to protect patients from fungal and bacterial disease, which can be recurrent, drug-resistant and in some cases, life-threatening. NovaDigms lead development candidate, NDV-3A, is the first vaccine to demonstrate preclinical efficacy in reducing the severity of disease caused by both fungal and bacterial pathogens. NDV-3A is in Phase 2 clinical development for recurrent vulvovaginal candidiasis (RVVC) with follow-on indications planned for Candida, including nosocomial candidiasis, a severe life threatening infection and Staphylococcus aureus, including MRSA. ...
Michael Waring is a Principal Scientist in the Oncology medicinal chemistry group at AstraZeneca. He earned his PhD from the University of Manchester under the supervision of Prof. Timothy Donohoe (1999) followed by postdoctoral research with Prof. Philip Magnus at the University of Texas at Austin. Mike joined AstraZeneca in 2001 and has worked on projects at all stages of drug discovery across both oncology and cardiovascular disease areas, culminating in the discovery of 14 development candidates, including AZD9291. From summer 2015 will be Professor of Medicinal Chemistry at Newcastle University ...
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The EM Radiation Research Trust is an independent body. The aim of the organisation is to provide the facts about electro-magnetic radiation and our health to the public and the media.. Follow us on:. ...
This study examined the development of resistance to anthelmintics in Haemonchus contortus in lambs under suppressive or selective treatment regimens that included monepantel. Twenty Ile de France and 20 Santa Ines lambs were allocated to two anthelmintic treatment regimens, based on body weight and nematode faecal egg counts (FEC): targeted selective treatment (TST) or suppressive treatment, both with monepantel. Lambs of the TST group were treated individually when they presented with a packed cell volume (PCV) ≤20%. On 7 October 2016, the lambs were allocated to clean pastures, where they grazed in separated paddocks by group until late February 2017. The experimental area was contaminated with nematodes that were introduced with the experimental Ile de France and Santa Ines lambs, naturally infected with gastrointestinal nematodes. To maintain the grazing lambs in the suppressive treatment group and their pasture as free of worms as possible, these lambs were treated with anthelmintics before
SYRACUSE, N.Y.-- Upstate Medical University has signed an agreement with the Connecticut-based development stage company NanoViricides to test drug candidates against varicella zoster virus (VZV), also know as the shingles virus.. Shingles is a painful skin rash that can have debilitating effects on sufferers, especially older adults.. The research will be performed in the laboratory of Jennifer Moffat, PhD, associate professor of microbiology and immunology, and will include in vitro, ex vivo and possibly in vivo studies.. We are pleased to study the new antiviral compounds from NanoViricides in our VZV models, Moffat said. Using nanoparticles to target viruses is an innovative approach and were eager to collaborate on this project.. Moffat has extensive experience in varicella zoster virus infection and antiviral agent discovery. The goal of these studies is to help select a clinical drug development candidate for toxicology and safety evaluation intended for clinical trials for the ...
Aldrich-252654; N-(Diphenylmethylene)aminoacetonitrile 0.98; CAS Number: 70591-20-7; Linear Formula: (C6H5)2C=NCH2CN; find related products, papers, technical documents, MSDS & more at Sigma-Aldrich.
approved drugs in the high need areas of pain, ADHD and other central nervous system disorders. KemPharms co-lead clinical development candidates are KP415 and KP484, both based on a prodrug of methylphenidate, but with differing extended-release profiles for the treatment of ADHD, and KP201/IR, an acetaminophen-free formulation of the companys immediate release abuse deterrent hydrocodone product candidate, KP201. For more information on ...
This is the first monoclonal antibody encoded by mRNA to be dosed in a human and the first development candidate from the Companys systemic therapeutics modalities to start clinical testing.. We believe this trial will give us important information about how mRNA may be used to make systemically-available complex therapeutic proteins in a consistent, dose-dependent fashion, said Tal Zaks, M.D., Ph.D., chief medical officer at Moderna. Dosing the first monoclonal antibody encoded by mRNA in humans is a significant milestone for our team and mRNA platform. We look forward to learning about the functionality of our mRNA-encoded antibody in neutralizing the Chikungunya virus.. mRNA-1944 encodes a fully human IgG antibody originally isolated from B cells of a patient with a prior history of potent immunity against Chikungunya infection. It is composed of two mRNAs that encode the heavy and light chains of this anti-Chikungunya antibody within Modernas proprietary lipid nanoparticle (LNP) ...
Our overall theme and objective of this Center is to develop new classes of host-targeting antiviral therapeutics that are capable of treating multiple NIAID Emerging and Re-emerging Priority Pathogen viruses, when used alone or in combination with other available agents. The range of planned activities spans the translational development spectrum: from generating new host target focused leads, to validating promising lead molecules, and advancing optimized leads. We hypothesize that a collection of exciting preliminary datasets now offer the potential to be collaboratively translated into the development of novel broad spectrum antivirals. More specifically, we will test the following hypotheses: 1) human haploid genetic screens can identify novel host genes required for multiple RNA viruses, and recombinant AAV viral vectors can both validate these targets and serve as development candidates against the identified genes;2) a suite of novel computational methods can identify compounds with ...
