fibrils

NQTrp is an inhibitor of the aggregation of the tau protein with generic anti-amyloidogenic effects.

SynuClean-D (SC-D) is an α-synuclein aggregation inhibitor that prevents fibril propagation, disrupts mature amyloid fibrils, and abolishes dopaminergic neuron degeneration in an animal model of Parkinson's disease.

(-)-Epigallocatechin, the predominant flavonoid in green tea, possesses the unique ability to attach to unfolded native polypeptides, thereby inhibiting their transformation into amyloid fibrils.

EUK-134, a synthetic superoxide dismutase (SOD) catalase mimetic, exhibits potent antioxidant activities and inhibits the formation of β-amyloid and related amyloid fibrils.

BF 227 is a candidate for an amyloid imaging probe for PET [Ki: 4.3 nM for Aβ1-42 fibrils].

12-Crown-4 disrupts Aβ40 fibrils. 12-Crown-4 can enter into the hydrophobic core region and form competitive, hydrophobic interactions with key hydrophobic residues.

O4 is a novel stabilizer of amyloid- fibrils. O4 used for accelerating the formation of end-stage mature fibrils.

Aβ aggregation-IN-1 (Compound 1b) is an inhibitor of amyloid-beta precursor protein. It suppresses the aggregation and disaggregation of amyloid-beta fibrils with IC50 values of 3.92 and 7.19 M, respectively. Additionally, Aβ aggregation-IN-1 reduces malondialdehyde formation in neuronal cells, increases intracellular levels of reduced glutathione (GSH), and inhibits caspase 3.

AChE-IN-80 (Compound 1) is an inhibitor of acetylcholinesterase (AChE). It suppresses inflammation and reactive oxygen species (ROS) production in cultured neurons and microglia, induces autophagy, and prevents the spread of beta-amyloid (Aβ) fibrils. AChE-IN-80 exhibits antioxidant activity and neuroprotective effects, making it valuable for Alzheimer's disease research.

Flutafuranol, also known as AZD 4694 and NAV4694, is a bio-active chemical. AZD4694 shows high affinity for beta-amyloid fibrils in vitro (K(d) = 2.3 +/- 0.3 nM). The fluorine-18 labeled AZD4694 may have potential for PET-visualization of cerebral beta-am

Lawsoniaside can hinder the growth of amyloid-β42 fibrils.

DC-Chol hydrochloride(DC-Cholesterol hydrochloride) inhibited the formation of Aβ40 fibrils under appropriate experimental conditions and significantly inhibited amyloid formation from oxidized hCT in a dose-dependent manner.DC-Chol hydrochloride induces an improved and balanced immunity, which could contribute to hepatitis B vaccine research.

Amyloid-β (1-42) (Aβ42) is a neurotoxic 42-amino acid protein fragment found in amyloid plaques in postmortem cerebral cortex from patients with Alzheimer's disease.1,2,3Aggregation of Aβ42 results in the formation of neurotoxic fibrils or globular oligomers.1Aβ42 accumulates in the brain of many transgenic mouse models of Alzheimer's disease and, in many models, the onset of amyloid deposition positively correlates with deficits in spatial learning and memory.4 1.Wolfe, M.S.Therapeutic strategies for Alzheimer's diseaseNat. Rev. Drug Discov.1(11)859-866(2002) 2.Iwatsubo, T., Odaka, A., Suzuki, N., et al.Visualization of Aβ42(43) and Aβ40 in senile plaques with end-specific Aβ monoclonals: Evidence that an initially deposited species is Aβ42(43)Neuron13(1)45-53(1994) 3.Hardy, J.A., and Higgins, G.A.Alzheimer's disease: The amyloid cascade hypothesisScience256(5054)184-185(1992) 4.Jankowsky, J.L., and Zheng, H.Practical considerations for choosing a mouse model of Alzheimer's diseaseMol. Neurodegener.12(1)89(2017)

Amyloid-β (25-35) (Aβ (25-35)) is an 11-residue fragment of the Aβ protein that retains the physical and biological characteristics of the full length peptide. It forms fibrils that react to thioflavin T and Congo red and are organized in a cross-β arrangement of β-strands similar to Aβ (1-40) and Aβ (1-42) fibrils. Aggregated Aβ (25-35) decreases the viability of rat adrenal PC12 cells. It also decreases the viability of primary rat cortical neurons at concentrations ranging from 1 nM to 30 μM. In vivo, intracerebral injection of Aβ (25-35) (20 nmol) in rats induces lesions of neuronal and tissue loss. Aggregated Aβ (25-35) administered intracerebroventricularly to rats induces learning and memory impairments in the Y-maze, novel object recognition, and contextual fear conditioning tests.

TAMRA-Amyloid-β (1-42) peptide is a fluorescently labeled peptide. Amyloid-β (1-42) (Aβ42) is a neurotoxic 42-residue protein fragment found in amyloid plaques in postmortem cerebral cortex from patients with Alzheimer's disease. Aggregation of Aβ42 results in the formation of neurotoxic fibrils or globular oligomers. TAMRA-Amyloid-β (1-42) peptide is a labeled form of Aβ42 containing carboxytetramethyl rhodamine (TAMRA), which displays excitation/emission maxima of 543/572 nm, respectively.

Eprodisate is a novel compound specifically developed to disrupt the interactions between amyloidogenic proteins and glycosaminoglycans, effectively impeding the polymerization of amyloid fibrils and their deposition in tissues. This compound shows potential for delaying the advancement of AA amyloidosis-related renal disease and could apply to various forms of amyloidosis.

Crocin-4, a carotenoid compound found in saffron, possesses potent antioxidant properties and can penetrate the brain. It effectively inhibits the aggregation and deposition of Aβ fibrils, making it useful for Alzheimer's Disease research. Additionally, Crocin-4 demonstrates antitumor and anti-inflammatory activities.

BTA-1, an uncharged derivative of thioflavin-T, exhibits high affinity for Aβ fibrils and demonstrates excellent brain entry and clearance [1].

THK-5117 is an arylquinoline derivative with the potential as a PET probe for tau imaging. THK-5117 shows high binding affinity to tau fibrils with a Ki value of 10.5 nM. THK-5117 also shows high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD) brain homogenates [1].

THK-5105, an arylquinoline derivative, demonstrates high binding affinity for tau fibrils, protein aggregates, and tau-rich Alzheimer's disease (AD) brain homogenates, indicating its potential as a tau imaging PET (Positron Emission Tomography) probe with the radiolabeled version, 18F-THK-5105 [1].

ADS-J1 is an HIV-1 entry inhibitor that potently inhibits seminal amyloid fibrillization and block fibril-mediated enhancement of viral infection. Semen-derived amyloid fibrils, comprising SEVI (semen-derived enhancer of viral infection) fibrils and SEM1 fibrils, may remarkably enhance HIV-1 sexual transmission and are potential targets for the development of an effective microbicide.

q-FTAA, a potential research compound for Alzheimer's disease (AD), demonstrates binding affinity to Aβ1-42 fibrils and the Alzheimer's disease PIB binding complex (ADPBC), with EC50 values ranging from 330-630 nM and 300-500 nM, respectively.

Maysin, a neuroprotective C-glycosyl-flavone isolated from corn silk, protects against Syn amyloid aggregates-oligomers and fibrils-induced damage by preventing oxidative stress and intracellular calcium imbalance through autophagic activation. It is utilized in Parkinson's disease (PD) research [1].

Aβ Fibrillization Modulator 1 stabilizes amyloid-beta (Aβ) monomers, preventing their aggregation into fibrils.