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Suicide Inhibition
In biochemistry, suicide inhibition, also known as suicide inactivation or mechanism-based inhibition, is an irreversible form of enzyme inhibition that occurs when an enzyme binds a substrate analog and forms an irreversible complex with it through a covalent bond during the normal catalysis reaction. The inhibitor binds to the active site where it is modified by the enzyme to produce a reactive group that reacts irreversibly to form a stable inhibitor-enzyme complex. This usually uses a prosthetic group or a coenzyme, forming electrophilic alpha and beta unsaturated carbonyl compounds and imines. Examples Some clinical examples of suicide inhibitors include: * Disulfiram, which inhibits the acetaldehyde dehydrogenase enzyme. * Aspirin, which inhibits cyclooxygenase 1 and 2 enzymes. * Clavulanic acid, which inhibits β-lactamase: clavulanic acid covalently bonds to a serine residue in the active site of the β-lactamase, restructuring the clavulanic acid molecule, creating a muc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Soman Structural Formulae Stereoisomers V
Soman (or GD, EA 1210, Zoman, PFMP, A-255, systematic name: ''O''-pinacolyl methylphosphonofluoridate) is an extremely toxic chemical substance. It is a nerve agent, interfering with normal functioning of the mammalian nervous system by inhibiting the enzyme cholinesterase. It is an inhibitor of both acetylcholinesterase and butyrylcholinesterase. As a chemical weapon, it is classified as a weapon of mass destruction by the United Nations according to UN Resolution 687. Its production is strictly controlled, and stockpiling is outlawed by the Chemical Weapons Convention of 1993 where it is classified as a Schedule 1 substance. Soman was the third of the so-called ''G-series'' nerve agents to be discovered along with GA (tabun), GB (sarin), and GF (cyclosarin). When pure, soman is a volatile, corrosive, and colorless liquid with a faint odor like that of mothballs or rotten fruit. More commonly, it is a yellow to brown color and has a strong odor described as similar to cam ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sulbactam
Sulbactam is a β-lactamase inhibitor. This drug is given in combination with β-lactam antibiotics to inhibit β-lactamase, an enzyme produced by bacteria that destroys the antibiotic An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting pathogenic bacteria, bacterial infections, and antibiotic medications are widely used in the therapy ...s. It was patented in 1977 and approved for medical use in 1986. Medical uses The combination ampicillin/sulbactam (Unasyn) is available in the United States. The combination cefoperazone/sulbactam (Sulperazon) is available in many countries but not in the United States. The co-packaged combination sulbactam/durlobactam was approved for medical use in the United States in May 2023. Mechanism Sulbactam is primarily used as a suicide inhibitor of β-lactamase, shielding more potent beta-lactams such as ampicillin. Sulbactam itself contains a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluorouracil
Fluorouracil (5-FU, 5-fluorouracil), sold under the brand name Adrucil among others, is a cytotoxic chemotherapy medication used to treat cancer. By intravenous injection it is used for treatment of colorectal cancer, oesophageal cancer, stomach cancer, pancreatic cancer, breast cancer, and cervical cancer. As a cream it is used for actinic keratosis, basal cell carcinoma, and skin warts. Side effects of use by injection are common. They may include inflammation of the mouth, loss of appetite, low blood cell counts, hair loss, and inflammation of the skin. When used as a cream, irritation at the site of application usually occurs. Use of either form in pregnancy may harm the fetus. Fluorouracil is in the antimetabolite and pyrimidine analog families of medications. How it works is not entirely clear, but it is believed to involve blocking the action of thymidylate synthase and thus stopping the production of DNA. Fluorouracil was patented in 1956 and came into medical u ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lability
Lability refers to the degree that something is likely to undergo change. It is the opposite ( antonym) of stability. Biochemistry In reference to biochemistry, this is an important concept as far as kinetics is concerned in metalloproteins. This can allow for the rapid synthesis and degradation of substrates in biological systems. Biology Cells Labile cells refer to cells that constantly divide by entering and remaining in the cell cycle. These are contrasted with "stable cells" and "permanent cells". An important example of this is in the epithelium of the cornea, where cells divide at the basal level and move upwards, and the topmost cells die and fall off. Proteins In medicine, the term "labile" means susceptible to alteration or destruction. For example, a heat-labile protein is one that can be changed or destroyed at high temperatures. The opposite of labile in this context is "stable". Soils Compounds or materials that are easily transformed (often by ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acetylcholinesterase
Acetylcholinesterase (HUGO Gene Nomenclature Committee, HGNC symbol ACHE; EC 3.1.1.7; systematic name acetylcholine acetylhydrolase), also known as AChE, AChase or acetylhydrolase, is the primary cholinesterase in the body. It is an enzyme that catalysis, catalyzes the breakdown of acetylcholine and some other choline esters that function as neurotransmitters: : acetylcholine + H2O = choline + acetate It is found at mainly neuromuscular junctions and in chemical synapses of the cholinergic type, where its activity serves to terminate cholinergic neurotransmission, synaptic transmission. It belongs to the carboxylesterase family of enzymes. It is the primary target of inhibition by organophosphorus compounds such as nerve agents and pesticides. Enzyme structure and mechanism AChE is a hydrolase that hydrolyzes choline esters. It has a very high catalytic activity—each molecule of AChE degrades about 5,000 molecules of acetylcholine (ACh) per second, approaching the limit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Parathion
Parathion, also called parathion-ethyl or diethyl parathion, is an organophosphate insecticide and acaricide. It was originally developed by IG Farben in the 1940s. It is highly toxic to non-target organisms, including humans, so its use has been banned or restricted in most countries. In response to safety concerns, the less toxic but still dangerous analogue parathion methyl was later developed. History Parathion was developed by Gerhard Schrader for the German trust IG Farben in the 1940s. After World War II and the collapse of IG Farben due to the war crime trials, the Western allies seized the patent, and parathion was marketed worldwide by different companies and under different brand names. The most common German brand was E605 (banned in Germany after 2002); this was not a food-additive "E number" as used in the EU today. "E" stands for ''Entwicklungsnummer'' (German for "development number"). It is an irreversible acetylcholinesterase inhibitor. Safety concerns later l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nerve Agent
Nerve agents, sometimes also called nerve gases, are a class of organic chemistry, organic chemicals that disrupt the mechanisms by which nerves transfer messages to organs. The disruption is caused by the blocking of acetylcholinesterase (AChE), an enzyme that catalyzes the breakdown of acetylcholine, a neurotransmitter. Nerve agents are irreversible acetylcholinesterase inhibitors used as poison. Poisoning by a nerve agent leads to constriction of pupils, profuse salivation, convulsions, and involuntary urination and defecation, with the first symptoms appearing in seconds after exposure. Death by asphyxiation or cardiac arrest may follow in minutes due to the loss of the body's control over Respiration (physiology), respiratory and other muscles. Some nerve agents are readily vaporized or aerosolized, and the primary portal of entry into the body is the respiratory system. Nervous agents can also be absorbed through the skin, requiring that those likely to be subjected to su ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ornithine Decarboxylase
The enzyme ornithine decarboxylase (, ODC) catalyzes the decarboxylation of ornithine (a product of the urea cycle) to form putrescine. This reaction is the committed step in polyamine synthesis. In humans, this protein has 461 amino acids and forms a homodimer. In humans, ornithine decarboxylase (ODC) is expressed by the gene ''ODC1''. The protein ODC is sometimes referred to as "ODC1" in research pertaining to humans and mice, but certain species such as ''Drosophila'' (''dODC2''), species of Solanaceae plant family (''ODC2''), and the lactic acid bacteria '' Paucilactobacillus wasatchensis'' (''odc2'') have been shown to have a second ODC gene. Reaction mechanism Lysine 69 on ornithine decarboxylase (ODC) binds the cofactor pyridoxal phosphate to form a Schiff base. Ornithine displaces the lysine to form a Schiff base attached to orthonine, which decarboxylates to form a quinoid intermediate. This intermediate rearranges to form a Schiff base attached to putrescine ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
African Trypanosomiasis
African trypanosomiasis is an insect-borne parasitic infection of humans and other animals. Human African trypanosomiasis (HAT), also known as African sleeping sickness or simply sleeping sickness, is caused by the species ''Trypanosoma brucei''. Humans are infected by two types, ''Trypanosoma brucei gambiense'' (TbG) and ''Trypanosoma brucei rhodesiense'' (TbR). TbG causes over 92% of reported cases. Both are usually transmitted by the bite of an infected tsetse fly and are most common in rural areas. Initially, the first stage of the disease is characterized by fevers, headaches, itchiness, and joint pains, beginning one to three weeks after the bite. Weeks to months later, the second stage begins with confusion, poor coordination, numbness, and trouble sleeping. Diagnosis involves detecting the parasite in a blood smear or lymph node fluid. A lumbar puncture is often needed to tell the difference between first- and second-stage disease. Prevention of severe disease in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eflornithine
Eflornithine, sold under the brand name Vaniqa among others, is a medication used to treat African trypanosomiasis (sleeping sickness) and excessive hair growth on the face in women. Specifically it is used for the second stage of sleeping sickness caused by '' T. b. gambiense'' and may be used with nifurtimox. It is taken intravenously (injection into a vein) or topically. It is an ornithine decarboxylase inhibitor. Common side effects when applied as a cream include rash, redness, and burning. Side effects of the injectable form include bone marrow suppression, vomiting, and seizures. It is unclear if it is safe to use during pregnancy or breastfeeding. It is recommended typically for children over the age of 12. Eflornithine was developed in the 1970s and came into medical use in 1990. It is on the World Health Organization's List of Essential Medicines. In the United States the injectable form can be obtained from the US Centers for Disease Control and Prevention. I ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
HIV/AIDS
The HIV, human immunodeficiency virus (HIV) is a retrovirus that attacks the immune system. Without treatment, it can lead to a spectrum of conditions including acquired immunodeficiency syndrome (AIDS). It is a Preventive healthcare, preventable disease. It can be managed with treatment and become a manageable chronic health condition. While there is no cure or vaccine for HIV, Management of HIV/AIDS, antiretroviral treatment can slow the course of the disease, and if used before significant disease progression, can extend the life expectancy of someone living with HIV to a nearly standard level. An HIV-positive person on treatment can expect to live a normal life, and die with the virus, not of it. Effective #Treatment, treatment for HIV-positive people (people living with HIV) involves a life-long regimen of medicine to suppress the virus, making the viral load undetectable. Treatment is recommended as soon as the diagnosis is made. An HIV-positive person who has an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Reverse Transcriptase
A reverse transcriptase (RT) is an enzyme used to convert RNA genome to DNA, a process termed reverse transcription. Reverse transcriptases are used by viruses such as HIV and hepatitis B to replicate their genomes, by retrotransposon mobile genetic elements to proliferate within the host genome, and by eukaryotic cells to extend the telomeres at the ends of their linear chromosomes. The process does not violate the flows of genetic information as described by the classical central dogma, but rather expands it to include transfers of information from RNA to DNA. Retroviral RT has three sequential biochemical activities: RNA-dependent DNA polymerase activity, ribonuclease H (RNase H), and DNA-dependent DNA polymerase activity. Collectively, these activities enable the enzyme to convert single-stranded RNA into double-stranded cDNA. In retroviruses and retrotransposons, this cDNA can then integrate into the host genome, from which new RNA copies can be made via host-cell ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