Homology Medicines, Inc., a genetic medicines company translating proprietary gene editing and gene therapy technologies into novel treatments for patients, announced today the closing of an $83.5 million Series B financing led by Deerfield Management. New investors include Fidelity Management and Research Company, HBM Healthcare Investments, Maverick Ventures, Novartis, Rock Springs Capital, Vida Ventures, Vivo Capital and Alexandria Venture Investments. Existing investors 5AM Ventures, ARCH Venture Partners and Temasek also participated in the financing. Homology has raised $127 million since the Company launched in 2016. The proceeds from the Series B are expected to be used to advance Homologys lead development candidate that is currently in preclinical IND-enabling studies for an inborn error of metabolism disease. The proceeds are also expected to support continued work to progress Homologys AMEnDR™ (AAV-Mediated Editing by Direct Homologous Recombination) technology into the clinic ...
PALATINE, IL -- (Marketwired) -- 08/15/14 -- Acura Pharmaceuticals Inc. (NASDAQ: ACUR), announced today preliminary discussions from a meeting held with the U.S. Food and Drug Administration (FDA) regarding the development pathway for Acuras AVERSION® hydrocodone with acetaminophen tablet development candidate, which is intended to provide abuse-deterrent features to address abuse by nasal snorting and injection. In a May 2014 letter to Acura, FDA questioned the relevance of abuse of hydrocodone with acetaminophen products by nasal snorting after reviewing clinical and epidemiology data submitted by Acura. The FDA continues to question the relevance of abuse of hydrocodone with acetaminophen products by the intranasal route of administration and suggested additional information may help better inform their decision. The FDA indicated in the discussions that Acura may conduct an additional nasal abuse liability study for its AVERSION hydrocodone with acetaminophen product candidate, the ...
This analysis of the global clinical antibacterial pipeline was done in support of the Global Action Plan on Antimicrobial Resistance. The study analysed to what extent antibacterial and antimycobacterial drugs for systemic human use as well as oral non-systemic antibacterial drugs for Clostridium difficile infections were active against pathogens included in the WHO priority pathogen list and their innovativeness measured by their absence of cross-resistance (new class, target, mode of action). As of July 1, 2018, 30 new chemical entity (NCE) antibacterial drugs, ten biologics, ten NCEs against Mycobacterium tuberculosis, and four NCEs against C difficile were identified. Of the 30 NCEs, 11 are expected to have some activity against at least one critical priority pathogen expressing carbapenem resistance. The clinical pipeline is dominated by derivatives of established classes and most development candidates display limited innovation. New antibacterial drugs without pre-existing cross-resistance are
B) Preparation of Glycine.-To a boiling suspension of 253 g. (0.8 mole) of barium hydroxide octahydrate in 500 cc. of water in a 1-l. beaker is added, in portions, 61.6 g. (0.4 mole) of aminoacetonitrile hydrogen sulfate at such a rate that the mixture does not froth over. The beaker is then covered with a 1-l. round-bottomed flask containing cold running water, and boiling is continued until no more ammonia is evolved. This requires six to eight hours. The barium is then quantitatively precipitated by the addition of exactly the necessary amount of 50 per cent sulfuric acid (Note 5). The filtrate is concentrated on a water bath to a volume of 50-75 cc.; on chilling, crude glycine crystallizes and is filtered off. The filtrate is again concentrated and chilled and the crystals removed. This process is continued until the final filtrate amounts to about 5 cc. The yield of crude glycine so obtained amounts to 25-27 g. This is systematically recrystallized from water, decolorizing with Norite and ...
Professor David L Morris is a Clinical Academic of the St George & Sutherland Clinical School, located on the grounds of St George Hospital. Research Interests: Surgical Oncologist, principally interested in treating metastatic cancer. Large databases of peritoneal and liver surgery Peritoneal and lung metastases. Basic cancer research lab, cell biology and drug development. Three drugs from our laboratory are under development: aminoacetonitrile pathway inhibitor, benzimidazole carbamate VEGF inhibitor and enzyme combination treatment for mucin-containing cancers. Also tumour ablation - bipolar RFA probe developer.. Broad Research Areas: Cancer Research. Qualifications:. MB, ChB, FRCS, FRCSE, MD, PhD, FRACS Specific Research Keywords:. Peritonectomy, cytoreductive surgery, hyperthermic intraperitoneal chemotherapy, RF Ablation, Albendazole, Bromelain, N-acetylcysteine, MUC, Monepantel. ILP/Honours research projects available for 2016:. Peritoneal cancers, effect of targeted anti-mucin ...
We found that MRCs were retained in all three mutant genotypes ( Figure 5A; Table 1), indicating that neither TRPV protein is required for the generation of MRCs. Additionally, loss of one or both of these ASH-expressed TRPV channels had no detectable effect on the size, latency, or time course of MRCs ( Table 1). Furthermore, though TRPV null. CHIR99021 mutations shifted the MRC current-voltage relationship toward 0 mV, MRCs reversed above +40 mV. Thus, the major component of MRCs in TRPV mutants remains a Na+-permeable channel, indicating that neither TRPV channel is a major contributor to MRCs in ASH ( Figures 5B and 5C). Next, we determined how the loss of ocr-2 and osm-9 affected the minor deg-1-independent MRC and found that MRCs in osm-9ocr-2;deg-1 triple mutants were the same size and had the same kinetics as deg-1 single mutants ( Figure 5A; Table 1). The triple mutant also had the same reversal potential as deg-1 mutants ( Figure 5B). Collectively, these data establish that neither the ...
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M Treinin] suppression of deg-3(u662) induced degenerations, Coilers, Levamisole resistance, Aldicarb resistance, pharyngeal pumping defect, temperature sensitive ...
Y-box binding protein-1 (YB-1) is the first reported oncogenic transcription factor to induce the tumor-initiating cell (TIC) surface marker CD44 in triple-negative breast cancer (TNBC) cells. In order for CD44 to be induced, YB-1 must be phosphorylated at S102 by p90 ribosomal S6 kinase (RSK). We therefore questioned whether RSK might be a tractable molecular target to eliminate TICs. In support of this idea, injection of MDA-MB-231 cells expressing Flag-YB-1 into mice increased tumor growth as well as enhanced CD44 expression. Despite enrichment for TICs, these cells were sensitive to RSK inhibition when treated ex vivo with BI-D1870. Targeting RSK2 with small interfering RNA (siRNA) or small molecule RSK kinase inhibitors (SL0101 and BI-D1870) blocked TNBC monolayer cell growth by similar to 100%. In a diverse panel of breast tumor cell line models RSK2 siRNA predominantly targeted models of TNBC. RSK2 inhibition decreased CD44 promoter activity, CD44 mRNA, protein expression, and mammosphere ...
Abstract Rationale The inability to stop a repetitive maladaptive behavior is a main problem in addictive disorders. Neuroadaptations that are associated with behavioral inflexibility may be involved in compulsive drug use. Objectives The aim of the present study was to investigate the pattern of behavioral inflexibility during morphine withdrawal
The treatment currently involves a relatively large number of capsules, so dogs that are difficult to orally medicate wouldnt be great candidates, said Dr Frimberger. But we are working on reformulating the drug to make it better tasting and easier to administer to dogs before the full trials commence next year.. The MPL program involves two consultations/treatments at the Animal Referral Hospital (ARH) in Homebush, NSW. Owners would have to transport their dogs to and from Homebush for the two treatments. PharmAust will cover all compassionate use program costs, including travel expenses to and from the ARH, as well as costs for the initial conventional chemotherapy treatment upon program completion.. For more information or to enrol, please contact Dr Angela Frimberger on [email protected] What is canine lymphoma? Cancer is the number one cause of death in dogs over the age of 2, with 25 per cent of deaths attributed to cancer¹. Approximately one in four dogs and one in ...
Morphine withdrawal can be both physically and emotionally significant, including flu-like physical symptoms and extreme mood swings and mental lows. Learn more about what to expect during withdrawal from morphine.
The present study was designed to investigate the role of protein kinase C (PKC) in this process by estimating changes in PKCalpha and PKCgamma immunoreactivity, and whether pharmacological inhibition of PKC would attenuate morphine withdrawal-induced c-Fos expression and changes in tyrosine hydroxylase (TH) immunoreactivity levels in the PVN and nucleus tractus solitarius/ ventrolateral medulla (NTS/VLM ...
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drugs: benzimidazoles, levamisole, macrocyclic lactones, amino acetonitrile derivatives and spiroindoles. Narrow spectrum drugs ...
Experimental investigation of nitrile formation from VUV photochemistry of interstellar ices analogs: acetonitrile and amino acetonitrile ...
Monepantel (aminoacetonitrile class) - effective against a variety of nematodes including those resistant to other anthelmintic ... This is especially true of nematodes, and has helped spur development of aminoacetonitrile derivatives for treatment against ...
2008), "Detection of amino acetonitrile in Sgr B2(N)", Astronomy & Astrophysics, 482 (1): 179-196, arXiv:0801.3219, Bibcode: ...
Many species of molecule, including aminoacetonitrile (a molecule related to glycine), ethyl formate, and butyronitrile, have ...
For instance, 2-methyl-5-aminothiazoles were prepared via condensation and cyclization of aminoacetonitrile and ... 5-amino-2-benzylthiazole and 5-amino-4-carbethoxy-2-benzylthiazole by reacting dithiophenylacetic acid with aminoacetonitrile ...
... the Max Planck Institute for Radio Astronomy discovered the spectral lines of a glycine-like molecule aminoacetonitrile in the ...
... can react with ammonia to give aminoacetonitrile, which can be hydrolysed to give glycine: HOCH2CN + NH3 → ...
... formally an aminoacetonitrile derivative of isoindolinone with two moles of HCN. When substituted 2-formylbenzoic acid, ...
