Redox regulation of protein tyrosine phosphatase 1B (PTP1B) involves oxidative conversion of the active site cysteine thiolate into an electrophilic sulfenyl amide residue. Reduction of the sulfenyl amide by biological thiols regenerates the native cysteine residue. Here we explored fundamental chemical reactions that may enable covalent capture of the sulfenyl amide residue in oxidized PTP1B. ...

Abstract The direct arylation of 1,3‐benzodioxole and 2,2‐difluorobenzo[1,3]dioxole with 26 different aryl bromides yields the respective 4‐substitued products in >80% requiring between 0.05–1 mol % Na 2 PdCl 4 , 30 pivalic acid, 1.3 equivs. K CO 3 ca. 250 diethylacetamide per Pd at T =120 °C. nature amide concentration reactants are crucial for optimization reaction conditions. primary role...

Surface active amide-functionalized ionic liquids (ILs) consisting of a long alkyl chain (C6C14) connected to a polar head group (methylimidazolium or pyridinium cation) via an amide functional group were synthesized and their thermal stability, micellar properties and antimicrobial activity in aqueous solution investigated. The incorporation of an amide group increased the thermal stability of...

this study was carried out to determine the protein and carbohydrate molecular structure of sorghum cultivars using fourier transform infrared spectroscopy (ftir) with multivariate molecular spectroscopy analyses. sorghum cultivars included: 1- kimia, 2- sepideh, 3- m2 and 4- m8. protein and carbohydrate molecular functional groups studied included: peak area and height amide i, amide ii, α-hel...

The anti-metabolite chemotherapeutic, gemcitabine is relatively effective for a spectrum of neoplastic conditions that include various forms of leukemia and adenocarcinoma/carcinoma. Rapid systemic deamination of gemcitabine accounts for a brief plasma half-life but its sustained administration is often curtailed by sequelae and chemotherapeutic-resistance. A molecular strategy that diminishes ...

AIMS Delineate the feasibility of simultaneous, dual selective "targeted" chemotherapeutic delivery and determine if this molecular strategy can promote higher levels anti-neoplastic cytotoxicity than if only one covalent immunochemotherapeutic is selectively "targeted" for delivery at a single membrane associated receptor over-expressed by chemotherapeutic-resistant mammary adenocarcinoma. M...

Neutral trialanine (Ala3), which is geometrically constrained to have its peptide bond at Phi and Psi angles of alpha-helix and PPII-like conformers, are studied at the B3LYP/6-31+G(d,p) level of theory to examine vibrational interactions between adjacent peptide units. Delocalization of the amide I, amide II, and amide III3 vibrations are analyzed by calculating their potential energy distribu...

OBJECTIVE Protease-activated receptors (PARs) 1 and 2 are expressed in various blood vessels including rat aorta, modulating vascular tone. We investigated the roles of PAR-1 and PAR-2 in vasomotor modulation in rat superior mesenteric artery. METHODS AND RESULTS Effects of the PAR-2-activating peptide Ser-Leu-Ile-Gly-Arg-Leu-amide (SLIGRL-amide) and the PAR-1-activating peptide Thr-Phe-Leu-L...

In the crystal of the title compound, C(8)H(9)NO(2)S, synthesized by the oxidation of 2-(methyl-sulfan-yl)benzamide using NaOCl with 2,2,6,6-tetra-methyl-piperidyl-1-oxy (TEMPO) as the catalyst, mol-ecules are linked via inter-molecular N-H⋯O(amide) hydrogen bonds, forming centrosymmetric amide-amide dimers which are extended into a two-dimensional lamellar framework parallel to (100) through a...