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S1PR1 Targeted Libraries

S1PR1 Targeted LibrariesSphingosine-1-phosphate receptor 1 (S1PR1, S1P receptor 1, S1P1, endothelial differentiation gene 1, EDG1) is a G-protein-coupled receptor which binds the bioactive signaling molecule sphingosine 1-phosphate (S1P). S1PR1 has an important role in regulating endothelial cell cytoskeletal structure, migration, vascular maturation and capillary-like network formation. Also S1PR1 signaling is important in the regulation of lymphocyte maturation, migration and trafficking. Abnormal functioning of S1PR1 is associated with cancer and multiple sclerosis. Agonists and antagonists of this receptor may have therapeutic potential in the treatment of such diseases.

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RAR-related Orphan Receptor-γ Targeted Library

The Retinoic Acid Receptor-related Orphan Receptor-γ Targeted LibraryThe Retinoic Acid Receptor-related Orphan Receptor-γ (RORγ, RORc, NR1F3, RORG, RZR-GAMMA, RZRG, TOR or IMD42) plays an important role in metabolism, inimmunity and circadian rhythm. Abnormal functioning of RORγ is associated with inflammatory, immune and skin diseases including psoriasis. Antagonists and inverse agonists of this receptor may have therapeutic potential in the treatment of such diseases.

 

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MMP2 Targeted Library

MMP2 Targeted LibrariesThe Matrix metalloproteinase-2 (MMP2, gelatinase A, 72 kDa type IV collagenase) is involved in different functions such as reconstruction of the vasculature, angiogenesis, tissue repair, inflammation, tumor invasion and atherosclerotic plaque rupture. Mutations in the MMP2 gene are associated with Torg-Winchester syndrome, arthritis syndrome, multicentric osteolysis and other pathologies. Therefore, small molecule compounds targeting metalloproteinase-2 may be potential treatment for a variety of diseases related to abnormality functioning of MMP2.

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Natural Product-Like Library
Natural Product-Like LibraryNatural Product-Like Library has been designed as a special screening library containing synthetic compounds similar to natural.
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Agro-Targeted Libraries

Screening Compounds for Agrochemical DiscoveryTo facilitate a process of finding new agrochemicals within the fields of weed, pest and disease control, OTAVAchemicals design a set of focused libraries of diverse compounds for agrochemical research and development.

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GABA Receptors Targeted Libraries

GABA Receptors Targeted LibrariesThe GABA receptors (GABAA and GABAB) respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory compound in the mature vertebrate central nervous system. GABA receptors agonists produce typically sedative effects, and may also cause other effects such as anticonvulsant, anxiolytic and muscle relaxant effects. Antagonists of GABA receptors inhibit the action of GABA. In general they produce stimulant and convulsant effects. Therefore, small molecule compounds modulating GABA receptors activity may have significant therapeutic potential.

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ß-Arrestin/ß2-Adaptin Interaction Targeted Library

Caspase 2 Targeted LibrariesBeta-arrestins (ß-arrestin 1 and ß-arrestin 2) play central roles in the mechanisms regulating G protein-coupled receptors signalling and trafficking. They participate in agonist-mediated desensitization of GPCR and cause specific dampening of cellular responses to stimuli such as sensory signals, hormones or neurotransmitters [1].

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Nuclear ER Targeted Libraries

Estrogen Receptor Targeted LibrariesNuclear estrogen receptors (ERα and Erβ) are members of the nuclear receptor family of intracellular receptors. Estrogen receptors (ERs) are involved in modulation of biological activities, such as reproductive organ development, bone modeling, cardiovascular system functioning, metabolism and behavior in both females and males.

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AD Polypharmacology Library

AD Targeted Polypharmacology Library

Alzheimer's disease (AD) is a complex neurodegenerative disorder of the central nervous system that usually starts slowly and gets worse over time. It is characterized by progressive loss of dementia, cognitive ability, and eventually death. Currently there is no cure for the disease.

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PRMTs Targeted Library

Protein Arginine Methyltransferases Targeted Library Epigenetic targets are a major new category for successful drug research. Among them the protein methyltransferases (PMTs) which have crucial roles in gene transcription are an important group of enzymes that play key parts in normal physiology and human diseases. There has been a significant increase in attention towards protein arginine methyltransferases (PRMTs) which catalyze methylation of nitrogen of specific arginine residues in proteins and impact on numerous essential biological pathways by methylating different nuclear, cytoplasmic and membrane protein substrates.