... is the organic compound with the formula NCCH2NH2. The compound is a colorless liquid. It is unstable at room ... Using radio astronomy, aminoacetonitrile was discovered in the Large Molecule Heimat, a giant gas cloud near the galactic ... Aminoacetonitrile derivatives are useful antihelmintics. They act as nematode specific ACh agonists causing a spastic paralysis ... Tauber, Johannes; Opatz, Till (2015). "2-Aminoacetonitrile". E-EROS Encyclopedia of Reagents for Organic Synthesis: 1-4. doi: ...
... is the silicon analogue of methane. Because of the greater electronegativity of hydrogen in comparison to silicon, this Si-H bond polarity is the opposite of that in the C-H bonds of methane. One consequence of this reversed polarity is the greater tendency of silane to form complexes with transition metals. A second consequence is that silane is pyrophoric - it undergoes spontaneous combustion in air, without the need for external ignition.[11] However, the difficulties in explaining the available (often contradictory) combustion data are ascribed to the fact that silane itself is stable and that the natural formation of larger silanes during production, as well as the sensitivity of combustion to impurities such as moisture and to the catalytic effects of container surfaces causes its pyrophoricity.[12][13] Above 420 °C, silane decomposes into silicon and hydrogen; it can therefore be used in the chemical vapor deposition of silicon. The Si-H bond strength is around 384 kJ/mol, which ...
The RNA world hypothesis is supported by RNA's ability to store, transmit, and duplicate genetic information, as DNA does. RNA can act as a ribozyme, a special type of enzyme. Because it can perform the tasks of both DNA and enzymes, RNA is believed to have once been capable of supporting independent life forms.[15] Some viruses use RNA as their genetic material, rather than DNA.[45] Further, while nucleotides were not found in experiments based on Miller-Urey experiment, their formation in prebiotically plausible conditions was reported in 2009;[22] the purine base known as adenine is merely a pentamer of hydrogen cyanide. Experiments with basic ribozymes, like Bacteriophage Qβ RNA, have shown that simple self-replicating RNA structures can withstand even strong selective pressures (e.g., opposite-chirality chain terminators).[46] Since there were no known chemical pathways for the abiogenic synthesis of nucleotides from pyrimidine nucleobases cytosine and uracil under prebiotic conditions, it ...
HCN (not HNC) was first detected in June 1970 by L. E. Snyder and D. Buhl using the 36-foot radio telescope of the National Radio Astronomy Observatory.[16] The main molecular isotope, H12C14N, was observed via its J = 1→0 transition at 88.6 GHz in six different sources: W3 (OH), Orion A, Sgr A(NH3A), W49, W51, DR 21(OH). A secondary molecular isotope, H13C14N, was observed via its J = 1→0 transition at 86.3 GHz in only two of these sources: Orion A and Sgr A(NH3A). HCN was then later detected extragalactically in 1988 using the IRAM 30-m telescope at the Pico de Veleta in Spain.[17] It was observed via its J = 1→0 transition at 90.7 GHz toward IC 342. A number of detections have been made towards the end of confirming the temperature dependence of the abundance ratio of [HNC]/[HCN]. A strong fit between temperature and the abundance ratio would allow observers to spectroscopically detect the ratio and then extrapolate the temperature of the environment, thus gaining great insight into the ...
A chemical formula is a way of information about the chemical proportions of atoms that constitute a particular chemical compound or molecule, using chemical element symbols, numbers, and sometimes also other symbols, such as parentheses, dashes, brackets, commas and plus (+) and minus (−) signs. These are limited to a single typographic line of symbols, which may include subscripts and superscripts. A chemical formula is not a chemical name, and it contains no words. Although a chemical formula may imply certain simple chemical structures, it is not the same as a full chemical structural formula. Chemical formulas can fully specify the structure of only the simplest of molecules and chemical substances, and are generally more limited in power than are chemical names and structural formulas.. The simplest types of chemical formulas are called empirical formulas, which use letters and numbers indicating the numerical proportions of atoms of each type. Molecular formulas indicate the simple ...
... poisoning is the most common type of fatal air poisoning in many countries.[28] Carbon monoxide is colorless, odorless, and tasteless, but highly toxic. It combines with hemoglobin to produce carboxyhemoglobin, which usurps the space in hemoglobin that normally carries oxygen, but is ineffective for delivering oxygen to bodily tissues. Concentrations as low as 667 ppm may cause up to 50% of the body's hemoglobin to convert to carboxyhemoglobin.[29] A level of 50% carboxyhemoglobin may result in seizure, coma, and fatality. In the United States, the OSHA limits long-term workplace exposure levels above 50 ppm.[30]. The most common symptoms of carbon monoxide poisoning may resemble other types of poisonings and infections, including symptoms such as headache, nausea, vomiting, dizziness, fatigue, and a feeling of weakness. Affected families often believe they are victims of food poisoning. Infants may be irritable and feed poorly. Neurological signs include confusion, ...
