X-Nico

unusual facts about inhibitor


Unc-5

Inhibitory factors such as UNC-5 play essential roles in the formation and maintenance of synaptic components.


4-Nonylphenylboronic acid

4-Nonylphenylboronic acid is a potent and selective inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC50 of 9.1nM, and 870x selectivity for FAAH over the related enzyme MAGL, which it inhibits with an IC50 of 7900nM.

Apocynin

Due to the selectivity of its inhibition, apocynin can be widely used as an inhibitor of NADPH oxidase without interfering in other aspects of the immune system.

Aromatic L-amino acid decarboxylase inhibitor

An aromatic L-amino acid decarboxylase inhibitor (synonyms: DOPA decarboxylase inhibitor, DDCI and AAADI) is a drug which inhibits the synthesis of dopamine by the enzyme aromatic L-amino acid decarboxylase (AAAD, or DOPA decarboxylase, DDC).

Astemizole

Astemizole does also act as FIASMA (functional inhibitor of acid sphingomyelinase).

ATP5E

The epsilon subunit is located in the stalk region of the F1 complex, and acts as an inhibitor of the ATPase catalytic core.

Atypical chronic myeloid leukemia

This sharply contrasts with the outcome for CML, for which the prognosis was dramatically improved by the development of imatinib as a specific inhibitor of the BCR-ABL protein and in particular for CML.

Atypical hemolytic uremic syndrome

Before the introduction of eculizumab (INN and USAN, trade name Soliris), a monoclonal antibody that is a first-in-class terminal complement inhibitor, management options for patients with aHUS were extremely limited.

Botanical identity of soma–haoma

Peganum Harmala contains Harmaline, which is a strong MAO-inhibitor, and it is therefore often used as a 1st component in Ayahuasca ceremonies in order to inhibit the metabolisation of an orally-administered DMT molecule (2nd component).

C20H27NO3

Trilostane, an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome

Carboxypeptidase A inhibitor

The N-terminal region and the mature inhibitor are weakly related to other solananaceous proteins found in this family, from potato, tomato and henbane, which have been incorrectly described as metallocarboxypeptidase inhibitors.

Carlo Gambacorti-Passerini

He is also the first researcher who (in June 2010) successfully treated a patient affected by ALK+ lymphoma with an ALK inhibitor (crizotinib).

Cathepsin K

Merck has a Cathepsin K inhibitor in Phase 3 clinical trials by the name of Odanacatib for an expected indication of osteoporosis.

Cipemastat

Cipemastat (rINN, also known as Ro 32-3555 and by the tentative trade name Trocade) is a selective inhibitor of matrix metalloproteinase-1 that has been investigated as an anti-arthritis agent.

CUTL1

Researchers from the Wellcome Trust Sanger Institute reported that the mutation of CUX1 reduces the inhibitory effects of a biological inhibitor, PIK3IP1 (phosphoinositide-3-kinase interacting protein 1), resulted in higher activity of the growth promoting enzyme, phosphoinositide 3-kinase (PI3K) which leads to tumor progression.

Duroia

In the case of Duroia hirsuta, the chemical inhibitor is aided by the leafcutter ant Myrmelachista schumanni resident on and in the tree, and playing an active role in suppressing and destroying plant growth in the vicinity of their host by injecting and spraying formic acid.

Funny current

Ivabradine is the most specific and selective If inhibitor and the only member of this family that is now marketed for pharmacological treatment of chronic stable angina in patients with normal sinus rhythm who have a contraindication or intolerance to beta-blockers.

GABA transaminase inhibitor

A GABA transaminase inhibitor is an enzyme inhibitor that acts upon GABA transaminase.

Gemigliptin

Gemigliptin is a competitive, reversible DPP-4 inhibitor (IC50 = 16 nM) with excellent selectivity over other critical human proteases such as DPP-2, DPP-8, DPP-9, elastase, trypsin, urokinase and cathepsin G.

GSK2606414

GSK2606414 is a drug which is the first selective inhibitor discovered for the enzyme protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK), which is involved in various processes relating to cancer and neurodegenerative disorders.

Guadinomine

Guadinomine B is the most potent known inhibitor of the Type III Secretion System (TTSS) of Gram-negative bacteria.

Hes3 signaling axis

:* Activation of the signaling pathway by Delta4, Angiopoietin 2, insulin, or a combination of the three and a JAK inhibitor induces motor skill improvements in adult rat models of Parkinson's disease (6-hydroxydopamine model).

Hyperchloremic acidosis

Renal tubular acidosis failure of HCO3- resorption(i.e., proximal renal tubular acidosis, or overdose of carbonic anhydrase inhibitor) or failure of H+ secretion (i.e. in distal renal tubular acidosis)

Methylthioninium chloride

Methylthioninium chloride (INN, or methylene blue, proposed trade name Rember) is an investigational drug being developed by the University of Aberdeen and TauRx Therapeutics that has been shown in early clinical trials to be an inhibitor of Tau protein aggregation.

Myeloperoxidase

Azide has been used traditionally as an MPO inhibitor, but 4-aminobenzoic acid hydrazide (4-ABH) is a more specific inhibitor of MPO.

Netherton syndrome

Netherton syndrome is an autosomal recessive disorder associated with mutations in the SPINK5 gene, which encodes the serine protease inhibitor lympho-epithelial Kazal-type-related inhibitor (LEKTI).

NFATC4

Indeed NFAT3 (NFATc4) is an inhibitor of cell motility by blocking the expression of LCN2.

Phenylethylidenehydrazine

Phenylethylidenehydrazine (PEH) is an inhibitor of the enzyme GABA transaminase (GABA-T).

Plasminogen activator inhibitor-1

Plasminogen activator inhibitor-1 has been shown to interact with ORM1.

PPP1R3C

Several targeting subunits of PP1 have been identified, including PPP1R5, the glycogen-binding subunits PTG and R6 and PPP1R4, and the nuclear inhibitor of PP1 (PPP1R8).

Prinomastat

Prinomastat (AG-3340) is a matrix metalloprotease (MMP) inhibitor with specific selectivity for MMPs 2, 3, 9, 13, and 14.

Pseudowintera

Polygodial has been tested as a very effective inhibitor of Candida albicans.

Pulse pressure

If the patient suffers from elevated pulse pressure, treatment may include medications that address this factor, such as an angiotensin-converting enzyme inhibitor (ACE inhibitor).

SERBP1

Plasminogen activator inhibitor 1 RNA-binding protein (serbp1, not to be confused with srebp1) is a protein that in humans is encoded by the SERBP1 gene.

Sivelestat

Sivelestat (INN, research name ONO 5046, marketed as Elaspol) is an inhibitor of human neutrophil elastase.

SPINK6

It is a potent inhibitor of epidermal proteases involved in maintaining skin homeostasis, including KLK5, KLK7 and KLK14.

Trichorrhexis invaginata

The Netherton syndrome Mendelian Inheritance in Man is inherited as an autosomal recessive disorder due to mutations of both copies of the SPINK5 gene (localized to band 5q31-32), which encodes the serine protease inhibitor LEKTI (lymphoepithelial Kazal-type-related inhibitor).

Trypsin inhibitor

A study revealing that protease inhibitor from the eggs of the freshwater snail Pomacea canaliculata, interacting as a trypsin inhibitor with the protease of potential predators, was reported in 2010, the first direct evidence for this mechanism in the animal kingdom.

Trypsinogen

A further safeguard against inappropriate trypsin activation is the presence of inhibitors such as bovine pancreatic trypsin inhibitor (BPTI) and serine protease inhibitor Kazal-type 1 (SPINK1), which binds to any trypsin formed.

Uncaria

rhynchophylla has also been shown to be a powerful MAO-B inhibitor.

Varespladib methyl

Varespladib methyl (also known as A-002, formerly LY333013 and S-3013) is a secretory phospholipase A2 (sPLA2) inhibitor formerly under development by Anthera Pharmaceuticals as a treatment for acute coronary syndrome (ACS).

Vibrionaceae

Members of this family also synthesize tetrodotoxin (TTX), an ancient marine alkaloid and powerful neurotoxin (Na+ pump inhibitor, 1 mg can kill an adult) that serves to protect members of an order of fishes, the Tetraodontiformes (tetras-four and odontos-tooth), which include the puffer fish (see fugu, raw puffer fish served in Japan).

Vitamin P

Fluoxetine (Prozac), euphemistically referred to as Vitamin P, a selective serotonin reuptake inhibitor (SSRI) used for depression and various mental disorders

Paroxetine (Paxil), euphemistically referred to as Vitamin P, a selective serotonin reuptake inhibitor (SSRI) used for depression and anxiety disorders

Volasertib

Volasertib (also known as BI 6727) is a small molecule inhibitor of the PLK1 (polo-like kinase 1) protein being developed by Boehringer Ingelheim for use as an anti-cancer agent.

WHEP-TRS protein domain

EPRS is a component of the interferon-gamma-activated inhibitor of translation (GAIT) complex, which interacts with stem-loop elements (GAIT elements) in mRNAs encoding proinflammatory proteins, for example, vascular endothelial growth factor-A (VEGFA).

Whey Acidic Protein

There have been several candidate markers for cancer; most notably genes coding for elafin, antileukoproteinase 1 (previously called secretory leucocyte proteinase inhibitor, SLPI), WAP four disulphide core domain protein 1 (previously called prostate stromal protein 20 kDa, PS20), and WAP four disulphide core domain protein 2 (previously called major human epididymis-specific protein E4, HE4).

ZIC3

ZIC2, another member of the ZIC family, has recently been found to interact with TCF7L2, enabling it to act as a Wnt/β-catenin signalling inhibitor.


see also