• substrates
  • Standard reuptake inhibitors are believed to act simply as competitive substrates that work by binding directly to the plasmalemma transporter of the neurotransmitter in question. (wikipedia.org)
  • In contrast to substrates and irreversible inhibitors, reversible inhibitors generally do not undergo chemical reactions when bound to the enzyme and can be easily removed by dilution or dialysis. (wikipedia.org)
  • In contrast to the camptothecins, the indenoisoquinolines are: 1) chemically stable in blood, 2) inhibitors of Top1 cleavable complexes at distinct sites, 3) not substrates of membrane transporters, and 4) more effective as anti-tumor agents in animal models. (wikipedia.org)
  • Classical lock and key inhibitors such as phosphoramidon and bestatin bind tightly by approximating the transition state of the hydrolysis of the peptide, preventing it from acting on other substrates. (wikipedia.org)
  • Most studies used analogues of the nucleotide substrates or derivatives of natural product inhibitors such as xanthine (e.g. theophylline) and papaverine. (wikipedia.org)
  • vesicular
  • Pure vesicular reuptake inhibitors tend to actually lower synaptic neurotransmitter concentrations, as blocking the repackaging of, and storage of the neurotransmitter in question leaves them vulnerable to degradation via enzymes such as monoamine oxidase (MAO) that exist in the cytoplasm. (wikipedia.org)
  • clinical
  • The selective nature of this compound, which targets only PDE4D, also greatly improves the tolerability of the drug over past-studied, general PDE4 inhibitors, which should facilitate clinical trials in this difficult-to-treat population. (eurekalert.org)
  • After several COX-2 inhibiting drugs were approved for marketing, data from clinical trials revealed that COX-2 inhibitors caused a significant increase in heart attacks and strokes, with some drugs in the class having worse risks than others. (wikipedia.org)
  • In response to a report of precancerous changes in the pancreases of rats and organ donors treated with the DPP-4 inhibitor sitagliptin, the United States FDA and the European Medicines Agency each undertook independent reviews of all clinical and preclinical data related to the possible association of DPP-4 inhibitors with pancreatic cancer. (wikipedia.org)
  • These compounds were nonpeptidic renin inhibitors, had acceptable oral bioavailability and were potent enough for clinical use. (wikipedia.org)
  • The importance of renin in the pathogenesis of cardiovascular disease was, however, not fully understood until in the 1970s, and 20 years later the first renin inhibitors went to clinical trials. (wikipedia.org)
  • Aliskiren, the only renin inhibitor to go into phase III clinical trials, is not structurally related to peptides, which makes it a third-generation renin inhibitor. (wikipedia.org)
  • norepinephrine
  • Hyperforin and adhyperforin are wide-spectrum inhibitors of the reuptake of serotonin, norepinephrine, dopamine, glutamate, GABA, glycine, and choline, and they exert these effects by binding to and activating the transient receptor potential cation channel TRPC6. (wikipedia.org)
  • drugs
  • Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. (wikipedia.org)
  • The potential exists for adverse drug interactions with other drugs which inhibit or induce CYP3A4, including HIV protease inhibitors, ketoconazole, and itraconazole. (wikipedia.org)
  • Some of the DPP-4 inhibitor drugs have gotten approval from the FDA to be used with metformin concomitantly with additive effect to increase glucagon-like peptide 1 (GLP-1) which also decrease hepatic glucose production. (wikipedia.org)
  • Protease inhibitors (pronounced PRO-tee-ace in-HIH-bi-ters) are a new type of drugs that slow down the spread of HIV (human immunodeficiency virus) inside a person's body. (encyclopedia.com)
  • Although not a cure for this disease, protease inhibitors have proven to be a powerful anti-HIV drug, especially when taken in combination with certain other drugs. (encyclopedia.com)
  • The new class of drugs are called protease inhibitors because they "inhibit" or discourage something from happening. (encyclopedia.com)