Diatomic elements played an important role in the elucidation of the concepts of element, atom, and molecule in the 19th century, because some of the most common elements, such as hydrogen, oxygen, and nitrogen, occur as diatomic molecules. John Dalton's original atomic hypothesis assumed that all elements were monatomic and that the atoms in compounds would normally have the simplest atomic ratios with respect to one another. For example, Dalton assumed water's formula to be HO, giving the atomic weight of oxygen as eight times that of hydrogen[6], instead of the modern value of about 16. As a consequence, confusion existed regarding atomic weights and molecular formulas for about half a century. As early as 1805, Gay-Lussac and von Humboldt showed that water is formed of two volumes of hydrogen and one volume of oxygen, and by 1811 Amedeo Avogadro had arrived at the correct interpretation of water's composition, based on what is now called Avogadro's law and the assumption of diatomic ...
Theoretical predictions of buckyball molecules appeared in the late 1960s and early 1970s,[7][8] but these reports went largely unnoticed. In the early 1970s, the chemistry of unsaturated carbon configurations was studied by a group at the University of Sussex, led by Harry Kroto and David Walton. In the 1980s, Smalley and Curl at Rice University developed experimental technique to generate these substances. They used laser vaporization of a suitable target to produce clusters of atoms. Kroto realized that by using a graphite target,[9] a range of carbon clusters could be studied.. Concurrent but unconnected to the Kroto-Smalley work, astrophysicists conducting were working with spectroscopists to study infrared emissions from giant red carbon stars.[10][11][12] Smalley and team were able to use a laser vaporization technique to create carbon clusters which could potentially emit infrared at the same wavelength as had been emitted by the red carbon star.[10][13] Hence, the inspiration came to ...
2O (β) can be crystallized from solutions of the proper composition, as listed above. However, solutions of NaOH can be easily supercooled by many degrees, which allows the formation of hydrates (including the metastable ones) from solutions with different concentrations.[10][17] For example, when a solution of NaOH and water with 1:2 mole ratio (52.6% NaOH by mass) is cooled, the monohydrate normally starts to crystallize (at about 22 °C) before the dihydrate. However, the solution can easily be supercooled down to -15 °C, at which point it may quickly crystallize as the dihydrate. When heated, the solid dihydrate might melt directly into a solution at 13.35 °C; however, once the temperature exceeds 12.58 °C. it often decomposes into solid monohydrate and a liquid solution. Even the n = 3.5 hydrate is difficult to crystallize, because the solution supercools so much that other hydrates become more stable.[10] A hot water solution containing 73.1% (mass) of NaOH is an eutectic that ...
... is a potent inhibitor of cellular respiration, acting on mitochondrial cytochrome c oxidase, hence blocking oxidative phosphorylation. This prevents the body from oxidizing food to produce useful energy. Lactic acidosis then occurs as a consequence of anaerobic metabolism. Initially, acute cyanide poisoning causes a red or ruddy complexion in the victim because the tissues are not able to use the oxygen in the blood. The effects of potassium and sodium cyanide are identical, and symptoms of poisoning typically occur within a few minutes of ingesting the substance: the person loses consciousness, and brain death eventually follows. During this period the victim may suffer convulsions. Death is caused by cerebral hypoxia. The median lethal dose (human) for potassium cyanide is estimated at 200-300 mg.[13] A number of prominent persons were killed or committed suicide using potassium cyanide, including members of the Young Bosnia and famous personalities in the Third Reich, such ...
Minor uses of ethylene glycol include the manufacture of capacitors, as a chemical intermediate in the manufacture of 1,4-dioxane, as an additive to prevent corrosion in liquid cooling systems for personal computers, and inside the lens devices of cathode-ray tube type of rear projection televisions. Ethylene glycol is also used in the manufacture of some vaccines, but it is not itself present in these injections. It is used as a minor (1-2%) ingredient in shoe polish and also in some inks and dyes. Ethylene glycol has seen some use as a rot and fungal treatment for wood, both as a preventative and a treatment after the fact. It has been used in a few cases to treat partially rotted wooden objects to be displayed in museums. It is one of only a few treatments that are successful in dealing with rot in wooden boats, and is relatively cheap. Ethylene glycol may also be one of the minor ingredients in screen cleaning solutions, along with the main ingredient isopropyl alcohol. Ethylene glycol is ...
Serpone N, Salinaro A, Emeline AV, Horikoshi S, Hidaka H, Zhao JC. 2002. "An in vitro systematic spectroscopic examination of the photostabilities of a random set of commercial sunscreen lotions and their chemical UVB/UVA active agents". Photochemical & Photobiological Sciences 1(12): 970-981. ...
