enzymatically

TMPD dihydrochloride is an active substrate of enzymatically convert redox and an electron donor for the reduction of heme peroxidases.

D-(+)-Cellobiose (Cellobiose) is a disaccharide, a reducing sugar, consists of two β-glucose molecules linked by a β(1→4) bond. It can be hydrolyzed to glucose enzymatically or with acid.

PSB-1114 tetrasodium shows >50-fold selectivity versus the P2Y4 (EC50: 9.3 μM) and P2Y6 (EC50: 7.0 μM) receptors. PSB-1114 tetrasodium is an effective, enzymatically stable, and subtype-selective P2Y2 receptor agonist (EC50: 134 nM) .

Bradykinin (acetate) is an active peptide that is generated by the kallikrein-kinin system. It is a inflammatory mediator and also recognized as a neuromediator and regulator of several vascular and renal functions. Enzymatically produced from kallidin in the blood, it is a powerful vasodilator that causes smooth muscle contraction, and may mediate inflammation. It has a role as a human blood serum metabolite and a vasodilator agent. It is a tautomer of a bradykinin(2+).

Ginsenoside F1 (20(S)-Ginsenoside F1) is an enzymatically modified derivative of ginsenoside Rg1, showing competitive inhibition of the activity of CYP3A4 and a weaker inhibition of the activity of CYP2D6.

Enzymatically-derived prostaglandin E2 (PGE2) is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings of oxidative stress via the isoprostane pathway. A proposed mechanism for the formation of rac-PGE2 involves the base catalyzed equilibration from 15-E2t-isoprostane (8-iso-PGE2), generated from the 15-H2t-isoprostane endoperoxide.

12-oxo Leukotriene B4 (12-Oxo-LTB4) is a potent pro-inflammatory lipid mediator classified as a dihydroxy fatty acid that is enzymatically derived from arachidonic acid metabolism via the 5-lipoxygenase (5-LO) pathway, and it promotes a diverse array of leukocyte functional responses including cellular aggregation, stimulation of transmembrane ion fluxes, enhancement of lysosomal enzyme release, superoxide anion generation, chemotaxis, and chemokinesis; 12-oxo Leukotriene B4 is an initial oxidative metabolite formed from Leukotriene B4 via the LTB4 12-hydroxydehydrogenase pathway, which undergoes rapid enzymatic conversion first to 10,11-dihydro-12-oxo-LTB4 followed by reduction of the 12-oxo group to yield 10,11-dihydro-LTB4, and this metabolite exhibits significantly reduced biological potency, being approximately 70-fold less potent than LTB4 in stimulating Ca2+ mobilization in human neutrophils (EC50 = 33 nM vs. 0.46 nM) and also markedly less effective at stimulating neutrophil migration (EC50 = 170 nM vs. 2.7 nM).

5-Fluorouridine 5'-O-β-D-galactopyranoside (also known as 5'-O-β-D-galactosyl-5-fluorouridine) is a prodrug of 5-Fluorouridine. It can be enzymatically converted by β-D-galactosidase into 5-Fluorouridine, a highly effective antineoplastic agent.

2'-O-(2-Methoxyethyl)guanosine (2'-O-MOE-rG), a modified nucleoside, can be enzymatically converted from 2'-O-(2-methoxyethyl)-2,6-diaminopurine riboside by adenosine deaminase; however, it is not readily phosphorylated by cytosolic nucleoside kinases and cannot be incorporated into cellular DNA or RNA.

NG-497 is a selective, small molecule inhibitor of human adipose triglyceride lipase (ATGL) that targets the enzymatically active patatin-like structural domain of human ATGL.NG-497 binds ATGL in a hydrophobic lumen adjacent to the active site.NG-497 abrogates lipolysis in human adipocytes in a dose-dependent and reversible manner.NG-497 has been shown to be useful in cancer research. can be used in cancer research.

Metrifonate is an organophosphorus prodrug that is metabolised non-enzymatically in the body to DDVP (dichlorvos), which acts as an irreversible cholinesterase (ChE) inhibitor. It inactivates ChE by phosphorylating the serine residue at its active site, making it useful for treating Alzheimer's disease and as an insecticide. Metrifonate affects AChE activity, oxidative stress, neurotoxicity, and cortisol levels in carp.

Vobramitamab (AEX-4089) is a humanized monoclonal antibody (mAb) targeting the B7-H3 antigen (CD276) which is conjugated to the prodrug seco-duocarmycin hydroxybenzamide azaindole (seco-DUBA) through a enzymatically cleavable peptide-based linker, thereby creating the investigational antibody-drug conjugate (ADC) known as MGC018.