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Renin Targeted Library

Renin Targeted LibraryThe Renin (REN, HNFJ2) is an aspartic protease (also known as an angiotensinogenase). It participates in arterial vasoconstriction and the body's renin–angiotensin–aldosterone system (RAAS) that mediates the volume of extracellular fluid (blood plasma, lymph and interstitial fluid). Thus, it regulates the body's mean arterial blood pressure. An over-active RAAS leads to vasoconstriction and retention of sodium and water. These effects cause hypertension. Therefore, renin inhibitors can be used for the treatment of hypertension.

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Kallikrein 6 Targeted Library

Kallikrein 6 Targeted LibrariesKallikrein 6 (KLK6, hK6, Bssp, Klk7, PRSS18, PRSS9, SP59, kallikrein related peptidase 6) plays an important role in various physiological processes. Disorders of KLK6 activity are observed at cancer and neurodegenerative diseases, such as Alzheimer’s disease and multiple sclerosis. Therefore, small molecule compounds modulating kallilrein 6 activity may have a significant therapeutic potential.

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Peptidomimetic Libraries

Peptidomimetic LibrariesThe interaction of proteins are critical to nearly all biological processes, including cellular signaling [1]. We offer special screening Peptidomimetic Libraries: β-Turn Peptidomimetic Library containing synthetic compounds which mimic beta-turns of proteins and a-Helix Peptidomimetic Library of compounds mimic alpha-helixes of proteins. These libraries are intended for research and drug discovery projects focused on protein-protein interactions.

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SARMs-Like Library

Selective Androgen Receptor Modulators-Like LibrarySelective androgen receptor modulators (SARMs) act on the androgen receptors (ARs) in a tissue-selective manner and provide an opportunity to promote the beneficial effects of androgens in target tissues with greatly reduced unwanted side-effects. SARMs have been proposed as treatments of choice for various diseases, including muscle-wasting, breast cancer, and osteoporosis.

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Caspase 2 Targeted Library

Caspase 2 Targeted LibrariesCaspase 2 (CASP2, CASP-2, ICH1, NEDD-2, NEDD2, PPP1R57) is an initiator caspase for cellular apoptosis. It is also involved in several other vital processes including oxidative stress responses, regulation of cell cycle checkpoints, autophagy and senescence. Disorders of CASP2 activity are observed at obesity, metabolic syndrome, nonalcoholic fatty liver disease and cancer [1, 2]. Therefore, small molecule compounds modulating CASP2 activity may have significant therapeutic potential.

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SERMs-Like Library

Selective Estrogen Receptor Modulators-Like LibrarySelective estrogen receptor modulators (SERMs) are compounds that act on the estrogen receptors (ERs). A characteristic that distinguishes these substances from pure ER antagonists and agonists (silent antagonists and full agonists) is that their action is different in various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues.

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Transporter Targeted Libraries

Estrogen Receptor Targeted Libraries Transporters are proteins that span the plasma membrane and regulate the traffic of small molecules in and out of the cell. They play a particularly important role in chemical signalling between neurons in the CNS, where they act to control the concentration of neurotransmitters in the synapse. Another key role for transporters is in excluding undesirable xenobiotics from the cell, whilst allowing key molecules required for the cell life cycle to enter. The majority of transporters are targets for drug discovery.

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ERR Gamma Targeted Library

Phenotypic Screening Library

Estrogen-related receptor gamma (ERRγ) is involved in energy metabolism, mitochondrial functions, biogenesis and tissue repair. Disorders of ERRγ are observed at type 2 diabetes, hypoxia, metabolic syndrome and cancer. Therefore, small molecule compounds modulating ERRγ activity may have significant therapeutic potential.

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SH2 Domain Targeted Library

SH2 Domain Targeted LibraryThe SH2 (Src Homology 2) domains play key roles in different kinase-mediated intracellular signal transduction pathways and many human diseases are associated with their dysregulation [1, 2].

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ClpP Targeted Library

Mitochondrial Proteases Targeted Libraries Caseinolytic protease (ClpP) found in the human mitochondria is a major member of mitochondrial protein quality control system. This serine protease removes damaged or misfolded proteins in mitochondrial matrix. It is overexpressed in a wide range of acute myeloid leukemia (AML) cases and not in normal hematopoietic precursors [1].

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