Tripterygium glycosides (TGs) are the most common form of traditional Chinese medicine, known as Tripterygium wilfordii Hook F (TWHF) [...
View Article and Find Full Text PDFPlant Dis
December 2024
Stripe or yellow rust (YR) caused by () is an important foliar disease affecting wheat production globally. Resistant varieties are the most economically and environmentally effective way to manage this disease. The common winter wheat ( L.
View Article and Find Full Text PDFMultitarget HDAC inhibitors capable of simultaneously blocking the BRD4-LIFR-JAK1-STAT3 signaling pathway hold great potential for the treatment of TNBC and other solid tumors. Herein, novel Fedratinib-based multitarget HDAC inhibitors were rationally designed, synthesized, and biologically evaluated, among which compound stood out as a potent HDAC/JAK/BRD4 triple inhibitor. Satisfyingly, compound led to concurrent inhibition of HDACs and the BRD4-LIFR-JAK1-STAT3 signaling pathway, which was validated by hyper-acetylation of histone and α-tubulin, hypo-phosphorylation of STAT3, downregulation of LIFR, MCL-1, and c-Myc in MDA-MB-231 cells.
View Article and Find Full Text PDFTheor Appl Genet
August 2023
We mapped a new race-specific seedling stripe rust resistance gene on wheat chromosome 5BL and a new APR locus QYr.hazu-2BS from CIMMYT wheat line Kfa/2*Kachu. Breeding resistant wheat (Triticum aestivum) varieties is the most economical and efficient way to manage wheat stripe rust, but requires the prior identification of new resistance genes and development of associated molecular markers for marker-assisted selection.
View Article and Find Full Text PDFFront Public Health
September 2022
An isolation strategy was used to control the transmission and rapid spread of COVID-19 in Yunnan. As a result, students were supposed to stay at home and disrupted their outside activities. It led to a detrimental influence on students' mental health.
View Article and Find Full Text PDFIntroduction: KRAS is one of the most important oncology proteins, which can activate multiple downstream signaling pathways. Despite the prevalence of KRAS mutations in approximately 30% of human cancers, it has long been considered to be 'undruggable' due to the lack of recognizable binding pockets.
Areas Covered: This review covers the recent patents (2019-2021) on KRAS inhibitors, which are mostly highlighted in terms of chemical structures, molecular mechanisms of action, pharmacokinetic properties, and potential clinical applications.
ACS Med Chem Lett
December 2021
Herein a novel series of APN and AKT dual inhibitors were derived from the clinical AKT inhibitor AZD5363. It was demonstrated that most compounds exhibited remarkable APN inhibitory activities with the most potent compound (IC = 0.05 ± 0.
View Article and Find Full Text PDFBioorg Chem
November 2021
Histone deacetylase 6 (HDAC6) is a promising therapeutic target for the treatment of cancers, neurodegenerative diseases and autoimmune disorders. Herein a novel series of pyrrolo[2,3-d]pyrimidine-based HDAC inhibitors were designed, synthesized and biologically evaluated, among which compounds 7a, 12a1, and 16a1 exhibited potent inhibitory activities and selectivities against HDAC6. Notably, compared with the well-known HDAC6 inhibitor Tubastatin A, our pyrrolo[2,3-d]pyrimidine-based HDAC6 inhibitors showed superior in vitro antiproliferative activity against human multiple myeloma cell lines RPMI 8226, U266 and MM.
View Article and Find Full Text PDFPlants (Basel)
April 2021
Genetic dissection kernel weight-related traits is of great significance for improving wheat yield potential. As one of the three major yield components of wheat, thousand kernel weight (TKW) was mainly affected by grain length (GL) and grain width (GW). To uncover the key loci for these traits, we carried out a quantitative trait loci (QTL) analysis of an F recombinant inbred lines (RILs) population derived from a cross of Henong 5290 (small grain) and 06Dn23 (big grain) with a 50 K single nucleotide polymorphism (SNP) array.
View Article and Find Full Text PDFThe characterization of leaf rust (caused by ) and stripe rust (caused by f. sp. ) resistance genes is the basis for breeding resistant wheat varieties and managing epidemics of these diseases in wheat.
View Article and Find Full Text PDFMolecules
October 2020
With five histone deacetylase (HDAC) inhibitors approved for cancer treatment, proteolysis-targeting chimeras (PROTACs) for degradation of HDAC are emerging as an alternative strategy for HDAC-targeted therapeutic intervention. Herein, three bestatin-based hydroxamic acids (, and ) were designed, synthesized and biologically evaluated to see if they could work as HDAC degrader by recruiting cellular inhibitor of apoptosis protein 1 (cIAP1) E3 ubiquitin ligase. Among the three compounds, the bestatin-SAHA hybrid exhibited comparable even more potent inhibitory activity against HDAC1, HDAC6 and HDAC8 relative to the approved HDAC inhibitor SAHA.
View Article and Find Full Text PDFFront Plant Sci
September 2017
Seeds per silique (SS), seed weight (SW), and silique length (SL) are important determinant traits of seed yield potential in rapeseed ( L.), and are controlled by naturally occurring quantitative trait loci (QTLs). Mapping QTLs to narrow chromosomal regions provides an effective means of characterizing the genetic basis of these complex traits.
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