  • Attachment inhibitors are part of a larger class of HIV drugs called entry inhibitors. (nih.gov)
  • Cytogenetics Discovery and development of tubulin inhibitors Medicinal molds Mitosis "What Are the Different Types of Chemotherapy Drugs? (wikipedia.org)
  • ALK inhibitors are potential anti-cancer drugs that act on tumours with variations of anaplastic lymphoma kinase (ALK) such as an EML4-ALK translocation. (wikipedia.org)
  • There are fixed-dose combination drugs, such as ACE inhibitor and thiazide combinations. (wikipedia.org)
  • Renin inhibitors are a group of pharmaceutical drugs used primarily in treatment of essential hypertension (high blood pressure). (wikipedia.org)
  • A CETP inhibitor is a member of a class of drugs that inhibit cholesterylester transfer protein (CETP). (wikipedia.org)
  • PDE4 inhibitors have proven potential as anti-inflammatory drugs, especially in inflammatory pulmonary diseases such as asthma, COPD, and rhinitis. (wikipedia.org)
  • Proteasome inhibitors are drugs that block the action of proteasomes, cellular complexes that break down proteins. (wikipedia.org)
  • Recognition that the knowledge about PDE could be used to develop drugs that were PDE inhibitors led to extensive research. (wikipedia.org)
  • PDE4
  • PDE4 inhibitors may have antidepressive effects and have also recently been proposed for use as antipsychotics. (wikipedia.org)
  • Treatment with a PDE4 inhibitor raised the deficient cAMP levels and restored some functionality to Hippocampus-based memory functions. (wikipedia.org)
  • biosynthesis
  • whereas antigonadotropins suppress gonadal production of sex steroids by effecting negative feedback on and thereby suppressing the hypothalamic-pituitary-gonadal axis, steroidogenesis inhibitors directly inhibit the enzymatic biosynthesis of steroids. (wikipedia.org)
  • HMG-CoA reductase (HMGCR) inhibitors, also known as statins, prevent the conversion of HMG-CoA into mevalonic acid, a relatively early step in the biosynthesis of cholesterol from acetyl coenzyme A (acetyl-CoA), and thereby decrease cholesterol levels. (wikipedia.org)
  • Farnesyl pyrophosphate synthase (FPPS) inhibitors prevent the conversion of isopentenyl pyrophosphate (IPP) into farnesyl pyrophosphate (FPP), a mid-range step in the biosynthesis of cholesterol from acetyl-CoA, and thereby inhibit cholesterol production. (wikipedia.org)
  • 7-Dehydrocholesterol reductase (7-DHCR) inhibitors such as AY-9944 and BM-15766 inhibit the production of cholesterol from 7-dehydrocholesterol, one of the last steps in cholesterol biosynthesis. (wikipedia.org)
  • 24-Dehydrocholesterol reductase (24-DHCR) inhibitors such as azacosterol and triparanol inhibit the production of cholesterol from desmosterol, one of the last steps in cholesterol biosynthesis, and were formerly used to treat hypercholesterolemia, but were withdrawn from the market due to toxicity caused by accumulation of desmosterol in tissues. (wikipedia.org)
  • drug
  • A phosphodiesterase type 5 inhibitor (PDE5 inhibitor) is a drug used to block the degradative action of cGMP-specific phosphodiesterase type 5 (PDE5) on cyclic GMP in the smooth muscle cells lining the blood vessels supplying the corpus cavernosum of the penis. (wikipedia.org)
  • The occurrence of adverse drug reactions (ADRs) with PDE5 inhibitors appears to be dose-related. (wikipedia.org)
  • In 2007, the U.S. Food and Drug Administration (FDA) announced that a warning about possible sudden hearing loss would be added to drug labels of PDE5 inhibitors. (wikipedia.org)
  • Selective COX-2 inhibitors are a type of nonsteroidal anti-inflammatory drug (NSAID) that directly targets cyclooxygenase-2, COX-2 , an enzyme responsible for inflammation and pain . (wikipedia.org)
  • FDA has added a new Warning and Precaution about this risk to the labels of all medicines in this drug class, called dipeptidyl peptidase-4 (DPP-4) inhibitors. (wikipedia.org)
  • Currently, attachment inhibitors are still under investigation and have not been approved by the Food and Drug Administration (FDA) for patient use. (nih.gov)
