Dysfunction of N-methyl-d-aspartate receptor (NMDAR) signaling in the nucleus accumbens (NAc) has been implicated in the pathophysiology of alcohol use disorders (AUD). Neurogranin (Ng), a calmodulin-binding protein, is exclusively expressed in the post-synapse, and mediates NMDAR driven synapti...

Neurogranin is a calmodulin binding protein that has been implicated in learning and memory, long-term potentiation and synaptic plasticity. Neurons expressing neurogranin in the cortex degenerate in late stages of Parkinson’s disease with widespread α-synuclein pathology. While analyzing neur...

ObjectivesNeurogranin (NRGN) is a small neuronal protein that plays an important role in synaptic signaling by regulating calmodulin (CaM) availability. In this study, we developed an ELISA to measure NRGN quantitatively in serum samples from a cohort of acute traumatic brain injury (TBI) patien...

IntroductionBiomarkers monitoring synaptic degeneration/loss would be valuable for Alzheimer's disease (AD) diagnosis. Postsynaptic protein neurogranin may be a promising cerebrospinal fluid (CSF) biomarker but has not yet been evaluated as a plasma biomarker.

Hypothalamic inflammation has been known as a contributor to high-fat diet (HFD)-induced insulin resistance and obesity. Myeloid-specific sirtuin 1 (SIRT1) deletion aggravates insulin resistance and hypothalamic inflammation in HFD-fed mice. Neurogranin, a calmodulin-binding protein, is expresse...

Glutamate dysregulation is known to contribute to many psychiatric disorders including schizophrenia. Aberrant cortico-striatal activity and therefore glutamate levels might be relevant to this disease characterized by reduced prepulse inhibition (PPI), however, the molecular and behavioral mech...

Xanthine oxidase is a key enzyme that catalyses hypoxanthine and xanthine to uric acid, whose overproduction leads to the gout-causing hyperuricemia. In this study, a series of 1-hydroxy/methoxy-4-methyl-2-phenyl-1H-imidazole-5-carboxylic acid derivatives (4a–4k and 6a–6k) was synthesized and ...

Single Diethyl [hydroxy (phenyl) methyl] phosphonate (DHPMP) crystal with chemical formula C11H17O4P, was synthesized via the base-catalyzed Pudovik reaction and Lewis acid as catalyst. The results of SXRD analyzes indicate that this compound crystallizes into a mono-clinic system with space gro...

The synthesis and stereochemical aspects of the aldol products, 5-methyl-3-(substituted phenyl)-5-[(substituted phenyl) hydroxy methyl]-2-thiooxazolidin-4-ones, are discussed.

A tridentate Schiff base ligand (5-methyl-2-hydroxy-acetophenone-S-methyl-thiosemicarbazone, H2L) and its mononuclear nickel complex, [NiL(PPh3)], were obtained and characterized by spectroscopic techniques. Structural analysis of the compounds was supported by complementing crystallographic stu...

A green and convenient synthetic method has been described for the synthesis of 2-hydroxy-3-((5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)(phenyl)methyl)naphthalene-1,4-dione derivatives by a one-pot, four-component reaction of aromatic aldehydes, 2-hydroxy-1,4-naphthoquinone, hydrazine ...

In the present study, a wide variety of 3-{[(1, 3-benzoxazol-2-yl) sulfanyl] (phenyl) methyl}-4-hydroxy-2H-1-benzopyran-2-one derivatives were synthesized through one-pot three-component reaction using 4-hydroxy coumarin, 2-mercapto benzoxazole and substituted aldehydes in presence of L-proline ...

The endiyne derivative, dynemicin, is postulated to undergo bioreductive cis ring opening of a benzylic epoxide and activate the endiyne unit for Bergman rearrangement to an arene-1,4-diyl.

Dynemicin A, a potent antitumor antibiotic has novel 10-membered cyclic enediyne moiety. The bicyclo[7.3.1]-tridecadiyne system having aniline moiety o

Utilizing a cross-coupling reaction between the arylstannane 5 and the iodoenone 7, the arylcyclohexenone 8 was prepared. This compound was then transformed into the enediyne aldehydes 16a,b. Treatment of 16a with cat. amounts of TBAF gave rise to the macrocyclic dynemicin analog 17a. This was c...

For the first time, the Bergman reaction of a naturally occurring enediyne, namely dynemicin A, is fully investigated at the DFT level of theory using the B3LYP hybrid functional and VDZ basis sets. The calculated geometry of dynemicin A agrees well with the X-ray structure of deoxydynemicin A. ...

Dynemicin A rearranged smoothly to dynemicin H, on treatment with aqueous sodium hydrosulfite in dioxane. The same reaction in d8-dioxane gave dynemicin H deuterated specifically at 24- and 27-positions indicating the generation of biradical species at these positions.

Background: Dynemicin A is an exceedingly potent antitumor antibiotic derived from microbial fermentation that cleaves double-stranded B-form DNA in vitro in the presence of activating factors such as NADPH or glutathione. Because of the structural complexity, high reactivity, and scarcity of na...

The new simplified dynemicin analogue 16 was prepared enantio- and diastereoselectively in 17 steps starting from monoacetate (S) 7. It is equipped with a side arm containing a protected primary alcoholic function (`handle'), which can be used for conjugation with DNA-complexing agents or f...

:Dynemicin A 2-1 was first isolated in the mid-1980s from Micromonospora chersina, a soil microorganism collected in the state of Gujarat in India. From a 200 L culture broth, it was possible to obtain 5.7 mg of 2-1 as a violet amorphous solid after extraction and purification. The production of...