Enzyme inhibitors

Diphenhydramine, sold under the brand name Benadryl among others, is an antihistamine and sedative. Although generally considered sedating, diphenhydramine can cause paradoxical central nervous system stimulation in some individuals, particularly at higher doses. This may manifest as agitation, anxiety, or restlessness rather than sedation. It is a first-generation H1-antihistamine and it works by blocking certain effects of histamine, which produces its antihistamine and sedative effects. Diphenhydramine is also a potent anticholinergic. It is mainly used to treat allergies, insomnia, and sym

molecule that binds to an enzyme and decreases its activity

Quinidine is a class IA antiarrhythmic agent used to treat heart rhythm disturbances. It is a diastereomer of antimalarial agent quinine, originally derived from the bark of the cinchona tree. The drug causes increased action potential duration, as well as a prolonged QT interval. As of 2019, its IV formulation is no longer being manufactured for use in the United States.

α-Amanitin ('''alpha-Amanitin') is a cyclic peptide of eight amino acids. It is possibly the most deadly of all the amatoxins, toxins found in several species of the mushroom genus Amanita, one being the death cap (Amanita phalloides) as well as the destroying angel, a complex of similar species, principally A. virosa and A. bisporigera. It is also found in the mushrooms Galerina marginata, Lepiota subincarnata and Conocybe rugosa''. The oral of amanitin is 100 μg/kg for rats.

Milnacipran (trade names Ixel, Savella, Dalcipran, Toledomin) is a serotonin–norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia, major depressive disorder, and neuropathic pain. In the US, it is solely approved for the treatment of fibromyalgia, even though it is also approved for the treatment of major depressive disorder (but not fibromyalgia) in other countries (e.g. France).

thumb|3-Amino-1,2,4-triazole in powder form 3-Amino-1,2,4-triazole (3-AT) is a heterocyclic organic compound that consists of 1,2,4-triazole with an amino group as a substituent.

interruption of a chemical pathway when one substance inhibits the effect of another by competing with it for binding or bonding

Levomilnacipran, sold under the brand name Fetzima, is an antidepressant, used for the treatment of major depressive disorder in adults. It is the levorotatory enantiomer of milnacipran, and has similar effects and pharmacology, acting as a serotonin–norepinephrine reuptake inhibitor.

type of enzyme inhibition

chemical compound

'''N-Ethylmaleimide (NEM''') is an organic compound that is derived from maleic acid. It is a unstable substance that reacts rapidly with thiols and is commonly used to modify cysteine residues in proteins and peptides.

Dabrafenib, sold under the brand name Tafinlar among others, is an anti-cancer medication used for the treatment of cancers associated with a mutated version of the gene BRAF. Dabrafenib acts as an inhibitor of the associated enzyme B-Raf, which plays a role in the regulation of cell growth.

Halicin (SU-3327) is an experimental drug that acts as an enzyme inhibitor of c-Jun N-terminal kinase (JNK). Originally, it was researched for the treatment of diabetes, but development was discontinued for this application due to poor results in testing. In 2019, this molecule was found by an artificial intelligence (AI) model to show antibiotic properties against a number of bacteria.

type of enzyme inhibition

type of enzyme inhibition

3-Nitrooxypropanol (abbreviated as 3-NOP or 3NOP, commercially known as Bovaer) is a synthetic organic compound with the formula HOCH2CH2CH2ONO2. It is the mononitrate ester of 1,3-propanediol and acts as an enzyme inhibitor that specifically targets methyl coenzyme M reductase (MCR), the enzyme that catalyzes the final step of methanogenesis in microbes living in the digestive system of ruminants, such as cows and sheep.

Saralasin is a competitive angiotensin II receptor antagonist with partial agonistic activity. The aminopeptide sequence for saralasin differs from angiotensin II at three sites: At position 1, sarcosine replaces aspartic acid, thereby increasing the affinity for vascular smooth muscle AT II receptors and making sara resistant to degradation by aminopeptidases. At position 5, isoleucine is replaced by valine At position 8, phenylalanine is replaced by alanine which leads to a smaller stimulatory effect. Saralasin was used to distinguish renovascular hypertension from essential hypertension

Allylglycine is a glycine derivative. It is an inhibitor of glutamate decarboxylase. Inhibition of glutamate decarboxylase blocks GABA biosynthesis, leading to lower levels of the neurotransmitter. Allylglycine is known to induce seizures in animals studies, presumably due to this GDC-inhibiting activity.

Odanacatib (INN; codenamed MK-0822) is an investigational treatment for osteoporosis and bone metastasis. It is an inhibitor of cathepsin K, an enzyme involved in bone resorption.

Myxothiazol is a chemical compound produced by the myxobacterium Myxococcus fulvus. It is an inhibitor of the mitochondrial cytochrome bc1 complex (coenzyme Q - cytochrome c reductase).

type of enzyme inhibition by forming an irreversible complex with the substrate

protein-coding gene in the species Homo sapiens

AOH1996 is an experimental anticancer medication which acts as a small molecule inhibitor of proliferating cell nuclear antigen (PCNA) and is in Phase I clinical trials at City of Hope as of August 2023 for the treatment of solid tumors.

chemical compound

Tipiracil is a drug used in the treatment of cancer. It is approved for use in form of the combination drug trifluridine/tipiracil for the treatment of unresectable advanced or recurrent colorectal cancer.

class of compounds

Orteronel (TAK-700) is a nonsteroidal CYP17A1 inhibitor that was being developed for the treatment of cancer by Takeda Pharmaceutical Company in conjunction with Millennium Pharmaceuticals. It completed two phase III clinical trials for metastatic, hormone-refractory prostate cancer but failed to extend overall survival rates, and development was voluntarily terminated as a result.