A novel and selective tyrosine functionalization strategy through SuFEx (sulfur fluoride exchange) chemistry is presented. In this approach, free tyrosine (Tyr) reacts selectively with aryl ...fluorosulfate in the presence of various nucleophilic amino acid residues in bio‐tolerable conditions. Chemoselectivity of this unique SuFEx reaction was confirmed in amino acid, peptide, and protein conjugations. The functions of peptides and proteins were well‐preserved as demonstrated from the Tyr‐specific modification of cell‐penetrating peptide and erythropoietin. This method is well‐suited for residue‐specific modification of native proteins, and thus would expand the versatility of bio‐conjugation in protein chemistry.
A bioconjugation method using a modified SuFEx (sulfur fluoride exchange) reaction of tyrosine and aryl fluorosulfate has been discovered. The reaction was highly chemoselective to tyrosine and non‐destructive to biomolecules.
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BFBNIB, FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SAZU, SBCE, SBMB, UL, UM, UPUK
Transition-metal-free multicomponent reactions involving aryne precursors, secondary amines, and sulfuryl fluoride are reported herein. Zwitterionic intermediates formed from the reaction of arynes ...with amine nucleophiles can capture SO2F2 under mild conditions, offering a novel and practical protocol for the synthesis of 2-dialkyl-, 2-alkylaryl-, or 2-diarylamino-substituted arenesulfonyl fluoride derivatives in good to excellent yields.
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IJS, KILJ, NUK, PNG, UL, UM
ABO incompatibility is no longer considered a contraindication for adult living donor liver transplantation (ALDLT) due to various strategies to overcome the ABO blood group barrier. We report the ...largest single‐center experience of ABO‐incompatible (ABOi) ALDLT in 235 adult patients. The desensitization protocol included a single dose of rituximab and total plasma exchange. In addition, local graft infusion therapy, cyclophosphamide, or splenectomy was used for a certain time period, but these treatments were eventually discontinued due to adverse events. There were three cases (1.3%) of in‐hospital mortality. The cumulative 3‐year graft and patient survival rates were 89.2% and 92.3%, respectively, and were comparable to those of the ABO‐compatible group (n = 1301). Despite promising survival outcomes, 17 patients (7.2%) experienced antibody‐mediated rejection that manifested as diffuse intrahepatic biliary stricture; six cases required retransplantation, and three patients died. ABOi ALDLT is a feasible method for expanding a living liver donor pool, but the efficacy of the desensitization protocol in targeting B cell immunity should be optimized.
This article presents the clinical results of ABO‐incompatible adult living donor liver transplantation in a single institution.
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BFBNIB, FZAB, GEOZS, GIS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, SBMB, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
A very simple synthesis of bimetallic Pd–Pt–Fe3O4 nanoflake-shaped alloy nanoparticles (NPs) for cascade catalytic reactions such as dehydrogenation of ammonia-borane (AB) followed by the reduction ...of nitro compounds (R-NO2) to anilines or alkylamines (R-NH2) in methanol at ambient temperature is described. The Pd–Pt–Fe3O4 NPs were easily prepared via a solution phase hydrothermal method involving the simple one-pot coreduction of potassium tetrachloroplatinate (II) and palladium chloride (II) in polyvinylpyrrolidone with subsequent deposition on commercially available Fe3O4 NPs. The bimetallic Pd–Pt alloy NPs decorated on Fe3O4 NPs provide a unique synergistic effect for the catalysis of cascade dehydrogenation/reduction. Various nitroarene derivatives were reduced to anilines with very specific chemoselectivity in the presence of other reducible functional groups. The bimetallic Pd–Pt–Fe3O4 NPs provide a unique synergistic effect for the catalysis of cascade dehydrogenation/reduction. The nitro reduction proceeded in 5 min with nearly quantitative conversions and yields. Furthermore, the magnetically recyclable nanocatalysts were readily separated using an external magnet and reused up to 250 times without any loss of catalytic activity. A larger scale (10 mmol) reaction was also successfully performed with >99% yield. This efficient, recyclable Pd–Pt–Fe3O4 NPs system can therefore be repetitively utilized for the reduction of various nitro-containing compounds.
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IJS, KILJ, NUK, PNG, UL, UM
Abstract
Thus far, attempts to develop drugs that target corticotropin-releasing hormone receptor 1 (CRF
1
R), a drug target in stress-related therapy, have been unsuccessful. Studies have focused on ...using high-resolution G protein-coupled receptor (GPCR) structures to develop drugs. X-ray free-electron lasers (XFELs), which prevent radiation damage and provide access to high-resolution compositions, have helped accelerate GPCR structural studies. We elucidated the crystal structure of CRF
1
R complexed with a BMK-I-152 antagonist at 2.75 Å using fixed-target serial femtosecond crystallography. The results revealed that two unique hydrogen bonds are present in the hydrogen bond network, the stalk region forms an alpha helix and the hydrophobic network contains an antagonist binding site. We then developed two antagonists—BMK-C203 and BMK-C205—and determined the CRF
1
R/BMK-C203 and CRF
1
R/BMK-C205 complex structures at 2.6 and 2.2 Å, respectively. BMK-C205 exerted significant antidepressant effects in mice and, thus, may be utilized to effectively identify structure-based drugs against CRF
1
R.
Propofol and fentanyl can be administered at the end of sevoflurane anaesthesia to decrease the incidence and severity of emergence agitation (EA), although it has not been determined which agent has ...superior efficacy. The purpose of this study was to compare the effects of propofol and fentanyl on EA.
