37804051
Development of tripeptidyl farnesyltransferase inhibitors.
The first example of tripeptide inhibitors of farnesyltransferase with sub-micromolar inhibition activity was developed based on the fact that CVFM is not a substrate for farnesyltransferase.
26762430
Angularly fused triquinanes from linear substrates through trimethylenemethane diyl [2 + 3] cycloaddition reaction.
Angularly fused triquinanes were synthesized from linear dienes and phenyl(propynyl)iodonium salt through trimethylenemethane (TMM) diyl mediated [2 + 3] cycloaddition reaction. TMM diyl intermediates were obtained from alkylidene carbenes generated from reactions of alkynyliodonium salts with nucleophiles.
40137340
Structure-activity relationship studies of the chromosome segregation inhibitor, Incentrom A.
A series of Incentrom A analogs that inhibit the chromosome segregation process in yeast were synthesized and tested for their effects on chromosome stability and cell proliferation. Pharmacophore and structure-activity relationship of Incentrom A for the anti-yeast activity were established.
41789429
A stereoselective enyne cross metathesis.
[reaction: see text] Intermolecular enyne metathesis reaction of alkynes with olefins catalyzed by second-generation Grubbs catalyst (1) proceeded stereoselectively under ethylene atmosphere to produce 1,3-disubstituted butadienes with E stereochemistry.
1036246
A Facile Construction of the Quadranoid Skeleton: Application to the Total Synthesis of (+/-)-Suberosenone.
A tandem free radical cyclization-rearrangement sequence was designed and executed to produce tricyclo[4.3.2.0(1,5)]undecane 7 from cyclopentene 6A in a single operation. The total synthesis of suberosenone was accomplished from 7.
41880483
One-pot three-component tandem metathesis/Diels-Alder reaction.
[reaction: see text] A tandem enyne, diene-ene metathesis reaction followed by Diels-Alder reaction accomplished a stereoselective three-component reaction protocol with four stereocenters.
32247792
Effects of 9-cis-retinoic acid on the insulin-like growth factor axis in former smokers.
PURPOSE
Insulin-like growth factor (IGF) axis has been associated with the risk of lung cancer. 9-cis-retinoic acid (9-cis-RA) has shown potential chemopreventive activities in former smokers. This study was designed to evaluate the effects of 9-cis-RA on IGF axis in former smokers to identify any benefit the retinoid may have in preventing lung cancer.


PATIENTS AND METHODS
Serum concentrations of IGF-I, IGF binding protein (IGFBP)-3, and their molar ratio (IGF-I/IGFBP-3) were measured with radioimmunoassay kits in stored blood samples from the participants of an original chemoprevention trial. The participants had ceased smoking for at least 12 months and were randomly assigned to receive 3 months of daily oral 9-cis-RA (100 mg) or placebo. All statistical tests were two-sided.


RESULTS
A total of 111 samples from the study's baseline and 84 samples from the 3 months treatment were analyzed. The serum concentrations of IGF-I and IGF-I/IGFBP-3 at baseline were significantly lower in female than in male participants. After 3 months of treatment, the serum level of IGF-I and IGF-I/IGFBP-3 were significantly lower in the 9-cis-RA group than in the placebo group (P = .03 and P < .01, respectively), but the IGFBP-3 level was significantly higher (P = .03).


CONCLUSION
9-cis-RA treatment modulated the IGF axis in former smokers, suggesting that the IGF axis is a potential target for the chemopreventive activities of 9-cis-RA and that the serum concentrations of IGF, IGFBP-3, and IGF-I/IGFBP-3 could serve as surrogate end point biomarkers of 9-cis-RA treatment.
11700956
Cardio–renal protection with aliskiren, a direct renin inhibitor, in the ASPIRE HIGHER program
Aliskiren is the first in a new class of orally effective direct renin inhibitors. Initial results of clinical efficacy studies have demonstrated at least equivalent or superior blood pressure-lowering efficacy when compared with existing drugs, and a favorable side-effect profile either as monotherapy or as a component of combination therapy. This report aims to introduce and provide a critical appraisal of the initial results of the ASPIRE HIGHER program, evaluating the potential cardio–renal protective effects of aliskiren.
43055872
Modeling T Cell Proliferation and Death in Vitro Based on Labeling Data: Generalizations of the Smith–Martin Cell Cycle Model
Abstract
The fluorescent dye carboxyfluorescein diacetate succinimidyl ester (CFSE) classifies proliferating cell populations into groups according to the number of divisions each cell has undergone (i.e., its division class). The pulse labeling of cells with radioactive thymidine provides a means to determine the distribution of times of entry into the first cell division. We derive in analytic form the number of cells in each division class as a function of time based on the distribution of times to the first division. Choosing the distribution of time to the first division to fit thymidine labeling data for T cells stimulated in vitro under different concentrations of IL-2, we fit CFSE data to determine the dependence of T cell kinetic parameters on the concentration of IL-2. As the concentration of IL-2 increases, the average cell cycle time is shortened, the death rate of cells is decreased, and a higher fraction of cells is recruited into division. We also find that if the average cell cycle time increases with division class then the qualify of our fit to the data improves.

5387554
Amicrobial Pustulosis-Like Rash in a Patient with Crohn’s Disease under Anti-TNF-Alpha Blocker
Amicrobial pustulosis of the folds (APF) is a recently described entity characterized by relapsing pustular lesions predominantly involving the cutaneous flexures and scalp. This disease typically occurs in association with systemic lupus erythematosus and a variety of other autoimmune diseases. We here describe an APF-like pustular eruption predominantly affecting the scalp, face and trunk, occurring during long-term infliximab treatment for Crohn’s disease. Immunohistochemical staining of skin biopsy specimens for myxovirus resistance protein A, a marker for type 1 interferon-inducible proteins, showed increased staining in the epidermis and dermal mononuclear inflammatory infiltrate. Our observation further extends the spectrum of cutaneous adverse reactions potentially related to anti-tumor necrosis factor-α, the clinical context in which APF can occur as well as its clinical presentations.
7785683
Anterior clinoid process and optic strut in Koreans.
The anterior clinoid process and the optic strut are often removed during operation on the anterior part of the cavernous sinus. Therefore it is important for neurosurgeons to verify their dimensions and variations. The purpose of this study was to investigate the dimension and the variation of the anterior clinoid process and to describe the locational variation of the optic strut. Seventy-three skulls of Korean adults were used. The average length, basal width and thickness of the anterior clinoid process were 9.18 +/- 1.55, 9.63 +/- 1.49 and 5.32 +/- 1.07 mm, respectively. The average thickness of the optic strut was 2.9 +/- 1.15 mm and it was commonly attached to anterior two-fifths of the anterior clinoid process. The complete caroticoclinoid canal was observed in 4.1%, however it was incomplete in 11.6%. The incidence of a caroticoclinoid canal in Koreans was relatively low compared with other races.