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据统计，2020年我国芝麻进口量达到历史高位，为101.61万 t，全国芝麻消费量保持增长态势，但在市场对芝麻的需求量扩大、市场前景广阔的背景下,广西芝麻的种植面积不增反降。为发挥广西芝麻种植优势，实现广西芝麻产业的高质量发展，详细论述了广西芝麻产业发展现状，分析了广西芝麻产业发展中存在的问题，并提出了发展对策。目前广西芝麻产业种植规模趋于稳定、种植品种类型多样、种植效益稳中有升、龙头企业引领市场,但仍然存在高产稳产品种不足,机械化生产能力薄弱,加工技术发展缓慢,产品销售渠道狭窄等问题。可通过加强良种技术攻关，提升器械应用水平，提高加工技术投入，拓宽产业市场渠道等对策，推动广西芝麻产业健康发展。 According to statistics，the import volume of sesame in China reached a historical high in 2020, with 1 016 100 t, and the national sesame consumption maintained a growth trend, but in the context of expanding market demand for sesame seeds and broad market prospects, the planting area of sesame in Guangxi decreased rather than increased. In order to give full play to the advantages of Guangxi′ sesame planting and realize the high-quality development of Guangxi′ sesame industry, the development status of Guangxi′ sesame industry was discussed in detail, the problems existing in the development of Guangxi′ sesame industry were analyzed, and countermeasures for development of Guangxi′ sesame industry were proposed. At present, the planting scale of Guangxi′ sesame industry tends to be stable, the types of planting varieties are diversified, the planting benefits are steadily rising, and leading enterprises lead the market, but there are still problems such as insufficient high-yielding and stable-yielding varieties, weak mechanized production capacity, slow development of processing technology, and narrow product sales channels. The healthy development of Guangxi′ sesame industry can be promoted by strengthening the technical research of improved variery, improving the application level of instruments,improving the investment in processing technology and broadening the market channels of the industry.

Reversible covalent electrophiles with the advantages of both reversible and covalent interactions receive much attention in the fields of chemical biology and medicinal chemistry. Here, we report two electron-deficient olefins activated by amide and ester, amide-substituted acrylamide and methyl ester-substituted acrylamide, targeting thiols in a reversible covalent manner. [ABSTRACT FROM AUTHOR]

Primary pulmonary salivary gland tumors (PSGT) constitute a rare subtype of non-small cell lung cancer (NSCLC). Currently, no established treatment guidelines exist for advanced PSGT. The efficacy of platinum-based chemotherapy for PSGT within the context of NSCLC remains uncertain. Therefore, we retrospectively collected 37 PSGT patients who underwent first-line platinum-based chemotherapy from 2010 to 2023. Survival analysis, employing the Kaplan–Meier method, and group comparisons via the log rank test were conducted. Our results show that first-line platinum-based chemotherapy demonstrates favorable efficacy and manageable safety in advanced PSGT, with the combination of Paclitaxel + Platinum emerging as a preferred option. [ABSTRACT FROM AUTHOR]

Background: The efficacy of definite for non‐small‐cell lung cancer (NSCLC) with uncommon epidermal growth factor receptor (EGFR) mutations has been preliminarily demonstrated. However, there is a paucity of data with which to compare the efficacy and safety of second‐ and third‐generation TKIs in patients with NSCLC carrying uncommon EGFR mutations. Methods: We compared the efficacy and safety of second‐ and third‐generation TKIs in all NSCLC patients in whom next‐generation sequencing confirmed uncommon EGFR mutations, including G719X, S768I, and L861Q. The parameters analyzed included the objective response rate (ORR), disease control rate (DCR), progression‐free survival (PFS), and overall survival (OS). The rate of treatment‐related adverse events (AEs) reflected the safety of these TKIs. Results: Eighty‐four NSCLC patients with uncommon EGFR mutations were enrolled between April 2016 and May 2022 at Zhejiang Cancer Hospital, including 63 treated with second‐generation TKIs and 21 treated with third‐generation TKIs. The ORR for all patients receiving TKIs was 47.6%, and the DCR was 86.9%. The median PFS for NSCLC patients with uncommon EGFR mutations receiving TKIs was 11.9 months and OS was 30.6 months. There was no significant difference in PFS after treatment with second‐ or third‐generation TKIs (13.3 vs. 11.0 months, respectively, P = 0.910) or in OS (30.6 vs. 24.6 months, respectively P = 0.623). The third‐generation TKIs showed no severe toxicity. Conclusions: The efficacy of second‐ and third‐generation TKIs for NSCLC with uncommon EGFR mutations does not differ, and so can be used to treat NSCLC patients with these mutations. [ABSTRACT FROM AUTHOR]

Advances in targeted covalent inhibitors (TCIs) have been made by using lysine-reactive chemistries. Few aminophiles possessing balanced reactivity/stability for the development of cell-active TCIs are however available. We report herein lysine-reactive activity-based probes (ABPs; 2-14) based on the chemistry of aryl fluorosulfates (ArOSO 2 F) capable of global reactivity profiling of the catalytic lysine in human kinome from mammalian cells. We concurrently developed reversible covalent ABPs (15/16) by installing salicylaldehydes (SA) onto a promiscuous kinase-binding scaffold. The stability and amine reactivity of these probes exhibited a broad range of tunability. X-ray crystallography and mass spectrometry (MS) confirmed the successful covalent engagement between ArOSO 2 F on 9 and the catalytic lysine of SRC kinase. Chemoproteomic studies enabled the profiling of >300 endogenous kinases, thus providing a global landscape of ligandable catalytic lysines of the kinome. By further introducing these aminophiles into VX-680 (a noncovalent inhibitor of AURKA kinase), we generated novel lysine-reactive TCIs that exhibited excellent in vitro potency and reasonable cellular activities with prolonged residence time. Our work serves as a general guide for the development of lysine-reactive ArOSO 2 F-based TCIs., (© 2024 Wiley-VCH GmbH.)

Despite recent interests in developing lysine-targeting covalent inhibitors, no general approach is available to create such compounds. We report herein a general approach to develop cell-active covalent inhibitors of protein kinases by targeting the conserved catalytic lysine residue using key SuFEx and salicylaldehyde-based imine chemistries. We validated the strategy by successfully developing (irreversible and reversible) covalent inhibitors against BCR-ABL kinase. Our lead compounds showed high levels of selectivity in biochemical assays, exhibited nanomolar potency against endogenous ABL kinase in cellular assays, and were active against most drug-resistant ABL mutations. Among them, the salicylaldehyde-containing A5 is the first-ever reversible covalent ABL inhibitor that possessed time-dependent ABL inhibition with prolonged residence time and few cellular off-targets in K562 cells. Bioinformatics further suggested the generality of our strategy against the human kinome., (© 2022 Wiley-VCH GmbH.)