Participation and Prognostic Impact of Cardiac Rehabilitation After Acute Coronary Syndrome: Big-Data Study of the Korean National Health Insurance Service.

BACKGROUND: To investigate the actual rate and quality of cardiac rehabilitation (CR) participation in South Korea and its short-term impact on clinical outcomes after acute coronary syndrome (ACS). METHODS: Data, including confirmed ACS diagnosis, socio-demographics, comorbidities, clinical outcomes, and CR claim codes, were collected from the Korean National Health Insurance Service claims database and compared between the CR and non-CR groups. RESULTS: Overall, 102,544 patients were included in the study, of which only 5.8% attended CR. Regarding testing, 83.6% of CR patients performed the cardiopulmonary exercise test, but follow-up testing was infrequently performed; in addition, 53.1% of them participated in an electrocardiogram monitoring exercise, but over half participated in only one session. After 1:1 propensity score matching, post-ACS cardiovascular events were significantly lower in the CR group than in the non-CR group. The cumulative 3-year hazard ratio for all-cause death was 0.612 (95% confidence interval [CI], 0.495-0.756), recurrent ACS was 0.92 (95% CI, 0.853-0.993), CR readmission was 0.817 (95% CI, 0.768-0.868), and major adverse cardiovascular events (MACE) was 0.827 (95% CI, 0.781-0.874) in the CR group. CR was associated with a significant dose-response effect on MACE, with a reduction in incidence from 0.854 to 0.711. CONCLUSION: The actual rate of CR participation in South Korea remains low, and participation quality was not outstanding despite National Health Insurance coverage. Nevertheless, the impact of CR on cardiovascular outcomes after ACS was significantly superior. Efforts to increase CR participation should be increased by establishing new CR facilities and strategies to resolve associated barriers.

Chemical inhibition of prometastatic lysyl-tRNA synthetase-laminin receptor interaction.

Lysyl-tRNA synthetase (KRS), a protein synthesis enzyme in the cytosol, relocates to the plasma membrane after a laminin signal and stabilizes a 67-kDa laminin receptor (67LR) that is implicated in cancer metastasis; however, its potential as an antimetastatic therapeutic target has not been explored. We found that the small compound BC-K-YH16899, which binds KRS, impinged on the interaction of KRS with 67LR and suppressed metastasis in three different mouse models. The compound inhibited the KRS-67LR interaction in two ways. First, it directly blocked the association between KRS and 67LR. Second, it suppressed the dynamic movement of the N-terminal extension of KRS and reduced membrane localization of KRS. However, it did not affect the catalytic activity of KRS. Our results suggest that specific modulation of a cancer-related KRS-67LR interaction may offer a way to control metastasis while avoiding the toxicities associated with inhibition of the normal functions of KRS.

Asymmetric synthesis of (-)-swainsonine.

We report a new asymmetric synthetic method for (-)-swainsonine utilizing a chiral oxazoline precursor. The key features in this strategy are the diastereoselective oxazoline formation reaction catalyzed by palladium(0), diasteroselective dihydroxylation, and the stereocontrolled allylation reaction with TiCl(4).

Stereoselective synthesis of (+)-polyoxamic acid based on the synthesis of chiral oxazine.

A concise, stereocontrolled synthesis of (+)-polyoxamic acid was achieved. Starting from trans-oxazoline as a chiral building block, the key step involves diastereoselective oxazine formation catalyzed by palladium(0).

Application of Pd(0)-catalyzed intramolecular oxazine formation to the efficient total synthesis of (-)-anisomycin.

The enantioselective total synthesis of (-)-anisomycin, a potent antibiotic agent, has been achieved. The key steps are a Pd(0)-catalyzed stereoselective intramolecular oxazine formation from d-tyrosine and pyrrolidine formation by catalytic hydrogenation of the oxazine.

A concise synthesis of a promising protein kinase C inhibitor: D-erythro-sphingosine.

In this study, we explored a convenient and concise route for synthesis of D-erythro-sphingosine 1 from commercially available and cheap L-serine. The key steps are simple preparation of amino ketone 5 from Weinreb amide 3 and high diastereoselective reduction of amino ketone 5 to give the natural erythro-(anti-) isomer.

Stereoselective synthesis of L-threo-sphingosine, L-threo-sphinganine, D-threo-sphingosine, and D-threo-sphinganine via oxazoline formation and olefin cross-metathesis; potent protein kinase C inhibitor analogues.

In this study, we explored a convenient and concise route for synthesis of L-threo-sphingosine, D-threo-sphingosine, L-threo-sphinganine and D-threo-sphinganine from commercially available L- or D-serine. The key steps are the simple preparation of trans-oxazoline and intermolecular olefin cross metathesis.

Diastereoselective synthesis of polysubstituted pyrrolidinone as a key intermediate for the anticancer agents by palladium(II)-catalyzed carboxylation.

Palladium(II)-catalyzed carboxylation of chiral olefins 6a-d has been examined under various conditions. In the weak basic condition (K2CO3), 7a-d were obtained in good yields. Alternatively, in the strong basic condition, pyrrolidinones 8a-d were obtained resulting in excellent yields and with high diastereoselectivity.

Diastereoselective synthesis of anti-1,2-aminoalcohol by palladium(II) catalyzed aza-Claisen rearrangement.

In this study, a highly diastereoselective synthesis of anti-1,2-aminoalcohol was explored starting from L-amino acids as chiral sources. The higher yield and diastereoselectivity was shown when the aza-Claisen rearrangement was performed with allylic trichloroacetimidate 6a in the presence of palladium(II) catalyst.