  • Griseofulvin, derived from a species of Penicillium is an mitotic inhibitor that is used as an antifungal drug. (wikipedia.org)
  • Thus far, Periostat (active ingredient is doxycycline hyclate) is the only MMP inhibitor that has been approved by the U.S. Food and Drug Administration (FDA). (wikipedia.org)
  • A TNF inhibitor is a pharmaceutical drug that suppresses the physiologic response to tumor necrosis factor (TNF), which is part of the inflammatory response. (wikipedia.org)
  • However, these inhibitors had also limited drug-like properties. (wikipedia.org)
  • A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), thereby preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s). (wikipedia.org)
  • Can the old drug, disulfiram, have a bright new future as a novel proteasome inhibitor? (wikipedia.org)
  • ketoconazole
  • Cholesterol side-chain cleavage enzyme (P450scc, CYP11A1) inhibitors such as aminoglutethimide, ketoconazole, and mitotane inhibit the production of pregnenolone from cholesterol and thereby prevent the synthesis of all steroid hormones. (wikipedia.org)
  • 17α-Hydroxylase/17,20-lyase (CYP17A1) inhibitors such as abiraterone acetate, etomidate, galeterone, ketoconazole, and orteronel inhibit the production of androgens and glucocorticoids and are used to reduce androgen levels in the treatment of prostate cancer. (wikipedia.org)
  • 11β-Hydroxylase (CYP11B1) inhibitors such as amphenone B, etomidate, ketoconazole, metyrapone, mitotane, and osilodrostat inhibit the production of the potent corticosteroids cortisol, corticosterone, and aldosterone from the less potent corticosteroids 11-deoxycorticosterone and 11-deoxycortisol and are used in the diagnosis and treatment of Cushing's syndrome. (wikipedia.org)
  • treatments
  • Use of topoisomerase inhibitors for antineoplastic treatments may lead to secondary neoplasms because of DNA damaging properties of the compounds. (wikipedia.org)
  • affinity
  • Two molecular features of most MMP inhibitors are responsible for the affinity. (wikipedia.org)
  • There is a similar twist in cAMP and there is general agreement that high affinity PDE3 inhibitors should adopt an energetically favoured planar conformation that mimics the anti conformation of cAMP. (wikipedia.org)
  • treatment
  • Grand Rapids, MI (Nov. 7, 2017) - New preclinical research suggests the potential utility of BPN14770, a selective PDE4D inhibitor currently under development by Tetra Discovery Partners as a prospective treatment for memory and cognitive problems associated with Alzheimer's disease, in the treatment of Fragile X Syndrome (FXS) and possibly other autism spectrum disorders. (eurekalert.org)
  • Angiogenesis inhibitors were once thought to have potential as a " silver bullet " treatment applicable to many types of cancer , but the limitations of anti-angiogenic therapy have been shown in practice. (wikipedia.org)
  • Because PDE5 is also present in the arterial wall smooth muscle within the lungs, PDE5 inhibitors have also been explored for the treatment of pulmonary hypertension, a disease in which blood vessels in the lungs become overloaded with fluid, usually as a result of failure of the right ventricle of the heart. (wikipedia.org)
  • PDE5 inhibitors such as sildenafil (Viagra), tadalafil (Cialis), and vardenafil (Levitra) are clinically indicated for the treatment of erectile dysfunction. (wikipedia.org)
  • Sildenafil, the prototypical PDE5 inhibitor, was originally discovered during the search of a novel treatment for angina. (wikipedia.org)
  • Development of dipeptidyl peptidase-4 inhibitors "FDA Approves New Treatment for Diabetes" (Press release). (wikipedia.org)
  • Mitotic inhibitors are used in cancer treatment, because cancer cells are able to grow and eventually spread through the body (metastasize) through continuous mitotic division. (wikipedia.org)
  • Examples of mitotic inhibitors frequently used in the treatment of cancer include paclitaxel, docetaxel, vinblastine, vincristine, and vinorelbine. (wikipedia.org)
  • Colchicine and griseofulvin are mitotic inhibitors used in the treatment of gout and toenail fungus, respectively. (wikipedia.org)
