HL156A
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HL156A
HL156A is a derivative of metformin and a potent oxidative phosphorylation, OXPHOS inhibitor and AMPK activating biguanide. Certain types of cancer cells requires OXPHOS to survive. By targeting it, HL156A might help in improving anticancer therapy. It is more potent than Acadesine, AICAR or metformin at activating AMPK. It is synthesized by Hanall Biopharma. Medical uses It is in Phases of clinical research, phase 1 trial in patients with advanced solid tumor and lymphoma. Pharmacology Apart from AMPK activation, it also inhibits expression and activation of insulin-like growth factor-1, IGF-1, AKT, mammalian target of rapamycin, mTOR, and Extracellular signal-regulated kinases, ERK. Research It is researched in multiple conditions like liver and renal fibrosis, cancer and drug resistance in cancer. A drug HL176OUT04 with similar pharmacology has been also developed. See also * Phenformin References

{{Reflist Pyrrolidines Guanidines Trifluoromethyl ethers Phe ...
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Metformin
Metformin, sold under the brand name Glucophage, among others, is the main first-line medication for the treatment of type 2 diabetes, particularly in people who are overweight. It is also used in the treatment of polycystic ovary syndrome. It is not associated with weight gain and is taken by mouth. It is sometimes used as an off-label adjunct to lessen the risk of metabolic syndrome in people who take antipsychotics. Metformin is generally well tolerated. Common adverse effects include diarrhea, nausea, and abdominal pain. It has a small risk of causing low blood sugar. High blood lactic acid level is a concern if the medication is used in overly large doses or prescribed in people with severe kidney problems. It is not recommended in those with significant liver disease. Metformin is a biguanide antihyperglycemic agent. It works by decreasing glucose production in the liver, increasing the insulin sensitivity of body tissues, and increasing GDF15 secretion, which redu ...
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Acadesine
Acadesine (INN), also known as 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, AICA-riboside, and AICAR, is an AMP-activated protein kinase activator which is used for the treatment of acute lymphoblastic leukemia and may have applications in treating other disorders such as diabetes. AICAR has been used clinically to treat and protect against cardiac ischemic injury. The drug was first used in the 1980s as a method to preserve blood flow to the heart during surgery. Acadesine is an adenosine regulating agent developed by PeriCor Therapeutics and licensed to Schering-Plough in 2007 for phase III studies. The drug is a potential first-in-class agent for prevention of reperfusion injury in CABG surgery. Schering began patient enrollment in phase III studies in May 2009. The trial was terminated in late 2010 based on an interim futility analysis. Chemistry Reaction of 2-bromo tribenzoyl ribose with diaminomaleonitrile results in the displacement of the anomeric halogen by one ...
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International Journal Of Oncology
The ''International Journal of Oncology'' is a monthly peer-reviewed medical journal of oncology, published by Spandidos Publications. It was established in 1992 and the editor-in-chief is Demetrios A. Spandidos (University of Crete). According to the ''Journal Citation Reports'', the journal has a 2020 impact factor The impact factor (IF) or journal impact factor (JIF) of an academic journal is a scientometric index calculated by Clarivate that reflects the yearly mean number of citations of articles published in the last two years in a given journal, as i ... of 5.650. References External links * Oncology journals Academic journals established in 1992 English-language journals Monthly journals Spandidos Publications academic journals {{oncology-journal-stub ...
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Guanidines
Guanidine is the compound with the formula HNC(NH2)2. It is a colourless solid that dissolves in polar solvents. It is a strong base that is used in the production of plastics and explosives. It is found in urine predominantly in patients experiencing renal failure. A guanidine moiety also appears in larger organic molecules, including on the side chain of arginine. Structure Guanidine can be thought of as a nitrogenous analogue of carbonic acid. That is, the C=O group in carbonic acid is replaced by a C=NH group, and each OH is replaced by a group. Isobutene can be seen as the carbon analogue in much the same way. A detailed crystallographic analysis of guanidine was elucidated 148 years after its first synthesis, despite the simplicity of the molecule. In 2013, the positions of the hydrogen atoms and their displacement parameters were accurately determined using single-crystal neutron diffraction. Production Guanidine can be obtained from natural sources, being first isolat ...
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Pyrrolidines
Pyrrolidine, also known as tetrahydropyrrole, is an organic compound with the molecular formula (CH2)4NH. It is a cyclic secondary amine, also classified as a saturated heterocycle. It is a colourless liquid that is miscible with water and most organic solvents. It has a characteristic odor that has been described as "ammoniacal, fishy, shellfish-like". In addition to pyrrolidine itself, many substituted pyrrolidines are known. Production and synthesis Industrial production Pyrrolidine is prepared industrially by the reaction of 1,4-butanediol and ammonia at a temperature of 165–200 °C and a pressure of 17–21 MPa in the presence of a cobalt- and nickel oxide catalyst, which is supported on alumina. : The reaction is carried out in the liquid phase in a continuous tube- or tube bundle reactor, which is operated in the cycle gas method. The catalyst is arranged as a fixed-bed and the conversion is carried out in the downflow mode. The product is obtained after mu ...
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Phenformin
Phenformin is an antidiabetic drug from the biguanide class. It was marketed as DBI by Ciba-Geigy, but was withdrawn from most markets in the late 1970s due to a high risk of lactic acidosis, which was fatal in 50% of cases. Phenformin was developed in 1957 by Ungar, Freedman and Seymour Shapiro, working for the US Vitamin Corporation. Clinical trials begun in 1958 showed it to be effective, but with gastrointestinal side effects. Toxicity Phenformin sales began to decline in the US from 1973 due to negative trial studies and reports of lactic acidosis. By October 1976, the FDA Endocrinology and Metabolism Advisory Committee recommended phenformin be removed from the market. The FDA began formal proceedings in May 1977, leading to its eventual withdrawal on November 15, 1978. In 1977, 385,000 patients with early-stage diabetes were taking phenformin in the US. Ralph Nader's Health Research Group put the US government under pressure to ban the drug. Ciba-Geigy Corp resisted, claim ...