PSB-1114 triethylamine is a potent, enzymatically stable, P2Y2 receptor agonist with a 134 nM EC50, exhibiting greater than 50-fold selectivity over P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors [1].

Poly(A) polymerase enzymatically adds a polyadenosine tail of 20-200 adenine bases to the 3' end of RNA, a process that involves integrating ATP as AMP. This modification enhances RNA stability and augments mRNA translation efficiency in eukaryotic cells, evidencing the enzyme's high tailing efficiency [1] [2].

GLP-1 (1-36) amide (human, rat) is a molecular variant of the GLP-1 (7-36) amide and has the capacity to stimulate [14C]aminopyrine accumulation in enzymatically dispersed, enriched rat parietal cells [1].

The sPLA2-IIA Inhibitor is a cyclic pentapeptide analog of FLSYK, specifically cyclic 2-Nal-Leu-Ser-2-Nal-Arg (c2), which interacts with human IIA phospholipase A2 (hGIIA) to impede its ester bond hydrolyzing function. As part of the esterase superfamily, sPLA2 enzymatically cleaves the sn-2 ester bond in glycerophospholipids, releasing arachidonic acid and lysophospholipids[1].

NBD-LLLLpY is a peptide synthesized enzymatically within the nucleus to selectively target and eliminate human induced pluripotent stem cells (hiPSCs).

Prostaglandin E2 Ethanolamide (PGE 2 -EA), an analog of PGE2, is enzymatically synthesized through COX-2 oxygenation of endocannabinoids. It has the potential to modulate the production of the proinflammatory cytokine TNF-α in human blood and monocytic cells [1] [2].

11(S)-HETE, an (S) enantiomer of 11(R)-HETE and a type of oxylipin, is non-enzymatically synthesized from arachidonic acid. Compared to its counterpart, 11(S)-HETE levels are found to be elevated in both isolated human plasma and serum, as well as in LPS-stimulated isolated human plasma. Notably, patients with allergic rhinitis exhibit a decrease in 11(S)-HETE levels in their serum following one year of double-mite subcutaneous immunotherapy (DM-SCIT), correlating with an enhanced quality of life, particularly in aspects related to rhinoconjunctivitis.

Oxidized low-density lipoprotein (oxLDL) encompasses low molecular weight entities that facilitate monocyte differentiation and activate polymorphonuclear leukocytes. A substance, recently isolated and purified from oxLDL and identified as azelaoyl PC, exemplifies this. Similarly, Butanoyl PAF, a compound closely related to azelaoyl PC, maintains over 10% of the agonist potency of platelet-activating factor (PAF). Notably, Butanoyl PAF's concentration in oxLDL surpasses that of enzymatically generated PAF by more than 100-fold, making it a significant signalling molecule within oxLDL.

Prostaglandin D2 (PGD2) is one of the five principal prostaglandins enzymatically derived from PGH2. It is abundantly generated in the cerebrospinal fluid (CSF) by lipocalin-type PGD synthase and in peripheral regions by myeloid cells, such as mast cells and basophils, via leukocyte-type PGD synthase. The compound 1,25-trans-PGD2 is an isomer of PGD2, characterized by the alteration of the double bond between carbons 5 and 6 from cis(Z) to trans(E). This trans isomer, found as a 2-5% impurity in most commercial PGD2 bulk drug preparations, is primarily synthesized as an analytical standard to identify and quantify this impurity. Based on existing studies of trans isomers of F-type prostaglandins, 5-trans-PGD2 likely exhibits biological activity comparable to its cis isomer, although no specific published reports confirm this for 5-trans-PGD2.

1,3-Diarachidoyl glycerol, a diacylglycerol featuring arachidic acid at the sn-1 and sn-3 positions, is identified within enzymatically randomized pig lard.

Rolinsatamabtalirine (ABBV 176) is an antibody-drug conjugate (ADC) that targets the Prolactin receptor (PRLR). It consists of the antibody Rolinsatamab, an enzymatically cleavable peptide linker, and the cytotoxic agent SGD-1882.

BT1769 is a bicyclic toxin conjugate targeting MT1-MMP (Matrilysin 1 type-MMP) with a KD of 3.35 nM. It is utilized for osteosarcoma research. BT1769 comprises an innovative bicyclic targeting peptide that selectively binds to MT1-MMP, a cytotoxin MMAE, and a dipeptide linker that can be enzymatically cleaved.