The large grains in interstellar space are probably complex, with refractory cores that condensed within stellar outflows topped by layers acquired subsequently during incursions into cold dense interstellar clouds. That cyclic process of growth and destruction outside of the clouds has been modeled[31][32] to demonstrate that the cores live much longer than the average lifetime of dust mass. Those cores mostly start with silicate particles condensing in the atmospheres of cool oxygen rich red-giant stars and carbon grains condensing in the atmospheres of cool carbon stars. The red-giant stars have evolved off the main sequence and have entered the giant phase of their evolution and are the major source of refractory dust grain cores in galaxies. Those refractory cores are also called Stardust (section above), which is a scientific term for the small fraction of cosmic dust that condensed thermally within stellar gases as they were ejected from the stars. Several percent of refractory grain ...
... is highly flammable and toxic at low doses. It undergoes explosive polymerization. The burning material releases fumes of hydrogen cyanide and oxides of nitrogen. It is classified as a Class 2B carcinogen (possibly carcinogenic) by the International Agency for Research on Cancer (IARC),[16] and workers exposed to high levels of airborne acrylonitrile are diagnosed more frequently with lung cancer than the rest of the population.[17] It evaporates quickly at room temperature (20 °C) to reach dangerous concentrations; skin irritation, respiratory irritation, and eye irritation are the immediate effects of this exposure.[7] Acrylonitrile increases cancer in high dose tests in male and female rats and mice.[18] Pathways of exposure for humans include emissions, auto exhaust, and cigarette smoke that can expose the human subject directly if they inhale or smoke. Routes of exposure include inhalation, oral, and to a certain extent dermal uptake (tested with volunteer humans and in rat ...
The structure of solid NaCN is related to that of sodium chloride.[5] The anions and cations are each six-coordinate. Potassium cyanide (KCN) adopts a similar structure. Each Na+ forms pi-bonds to two CN− groups as well as two "bent" Na---CN and two "bent" Na---NC links.[6] Because the salt is derived from a weak acid, sodium cyanide readily reverts to HCN by hydrolysis; the moist solid emits small amounts of hydrogen cyanide, which smells like bitter almonds (not everyone can smell it-the ability thereof is due to a genetic trait[7]). Sodium cyanide reacts rapidly with strong acids to release hydrogen cyanide. This dangerous process represents a significant risk associated with cyanide salts. It is detoxified most efficiently with hydrogen peroxide (H2O2) to produce sodium cyanate (NaOCN) and water:[4] ...
... s are a group of organic compounds sharing a common functional group with the general structure R1R2C=C=NR3. A ketenimine is a cumulated alkene and imine and is related to an allene and a ketene. The parent compound is ketenimine or CH2CNH. The most recent work by Bane et al. investigates the rovibrational structure of the ν8 and ν12 bands in the high-resolution FTIR spectrum, complementing the earlier analysis of the pure rotational spectrum. This pair of Coriolis coupled bands provide a rare example where intensity sharing between bands yields sufficient intensity for an otherwise invisible band (ν12).[1][2] ...
As a chemical feedstock, it is used for the manufacture of potassium hydroxide and potassium metal. It is also used in medicine, lethal injections, scientific applications, food processing, soaps, and as a sodium-free substitute for table salt for people concerned about the health effects of sodium. It is used as a supplement in animal feed to boost the number of nutrients in the feed, which in turn promotes healthy growth in animals. As an added benefit, it is known to increase milk production. It is sometimes used in water as a completion fluid in petroleum and natural gas operations, as well as being an alternative to sodium chloride in household water softener units. Glass manufacturers use granular potash as a flux, lowering the temperature at which a mixture melts. Because potash confers excellent clarity to glass, it is commonly used in eyeglasses, glassware, televisions, and computer monitors. KCl is useful as a beta radiation source for calibration of radiation monitoring equipment, ...
As part of its contribution to the Manhattan Project, Canada built and operated a 6-tonnes-per-year electrolytic heavy water plant at Trail, British Columbia, which started operation in 1943. The Atomic Energy of Canada Limited (AECL) design of power reactor requires large quantities of heavy water to act as a neutron moderator and coolant. AECL ordered two heavy water plants, which were built and operated in Atlantic Canada at Glace Bay, Nova Scotia (by Deuterium of Canada Limited) and Port Hawkesbury, Nova Scotia (by General Electric Canada). These plants proved to have significant design, construction and production problems. Consequently, AECL built the Bruce Heavy Water Plant (44°11′07″N 81°21′42″W / 44.1854°N 81.3618°W / 44.1854; -81.3618 (Bruce Heavy Water Plant)),[57] which it later sold to Ontario Hydro, to ensure a reliable supply of heavy water for future power plants. The two Nova Scotia plants were shut down in 1985 when their production proved unnecessary. ...
... is toxic in large amounts. It or its conjugate base bisulfite is produced biologically as an intermediate in both sulfate-reducing organisms and in sulfur-oxidizing bacteria, as well. The role of sulfur dioxide in mammalian biology is not yet well understood.[28] Sulfur dioxide blocks nerve signals from the pulmonary stretch receptors and abolishes the Hering-Breuer inflation reflex. It was shown that endogenous sulfur dioxide plays a role in diminishing an experimental lung damage caused by oleic acid. Endogenous sulfur dioxide lowered lipid peroxidation, free radical formation, oxidative stress and inflammation during an experimental lung damage. Conversely, a successful lung damage caused a significant lowering of endogenous sulfur dioxide production, and an increase in lipid peroxidation, free radical formation, oxidative stress and inflammation. Moreover, blockade of an enzyme that produces endogenous SO2 significantly increased the amount of lung tissue damage in the ...
