Flashcards: Enzyme inhibitors

Orlistat is a drug designed to treat obesity.

Clavulanic acid (rINN) /ˌklævjuːˈlænᵻk ˈæsᵻd/ is a β-lactam drug that functions as a mechanism-based β-Lactamase inhibitor.

Aztreonam (trade names Azactam injection, Cayston inhalation) is a monobactam antibiotic used primarily to treat infections caused by gram-negative bacteria.

Piceatannol is a stilbenoid, a type of phenolic compound.

LY294002 is a morpholine-containing chemical compound that is a potent inhibitor of numerous proteins, and a strong inhibitor of phosphoinositide 3-kinases (PI3Ks).

Milnacipran (trade names Ixel, Savella, Dalcipran, Toledomin) is a serotonin–norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia.

Azelaic acid is an organic compound with the formula (CH2)7(CO2H)2.

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

Wortmannin, a steroid metabolite of the fungi Penicillium funiculosum, Talaromyces wortmannii, is a non-specific, covalent inhibitor of phosphoinositide 3-kinases (PI3Ks).

3-Amino-1,2,4-triazole (3-AT) is a heterocyclic organic compound that consists of a 1,2,4-triazole substituted with an amino group.

Abiraterone acetate (INN, USAN, BAN, JAN) (brand names Zytiga, Abiratas, Abretone, Abirapro) is a steroidal antiandrogen, specifically an androgen synthesis inhibitor, used in combination with prednisone in metastatic castration-resistant prostate cancer (previously called hormone-resistant or hormone-refractory prostate cancer) – i.

Orteronel (TAK-700) is a non-steroidal antiandrogen that was being developed for the treatment of cancer by Takeda Pharmaceutical Company in conjunction with Millennium Pharmaceuticals.

Medroxyprogesterone acetate (MPA), sold under the brand name Depo-Provera among others, is a steroidal progestin of the 17α-hydroxyprogesterone group and a synthetic derivative of the progestational steroid hormone progesterone.

Fumonisin B1 is the most prevalent member of a family of toxins, known as fumonisins, produced by several species of Fusarium molds, such as Fusarium verticillioides, which occur mainly in maize (corn), wheat and other cereals.

3-Benzoxepin is an annulated ring system with an aromatic benzene ring and a non-aromatic, unsaturated, oxygen-containing seven-membered heterocyclic oxepin.

Tipiracil is a drug used in the treatment of cancer.

Fumonisin B2 is a fumonisin mycotoxin produced by the fungi Fusarium verticillioides and Fusarium moniliforme.

Seviteronel (INN; developmental code VT-464) is an experimental cancer treatment for a type of prostate cancer.

Non-competitive inhibition is a type of enzyme inhibition where the inhibitor reduces the activity of the enzyme and binds equally well to the enzyme whether or not it has already bound the substrate.

VNI is an experimental drug for treating Chagas disease currently being studied at Vanderbilt University.

Bifluranol (INN, BAN) (brand name Prostarex) (former developmental code name BX-341) is an non-steroidal estrogen of the stilbestrol group related to diethylstilbestrol that is used as an antiandrogen in the United Kingdom in the treatment of prostate cancer.

Saralasin is a partial agonist of angiotensin II receptors, though it is commonly mistaken as a competitive antagonist.

Calcium carbimide, sold as the citrate salt under the trade name Temposil, is an alcohol sensitizing agent.

Levomilnacipran (brand name Fetzima) is an antidepressant approved in the United States for the treatment of major depressive disorder (MDD) in adults.

JNJ-42165279 is a drug developed by Janssen which acts as a potent and selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC50 of 70nM.

Galeterone (TOK-001 or VN/124-1) is a novel steroidal antiandrogen under development by Tokai Pharmaceuticals for the treatment of prostate cancer.

Uncompetitive inhibition, also known as anti-competitive inhibition, takes place when an enzyme inhibitor binds only to the complex formed between the enzyme and the substrate (the E-S complex).

Decynium-22 is a cation derivative of quinoline, and a potent inhibitor of the plasma membrane monoamine transporter (PMAT), as well as all members of the organic cation transporter (OCT) family in both human and rat cells.

PF-04457845 is a potent and exquisitely selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC50 of 7.

PF-4800567 is a drug developed by Pfizer which acts as a selective inhibitor of the enzyme Casein kinase 1 epsilon (CK1-ε), and has mainly been used in the study of the casein kinase 1 enzymes in the regulation of circadian rhythm, as well as showing potential neuroprotective effects.

AMG319 is a drug developed by Amgen which acts as an inhibitor of the phosphoinositide 3-kinase enzyme subtype PI3Kδ.

3-Nitrooxypropanol, abbreviated 3NOP, is an organic compound with the formula HOCH2CH2CH2ONO2.

Epostane (INN, USAN, BAN) (developmental code name WIN-32729) is an inhibitor of 3β-hydroxysteroid dehydrogenase (3β-HSD) that was developed as an contraceptive, abortifacient, and oxytocic drug but was never marketed.

AZD3293, also known as LY3314814 is an oral beta-secretase 1 cleaving enzyme (BACE) inhibitor.

4-Nonylphenylboronic acid is a potent and selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC50 of 9.

Etomoxir, or 2[6(4-chlorophenoxy)hexyl]oxirane-2-carboxylate, is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane.