Geldanamycin (GM) is a natural antibiotic that binds Hsp90 and induces the degradation of receptor tyrosine kinases, steroid receptors, and Raf. It is a potent inhibitor of cancer cells that overexpress HER-kinases, but its effects on other important proteins may cause significant toxicity and limit its clinical use. We report the synthesis and identification of a GM dimer, GMD-4c, which had se...

Parallel visual pathways in the primate brain known as the dorsal and ventral streams receive retinal inputs mainly through the magnocellular (M) and parvocellular (P) layers of the lateral geniculate nucleus. Inputs from these layers terminate within distinct parts of layer 4C of V1 (visual area 1). Due to the complexity of M- and P-derived neural connectivity in V1 and higher visual areas, th...

Subunit proteins that comprise functional AMPA receptors were localized by immunocytochemical methods in the adult macaque primary visual cortex (V1). GluR1, GluR2/3/4c, and GluR4 immunoreactivity consisted of rich plexuses of punctate profiles scattered throughout the neuropil, in radial arrays, and outlining the membrane of somata and proximal dendrites. Cytoplasmic immunoreactivity was limit...

We cloned a major aliphatic glucosinolate (GSL) gene, BoGSL-ELONG in Brassica oleracea, using the Arabidopsis sequence database. We based our work on an Arabidopsis candidate gene forming part of a gene family coding for isopropyl malate synthetase-like enzymes (IPMS). This gene is presumably responsible for synthesis of GSL possessing side chains consisting of four carbons (4C). The similarity...

Visual inputs from the 2 eyes in most primates activate alternating bands of cortex in layer 4C of primary visual cortex, thereby forming the well-studied ocular dominance columns (ODCs). In addition, the enzymatic reactivity of cytochrome oxidase (CO) reveals "blob" structures within the supragranular layers of ODCs. Here, we present evidence for compartments within ODCs that have not been cle...

Define the Apéry polynomial of degree n by A n (x) = n k=0 n k 2 n + k k 2. We determine p−1 k=0 (−1) k A k (1/4) and p−1 k=0 (−1) k A k (1/16) modulo a prime p > 3. Let b and c be integers and let the generalized trinomial coefficient T n (b, c) be the coefficient of x n in the expansion of (x 2 +bx+c) n. We establish the following new congruence p−1 k=0 T k (b, c) 2 (b 2 − 4c) k ≡ c(b 2 − 4c)...

The formation of methylglyoxal from triose phosphates was studied in dialyzed whole cell homogenates of rat liver. In the cell-free system, methylglyoxal is largely derived from dihydroxyacetone phosphate (DHAP). The addition of the cofactor of glyoxalase activity, reduced glutathione (GSH), to the system inhibits the accumulation of methylglyoxal from DHAP, whereas the absence of GSH promo...

BACKGROUND Chalcones are an important class of natural compounds that have been widely applied as synthons in synthetic organic chemistry and possess diverse and interesting biological properties. METHODS We conducted tests with the synthetic substances 6-quinolinyl N-oxide chalcones 4c and 4e to determine their antifungal activity against several isolates of Paracoccidioides spp. and their a...

The present work describesthe development of highly potent mushroom tyrosinase inhibitor better than the standard kojic acid. Carvacrol derivatives 4a-f and 6a-d having substituted benzoic acid and cinnamic acidresidues were synthesized with the aim to possess potent tyrosinase inhibitory activity.The structures of the synthesized compounds were ascertained by their spectroscopic data (FTIR, 1H...

(+)-Trans-(5R,6R)-5-bromo-6-ethoxy-5-ethyl-5,6-dihydro-2'-deoxyuridine [(5R,6R)-BEEDU], a potential brain-targeted prodrug of 5-ethyl-2'-deoxyuridine (EDU), was synthesized by the regiospecific addition of BrOEt to the 5,6-olefinic bond of EDU. (5R,6R)-BEEDU is more lipophilic (log P = 0.04) than EDU (log P = -1.09). In vitro incubation of (5R,6R)-BEEDU with rat whole blood and brain homogenate...