A molecule is an electrically neutral group of two or more atoms held together by chemical bonds.[4][5][6][7][8] Molecules are distinguished from ions by their lack of electrical charge. However, in quantum physics, organic chemistry, and biochemistry, the term molecule is often used less strictly, also being applied to polyatomic ions. In the kinetic theory of gases, the term molecule is often used for any gaseous particle regardless of its composition. According to this definition, noble gas atoms are considered molecules as they are monatomic molecules.[9] A molecule may be homonuclear, that is, it consists of atoms of one chemical element, as with oxygen (O2); or it may be heteronuclear, a chemical compound composed of more than one element, as with water (H2O). Atoms and complexes connected by non-covalent interactions, such as hydrogen bonds or ionic bonds, are generally not considered single molecules.[10] Molecules as components of matter are common in organic substances (and therefore ...
The molecules in stars can be used to determine some characteristics of the star. The isotopic composition can be determined if the lines in the molecular spectrum are observed. The different masses of different isotopes cause vibration and rotation frequencies to significantly vary. Secondly the temperature can be determined, as the temperature will change the numbers of molecules in the different vibrational and rotational states. Some molecules are sensitive to the ratio of elements, and so indicate elemental composition of the star.[5] Different molecules are characteristic of different kinds of stars, and are used to classify them.[4] Because there can be numerous spectral lines of different strength, conditions at different depths in the star can be determined. These conditions include temperature and speed towards or away from the observer.[5] The spectrum of molecules has advantages over atomic spectral lines, as atomic lines are often very strong, and therefore only come from high in ...
Aminoacetonitrile is the organic compound with the formula NCCH2NH2. The compound is a colorless liquid. It is unstable at room ... Using radio astronomy, aminoacetonitrile was discovered in the Large Molecule Heimat, a giant gas cloud near the galactic ... Aminoacetonitrile derivatives are useful antihelmintics. They act as nematode specific ACh agonists causing a spastic paralysis ... Tauber, Johannes; Opatz, Till (2015). "2-Aminoacetonitrile". E-EROS Encyclopedia of Reagents for Organic Synthesis: 1-4. doi: ...
... aminoacetonitrile 0.98; CAS Number: 70591-20-7; Linear Formula: (C6H5)2C=NCH2CN; find related products, papers, technical ...
Amino-acetonitrile derivatives are a class of synthetic compounds with high activity against GI nematodes, including isolates ...
... Hydrochloride,Sulfate (1:1),Aminoacetonitrile Sulfate (1:1),Sulfate (2:1),Aminoacetonitrile Sulfate (2:1) ...
... you can Download free Aminoacetonitrile Nitrile Amine png photos as transparent and share with your friends. - ... Aminoacetonitrile Nitrile Amine png image file has been added to the Aminoacetonitrile category by Bernadette OKeefe at size ... Aminoacetonitrile Nitrile Amine png image file has been added to the Aminoacetonitrile category by Bernadette OKeefe at size ... of 251258, 915x1280 resolution, you can Download free Aminoacetonitrile Nitrile Amine png photos as transparent and share with ...
Aminoacetonitrile derivatives. Monepantel. 2008. Binds to some nicotinic receptor subunits. Paralysis. Unknown. ... And resistance to the aminoacetonitrile derivative monepantel has already appeared in worms, only seven to eight years after ...
The CSV is a delimited data format that has fields/columns separated by the semicolon character and records/rows separated by newlines. Fields that may contain a special character (semicolon, newline, or double quote), are enclosed in double quotes. For an easier handling, the list of Pre-registered substances is available in four parts ordered by EC number. They contain the same information as the following full list.. ...
Glycine hydrochloride can be prepared by the action of hydrochloric acid on hippuric acid,1 aminoacetonitrile,2 ... of water in a 1-l. beaker is added, in portions, 61.6 g. (0.4 mole) of aminoacetonitrile hydrogen sulfate at such a rate that ... 3. If the initial temperature of the acid mixture is below that indicated, there is a tendency for the aminoacetonitrile ... 4. The mother liquor contains a further quantity of aminoacetonitrile hydrogen sulfate which cannot, however, be recovered as ...
Aminoacetonitrile (C2H4N2). *1-Bromodocosane (C22H45Br) ...
Purine can be manufactured, for example, from aminoacetonitrile and formamide. Purines and purine derivatives are often ...
Find here Industrial Chemicals manufacturers, suppliers & exporters in Bhiwandi, Maharashtra. Get contact details & address of companies manufacturing and supplying Industrial Chemicals in Bhiwandi, Maharashtra.
Monepantel (aminoacetonitrile class) - effective against a variety of nematodes including those resistant to other anthelmintic ... This is especially true of nematodes, and has helped spur development of aminoacetonitrile derivatives for treatment against ...
