Structural Activity Relationship Study on Dual PLK1 /BRD4 Inhibitor, BI- 2536

Polo-like kinase 1 (PLK1) and BRD4 are two different therapeutic targets in cancer drug discovery. Recently it has been reported that PLK1 inhibitor, BI-2536, is also a potent inhibitor of BRD4. The simultaneous inhibition of PLK1 and BRD4 by a single drug molecule is interesting because this could lead to the development of effective therapeutic strategy for different types of disease conditions in which PLK1 and BRD4 are implicated. Structural activity relationship studies has been carried out on BI-2536 to generate analogs with enhanced dual inhibitory activity against BRD4 and PLK1 as well as to render the molecule selective to one target over the other. UMB101 and 160 have been found to exhibit enhanced dual inhibitory activity with selectivity fold of less than 30, UMB160 being the most potent dual-kinase bromodomain inhibitor (BRD4 IC50 = 28 nM, PLK1 IC50 = 40 nM). UMB131 was found to be the most selective PLK1 inhibitor over BRD4

Alpine Russet: A Potato Cultivar Having Long Tuber Dormancy Making it Suitable for Processing from Long-term Storage

Abstract Alpine Russet is a later maturing, oblong-long, lightly russeted potato cultivar, notable for having tuber dormancy comparable to Russet Burbank. Processing quality of Alpine Russet from long-term storage is superior to Russet Burbank, with low percent reducing sugars and uniform fry color due to a low percentage difference of sugars between the bud and stem ends. Alpine Russet yields were comparable to Russet Burbank in early harvest trials and were comparable or significantly larger in late harvest trials depending on the location. At two late season locations, Alpine Russet had the largest total and percent No. 1 yields and the largest percent mid-range No. 1 tubers compared to Ranger Russet and Russet Burbank. It has moderately high specific gravity and is resistant to most external and internal defects. Alpine Russet has been evaluated in public and industry trials throughout the Western U.S. for over 15 years. Resumen Alpine Russet es una variedad de papa de madures tardía, larga-oblonga, ligeramente como Russet, notable por tener una dormancia del tubérculo comparable a Russet Burbank. La calidad de procesamiento de Alpine Russet después de un almacenamiento prolongado es superior a Russet Burbank, con bajo porcentaje de azúcares reductores y color uniforme de freído debido a la baja diferencia en porcentaje de azúcares entre la yema apical y la base. Los rendimientos de Alpine Russet fueron comparables a Russet Burbank en ensayos de cosecha temprana y fueron comparables o significativamente mayores en ensayos de cosecha tardía, dependiendo del lugar. En dos lugares de ciclo tardío, Alpine Russet tuvo los mayores rendimientos totales y en porcentaje de No. 1, y el mayor porcentaje de tubérculos de amplitud media No. 1 comparada con Ranger Russet y Russet Burbank. Tiene moderadamente alta gravedad específica y es resistente a la mayoría de los defectos externos e internos. Alpine Russet ha sido evaluada en ensayos públicos y de la industria a lo largo del oeste de los E.U. por más de 15 años