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Pharmaceuticals (Basel, Switzerland)
This is a list of academic journals published by MDPI. As of September 2022, MDPI publishes 399 peer-reviewed academic journals and nine conference journals. {, class="wikitable sortable" , +List of MDPI journals !Journal name !Subject !Established !Impact factor !Scopus ranking (2021) !ISSN , - , ''Acoustics'' , Engineering , 2019 , Impact factors are calculated on the previous two years. Impact factors for journals established in 2019 will not be available until 2022. , – , 2624-599X , - , ''Actuators'' , Engineering , 2012 , 2.062nd percentile, 2076-0825 , - , ''Administrative Sciences'' , Business , 2011 , 69th percentile, 2076-3387 , - , ''Adolescents'' , Health , 2021 , Impact factors are calculated on the previous two years. Impact factors for journals established in 2021 will not be available until 2024. , – , 2673-7051 , - , ''Advances in Respiratory Medicine'' (formerly ''Pneumonologia i Alergologia Polska)'' , Health , , 27th percentile, 2451-4934 , - ...
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Oncotarget
''Oncotarget'' is a primarily oncology-focused, peer-reviewed, open access journal. The journal was established in 2010 and is published by Impact Journals. The editors-in-chief are Mikhail Blagosklonny and Andrei V. Gudkov. Abstracting and indexing The journal is abstracted and indexed in Index Medicus/MEDLINE/PubMed and Scopus. In 2022, it was re-indexed by Index Medicus/MEDLINE after being dropped in 2017. In 2018 Clarivate delisted the journal from the ''Journal Citation Reports'' and all of its other products because "the journal no longer meets the standards necessary for continued coverage", despite having listed the journal as a "Rising Star from Essential Science Indicators" only a few months prior. Reception The peer review process employed by the journal has been criticized by Jeffrey Beall, ---- a university librarian and expert on predatory open access publishing Predatory publishing, also write-only publishing or deceptive publishing, is an exploitative academic ...
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Cancer Science
''Cancer Science'' is a monthly peer-reviewed medical journal covering research in oncology, which is published by Wiley-Blackwell on behalf of the Japanese Cancer Association. Established in 1907, the journal publishes original articles, editorials, and letters to the editor, describing original research in the fields of basic, translational, and clinical cancer research. The editor-in-chief is Kohei Miyazono (University of Tokyo). According to the Journal Citation Reports, the journal has a 2020 impact factor of 6.71, ranking it 50 out of 242 journals in the category "Oncology". History The journal was established in 1907 as the ''Japanese Journal of Cancer Research'' by Katsusaburō Yamagiwa (University of Tokyo), who first produced tumors in animals by painting tar on their skin. In 1908, he joined the Japanese Foundation for Cancer Research as the first president, and the journal became the official journal of the foundation. The journal was transferred to the Japanese Canc ...
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Cancer
Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. These contrast with benign tumors, which do not spread. Possible signs and symptoms include a lump, abnormal bleeding, prolonged cough, unexplained weight loss, and a change in bowel movements. While these symptoms may indicate cancer, they can also have other causes. Over 100 types of cancers affect humans. Tobacco use is the cause of about 22% of cancer deaths. Another 10% are due to obesity, poor diet, lack of physical activity or excessive drinking of alcohol. Other factors include certain infections, exposure to ionizing radiation, and environmental pollutants. In the developing world, 15% of cancers are due to infections such as ''Helicobacter pylori'', hepatitis B, hepatitis C, human papillomavirus infection, Epstein–Barr virus and human immunodeficiency virus (HIV). These factors act, at least partly, by changing the genes of ...
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Fibrosis
Fibrosis, also known as fibrotic scarring, is a pathological wound healing in which connective tissue replaces normal parenchymal tissue to the extent that it goes unchecked, leading to considerable tissue remodelling and the formation of permanent scar tissue. Repeated injuries, chronic inflammation and repair are susceptible to fibrosis where an accidental excessive accumulation of extracellular matrix components, such as the collagen is produced by fibroblasts, leading to the formation of a permanent fibrotic scar. In response to injury, this is called scarring, and if fibrosis arises from a single cell line, this is called a fibroma. Physiologically, fibrosis acts to deposit connective tissue, which can interfere with or totally inhibit the normal architecture and function of the underlying organ or tissue. Fibrosis can be used to describe the pathological state of excess deposition of fibrous tissue, as well as the process of connective tissue deposition in healing. Define ...
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Oxidative Phosphorylation
Oxidative phosphorylation (UK , US ) or electron transport-linked phosphorylation or terminal oxidation is the metabolic pathway in which cells use enzymes to oxidize nutrients, thereby releasing chemical energy in order to produce adenosine triphosphate (ATP). In eukaryotes, this takes place inside mitochondria. Almost all aerobic organisms carry out oxidative phosphorylation. This pathway is so pervasive because it releases more energy than alternative fermentation processes such as anaerobic glycolysis. The energy stored in the chemical bonds of glucose is released by the cell in the citric acid cycle producing carbon dioxide, and the energetic electron donors NADH and FADH. Oxidative phosphorylation uses these molecules and O2 to produce ATP, which is used throughout the cell whenever energy is needed. During oxidative phosphorylation, electrons are transferred from the electron donors to a series of electron acceptors in a series of redox reactions ending in oxygen, who ...
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