Aminoacetonitrile hydrochloride?6011-14-9?,1,3-Dimethyladamantane?702-79-4?,1-Bromo-3,5-dimethyladamantane?941- ...
Bogey, M.; Dubus, H.; Guillemin, J.C., The millimeter-wave spectrum of aminoacetonitrile, J. Mol. Spectrosc., 1990, 143, 180-2 ...
drugs: benzimidazoles, levamisole, macrocyclic lactones, amino acetonitrile derivatives and spiroindoles. Narrow spectrum drugs ...
our publication on aminoacetonitrile (Belloche et al. 2008, A&A, 482, 179). suggests that the abundance of glycine, if present ... because the same team use the same data lasts year to reveal that the same galactic gas cloud also contains aminoacetonitrile. ...
3-Aryl-4-aminoimidazoles such as 3-phenyl-3H-imidazol-4-ylamine may be prepared by reacting phenylamine with aminoacetonitrile ... Chem., 1981, 46:856-9 and illustrated in scheme 3 below by reacting phenylamine with aminoacetonitrile. ...
Fiume L. Inhibition by aminoacetonitrile of early lesions induced in the liver of rats by carbon tetrachloride. J Pathol ... Fiume L, Favilli G. Inhibition of experimental cirrhosis by carbon tetrachloride following treatment with aminoacetonitrile. ...
N-(Diphenylmethylene)aminoacetonitrile. Purity: 98%. [70591-20-7], MFCD00009970. QA-2671. Diphenylmethylene-glycine benzyl ...
Formation of Negative Ions upon Dissociative Electron Attachment to the Astrochemically Relevant Molecule Aminoacetonitrile.. ...
2-phenyl-2-(1-phenylpropanyl-2-amino)acetonitrile. CAS Number. *17590-01-1 ...
But the aminoacetonitrile warhead of G0775 instead forms a covalent amidine with the lysine. ...
Amino-acetonitrile derivative (AAD). Resistance to this group is still unknown in Australia. So far, there is no claim for ...
Purine can be made for example of amino acetonitrile and formamide. Purines and purine derivatives are often isolated from ...
Purine can be made for example of amino acetonitrile and formamide. Purine und Purinderivate werden oft aus Naturstoffen ...
Ryosuke Takise, Kenichiro Itami, Junichiro Yamaguchi, Cyanation of Phenol Derivatives with Aminoacetonitriles by Nickel ...
The Therapeutic Effect of N-[N-(4-Carboxyphenyl) glycyl]-aminoacetonitrile on Chronic Hepatitis (Active Form)-A Double Blind ...
... an aminoacetonitrile derivative; AAD) [7]. Importantly, in the H. contortus gene set, we found a homolog acr-23 of the C. ...
AAD or amino-acetonitrile derivative group. *SPIRO or spiroindole group. *OP or organophosphate group ...
  • Aminoacetonitrile derivatives are useful antihelmintics. (wikipedia.org)
  • This is especially true of nematodes , and has helped spur development of aminoacetonitrile derivatives for treatment against drug-resistant nematodes, as well as exploration of doxycycline to kill their endosymbiotic Wolbachia bacteria. (wikipedia.org)
  • I guess we'll have to wait many years…" he told me, "A simple estimate we did in our publication on aminoacetonitrile (Belloche et al. (sciencebase.com)
  • Aminoacetonitrile compounds with pesticidal, especially insecticidal, activity for the protection of plants are described for example in EP 0 953 565 A2. (patentgenius.com)
  • Monepantel aminoacetonitrile class effective against a variety of nematodes including those resistant to other anthelmintic classes Spiroindoles e. undisclosed WormMail 201006091500 Monepantel 39 Zolvix 39 Novartis classed as an 39 amino acetonitrile derivative AAD 39 was registered a little over year ago in NZ. (dietistacatania.it)
  • Industrially aminoacetonitrile is produced from glycolonitrile by reaction with ammonia: HOCH2CN + NH3 → H2NCH2CN + H2O The aminoacetonitrile can be hydrolysed to give glycine: Being bifunctional, it is useful in the synthesis of diverse nitrogen-containing heterocycles. (wikipedia.org)
  • Aminoacetonitrile is the organic compound with the formula NCCH2NH2. (wikipedia.org)
  • Aminoacetonitrile Nitrile Amine png image file has been added to the Aminoacetonitrile category by Bernadette O'Keefe at size of 251258, 915x1280 resolution, you can Download free Aminoacetonitrile Nitrile Amine png photos as transparent and share with your friends. (picpng.com)
  • Create an account below to get 5 C&EN articles per month, receive newsletters and more - all free. (acs.org)
  • Three drugs from our laboratory are under development: aminoacetonitrile pathway inhibitor, benzimidazole carbamate VEGF inhibitor and enzyme combination treatment for mucin-containing cancers. (edu.au)
  • Theoretical Studies of Aminoacetonitrile Production in the Interstellar Medium [J]. Acta Phys. (pku.edu.cn)