In this prospective, randomized, double-blind study, 222 children, 18–72 months of age, undergoing sevoflurane anaesthesia were randomly assigned to one of the three groups receiving either propofol 1 mg kg−1 (Group P), fentanyl 1 µg kg−1 (Group F), or saline (Group S) at the end of anaesthesia. The incidence and severity of EA were evaluated with the paediatric anaesthesia emergence delirium (PAED) scale. Time to recovery and incidence of nausea/vomiting were assessed.
The mean PAED score was 4.3 in Group P and 4.9 in Group F (P=0.682), which were lower than 9.0 in Group S (P<0.001). Nausea and vomiting were significantly more frequent in Group F than Groups P and S (adjusted P=0.003 and adjusted P<0.001). Group F had also longer stay in the post-anaesthesia care unit (PACU) than Group S (P<0.001), while Group P did not. However, the differences in PACU stays between the P and F groups were considered clinically insignificant.
Small doses of propofol or fentanyl at the end of sevoflurane anaesthesia comparably reduced EA. Propofol was better than fentanyl due to a lower incidence of nausea and vomiting.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
The large volume of adult living donor liver transplantations (ALDLTs) at our center affords a unique opportunity to examine the impact of acute‐on‐chronic liver failure (ACLF) among high–Model for ...End‐Stage Liver Disease MELD score patients. From February 1998 to March 2010, 1958 cirrhotic recipients were analyzed to study the relationship between MELD scores and ALDLT outcomes. A total of 327 high‐MELD score recipients were categorized into ACLF and non‐ACLF groups, and their outcomes were compared. The 5‐year graft and patient survival in the high‐MELD group were 75.2% and 76.4%, respectively, which were significantly worse than the low and intermediate MELD groups. The presence of ACLF associated with higher MELD scores appeared to be the dominant factor responsible for the inferior results of patients with MELD score of 30–34 points. The 5‐year graft survivals in the ACLF group was 70.5% and in the non‐ACLF group it was 81.0% (p = 0.035). Therefore, ALDLT should be performed as soon as possible in high‐MELD score patients prior to ACLF development. Moreover, ACLF patients should be separately categorized when analyzing the outcomes of ALDLT. ALDLT for ACLF patients should not be discouraged because favorable outcomes can be expected through timely ALDLT and comprehensive management.
While adult living donor liver transplantation should be performed as soon as possible before acute‐on‐chronic liver failure develops, it should not be discouraged for patients with acute‐on‐chronic liver failure since timely transplantation and comprehensive management can bring a favorable outcome.
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BFBNIB, FZAB, GEOZS, GIS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, SBMB, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Exceedingly chemoselective preparation of secondary amines from the cascade reaction of nitro reduction followed by reductive amination of the resulting amine with an aldehyde through the use of ...bimetallic AuPd alloy nanoparticle catalyst is described. We prepared a AuPd alloy nanocatalyst supported on Fe3O4 in gram scale without calcination. One pot synthesis of a number of secondary amines was achieved from a variety of nitroarenes and aryl or alkyl aldehydes under 1 atm of H2 at room temperature. No N‐debenzylation was observed in the case of the reactions involving aryl aldehydes, which is often observed in the reductive amination catalysed by a transition metal catalyst such as palladium. We also accomplished efficient one‐pot synthesis of a number of N‐aryl substituted isoindolinone derivatives from 1‐formylbenzoic acid and several nitroarenes using the same reaction conditions. Furthermore, thanks to the magnetic property of the Fe3O4 support, the AuPd−Fe3O4 NPs could be easily separated and reused up to 20 times without the loss of its catalytic activity.
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BFBNIB, FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SAZU, SBCE, SBMB, UL, UM, UPUK
A new donor (D)–acceptor (A) type naphthalene-based oxazepine-containing fluorophore, OXN-1, is reported, which shows unusually high stability in various environments. Its photophysical properties ...and structural stabilities under harsh conditions are thoroughly examined. The high stability of OXN-1 is explained by quantum chemical calculations. Its exceptional bioimaging capabilities for cells with low cytotoxicity are verified. In addition, its deep tissue imaging ability with two-photon microscopy (TPM) is evaluated.
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IJS, KILJ, NUK, PNG, UL, UM
Background
National Health Insurance (NHI) claim records could provide valuable data for epidemiological studies of asthma in Korea. The aim of this study is to estimate the prevalence of adult ...asthma and to investigate asthma‐related healthcare use and prescription patterns in Korea over 5 years.
Methods
National Health Insurance claim records from January 1, 2006 to December 31, 2010 were analyzed in a retrospective, population‐based study. Outcome measures included asthma prevalence, healthcare use, and prescription patterns over time, by type of hospital, and by medical specialty. Additionally, we assessed differences in healthcare use between newly diagnosed and previously diagnosed patients in 2009.
Results
Over 5 years, the prevalence of asthma among Korean adults increased from 4944 to 5707 cases per 100 000 population (from 3760 to 4445 in men and from 6108 to 6951 in women). Asthma‐related outpatient visits decreased from 4.82 ± 8.02 to 3.44 ± 5.50. Approximately 3% of all patients were hospitalized and 2.4% received asthma‐related emergency treatment each year. Pulmonary function tests were performed in 10–11% of patients an average of 1.3 times per year. Newly diagnosed patients experienced fewer asthma‐related hospitalizations (1.78% vs 4.35%) and emergency department visits (0.80% vs 2.11%) than the previously diagnosed group. Prescriptions of inhaled corticosteroids‐based inhalers were maintained with about 20% of average of all types of hospitals.
Conclusions
The prevalence of asthma in Korea has increased over a recent 5‐year period, and asthma is still suboptimally controlled. Public health strategies are needed to improve the management of asthma in adults.
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BFBNIB, FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SAZU, SBCE, SBMB, UL, UM, UPUK
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