Site-Selective Antibody-Drug Conjugation by a Proximity-Driven S to N Acyl Transfer Reaction on a Therapeutic Antibody.

Immunoglobulin Gs (IgGs) contain many Lys and Cys residues, which results in an unwanted complex product mixture with conventional drug conjugation methods. We selectively acylated the ε-NH of K248 on trastuzumab using an IgG Fc-binding peptide (FcBP) equipped with a 5-norbornene-2-carboxylic acid thioester (AbClick-1). AbClick-1 locates its thioester close to the ε-NH of K248 while binding to trastuzumab.

Polyphyllin D Shows Anticancer Effect through a Selective Inhibition of Src Homology Region 2-Containing Protein Tyrosine Phosphatase-2 (SHP2).

Natural products have continued to offer tremendous opportunities for drug development, as they have long been used in traditional medicinal systems. SHP2 has served as an anticancer target. To identify novel SHP2 inhibitors with potential anticancer activity, we screened a library containing 658 natural products.

Photoconjugation of an Fc-Specific Peptide Enables Efficient DAR 2 Antibody-Drug Conjugate Formation.

Antibody-drug conjugates (ADCs) in current clinical usage have been constructed via the nonspecific conjugation of drugs to antibodies, rendering the manufacturing processes difficult. In this study, a high-affinity IgG Fc-binding peptide equipped with a photoreactive amino acid was developed and successfully conjugated to Glu-382 of trastuzumab in a site-specific manner. The resulting conjugate was employed to generate a DAR 2 ADC product using click chemistry.

Identification of chebulinic acid as a dual targeting inhibitor of protein tyrosine phosphatases relevant to insulin resistance.

Natural products as antidiabetic agents have been shown to stimulate insulin signaling via the inhibition of the protein tyrosine phosphatases relevant to insulin resistance. Previously, we have identified PTPN9 and DUSP9 as potential antidiabetic targets and a multi-targeting natural product thereof. In this study, knockdown of PTPN11 increased AMPK phosphorylation in differentiated C2C12 muscle cells by 3.

A relationship between personality and empathy in teenagers' school sports club participation.

This study aims to identify the relation between students' participation in sports club activities and personality and sympathy based on the findings obtained from personalty and sympathy study and understand what the interrelational characteristics are. This study investigated a total of 408 individuals (male, 58.3%; female, 41.

Label-Free Detection of Protein Tyrosine Phosphatase 1B (PTP1B) by Using a Rationally Designed Förster Resonance Energy Transfer (FRET) Probe.

A highly selective detection method of native protein tyrosine phosphatase 1B (PTP1B) is described using a target specific probe equipped with 1-naphthylamine (λ =330 nm, λ =445 nm). Irradiation of a mixture of PTP1B and Probe 1 with ultraviolet light of 280 nm (corresponding to PTP1B excitation maximum) resulted in significant fluorescence increase at 445 nm, following FRET characteristics. This phenomenon does not occur with other closely related phosphatases or cellular abundant alkaline phosphatase (APP).

Association between Cigarette Smoking Frequency and Health Factors among Korean Adults.

Background: Recently, there has been a trend that cigarette smoking rate in Asian and Africa adults has increased while the age group to start smoking has decreased gradually. This study aimed to investigate the relationships between lifetime smoking and hypertension, diabetes, obesity, waist measure, fasting blood pressure and food consumption, in order to look into health status depending on smoking status in Koreans.

Methods: Totally, 1075 men and 697 women with no disease participated in this study, in which one-way ANOVA was conducted by using SPSS version 18.

Ginkgolic acid as a dual-targeting inhibitor for protein tyrosine phosphatases relevant to insulin resistance.

Several protein tyrosine phosphatases (PTPs) that disrupt the insulin-signaling pathway were investigated by siRNAs to identify potential antidiabetic targets. Individual knockdown of PTPN9 and DUSP9 in 3T3-L1 preadipocytes increased AMPK phosphorylation, respectively, and furthermore, concurrent knockdown of both PTPN9 and DUSP9 synergistically increased AMPK phosphorylation. Next, 658 natural products were screened to identify dual inhibitors of both PTPN9 and DUSP9.

A study on macronutrient self-selection after acute aerobic exercise in college females.

[Purpose] This study was conducted to determine whether acute aerobic exercise (climbing) is associated with changes in the dietary intake pattern. [Subjects and Methods] Food intake and physical activity data for 15 female college students were sampled for 3 days and categorized according to routine activity or high-intensity activity such as hiking. Nutrient intake based on the data was analyzed using a nutrition program.

Electromyography comparison of normal chair-desk system and assistant chair-desk system on fatigue.

[Purpose] This study was designed to test the effects of the Assistant Chair-Desk System (ACDS), which can reduce the forward tilt of the neck and trunk and the level of fatigue during long lasting study in the sitting position. [Subjects] Fourteen middle school students and 14 college students of mixed gender participated in this study. [Methods] Fatigue level, the trapezius muscle, and the forward tilt angle of the head and trunk as well as distance factors were assessed before after using a normal chair-desk system (NCDS) and the ACDS for 120 minutes.

On school violence in Korean middle school, prevention and reaction measures.

This study is aiming to explore the practical and realistic measure in more variable way, which enables us to manage the problems about school violence we are currently facing as well as to overcome limitations in the current situation where we react only with punishments, mainly in the form of the law enforcement, supported by the police. This study was conducted on male and female students (n= 424) and teachers (n= 136) attending at the seven middle schools located in Seoul. The frequency analysis, one way ANOVA F-test, t -test, the multiple regression analysis were applied.