  • However, treatment with Top1 inhibitors, such as the camptothecins, stabilize the cleavable complexes, prevent DNA religation and induce lethal DNA strand breaks. (wikipedia.org)
  • ACE inhibitors were initially approved for the treatment of hypertension and can be used alone or in combination with other antihypertensive medications. (wikipedia.org)
  • A typical treatment plan often includes an ACE inhibitor, a beta blocker, a long-acting nitrate, and a calcium channel blocker, in combinations that are adjusted to the individual patient's needs. (wikipedia.org)
  • TNF is involved in autoimmune and immune-mediated disorders such as rheumatoid arthritis, ankylosing spondylitis, inflammatory bowel disease, psoriasis, hidradenitis suppurativa and refractory asthma, so TNF inhibitors may be used in their treatment. (wikipedia.org)
  • The main examples of FPPS inhibitors are nitrogenous bisphosphonates such as alendronate, ibandronate, pamidronate, risedronate, and zoledronate, which are used in the treatment of osteoporosis. (wikipedia.org)
  • Selective 17,20-lyase inhibitors such as seviteronel inhibit only androgen production without affecting glucocorticoid synthesis and are under development for the treatment of prostate cancer. (wikipedia.org)
  • lymphomas
  • Discontinued ASP-3026 (Astellas) NPM-ALK is a different variation/fusion of ALK that drives anaplastic large-cell lymphomas (ALCLs) and is the target of other ALK inhibitors. (wikipedia.org)
  • The important side effects of TNF inhibitors include lymphomas, infections (especially reactivation of latent tuberculosis), congestive heart failure, demyelinating disease, a lupus-like syndrome, induction of auto-antibodies, injection site reactions, and systemic side effects. (wikipedia.org)
  • cellular
  • Zinc finger inhibitors, or zinc ejectors, are substances or compounds that interact adversely with zinc fingers and cause them to release their zinc from its binding site, disrupting the conformation of the polypeptide chain and rendering the zinc fingers ineffective, thereby preventing them from performing their associated cellular functions. (wikipedia.org)
  • Metalloprotease inhibitors are cellular inhibitors of the Matrix metalloproteinases (MMPs). (wikipedia.org)
  • compounds
  • Topoisomerase inhibitors are chemical compounds that block the action of topoisomerase (topoisomerase I and II), which are enzymes that control the changes in DNA structure by catalyzing the breaking and rejoining of the phosphodiester backbone of DNA strands during the normal cell cycle. (wikipedia.org)
  • These compounds constitute a second generation of PDE inhibitors. (wikipedia.org)
  • citation needed
  • citation needed] To circumvent these limitations, Dr. Mark Cushman at Purdue University and Dr. Yves Pommier at the National Cancer Institute developed the non-camptothecin family of indenoisoquinoline inhibitors of Top1. (wikipedia.org)
  • inhibit the production
  • 3β-Hydroxysteroid dehydrogenase (3β-HSD) inhibitors such as amphenone B, azastene, cyanoketone, epostane, mitotane, and trilostane inhibit the conversion of Δ5-3β-hydroxysteroids into Δ4-3-ketosteroids and thereby inhibit the production of most of the steroid hormones. (wikipedia.org)
  • doses
  • When used in the central nervous system to alleviate neurological symptoms, such as rivastigmine in Alzheimer's disease, all cholinesterase inhibitors require doses to be increased gradually over several weeks, and this is usually referred to as the titration phase. (wikipedia.org)
  • Zinc
  • Zinc finger inhibitors are typically used to combat HIV. (wikipedia.org)
  • This method of using zinc finger inhibitors to target and destabilize zinc fingers represents a new method of fighting HIV. (wikipedia.org)
  • Other viruses such as SARS, polio, Ebola, measles, human coxsackie, Dengue, rabies, human hepatitis, human parainfluenza and human respiratory syncytical have similar zinc finger motifs and could potentially benefit from zinc finger inhibitor technology. (wikipedia.org)
  • In the design of these inhibitors, the basic protein backbone of collagen is maintained but the amide bond is replaced with a zinc-binding group. (wikipedia.org)