ABSTRACT
The interleukin-1 receptor associated kinase 4 (IRAK-4) is a member of serine-threonine kinase family, which plays an important role in the regulation of interleukin-1 receptors (IL-1R) and Toll-like receptors (TLRs) related signaling pathways. At present, the IRAK-4 mediated inflammation and related signaling pathways contribute to inflammation, which are also responsible for other autoimmune diseases and drug resistance in cancers. Therefore, targeting IRAK-4 to develop single-target, multi-target inhibitors and proteolysis-targeting chimera (PROTAC) degraders is an important direction for the treatment of inflammation and related diseases. Moreover, insight into the mechanism of action and structural optimization of the reported IRAK-4 inhibitors will provide the new direction to enrich the clinical therapies for inflammation and related diseases. In this comprehensive review, we introduced the recent advance of IRAK-4 inhibitors and degraders with regards to structural optimization, mechanism of action and clinical application that would be helpful for the development of more potent chemical entities against IRAK-4.
Subject(s)
Interleukin-1 Receptor-Associated Kinases , Signal Transduction , Toll-Like Receptors , Humans , Inflammation/drug therapy , Inflammation/metabolism , Interleukin-1 Receptor-Associated Kinases/antagonists & inhibitors , Protein Serine-Threonine Kinases/metabolism , Receptors, Interleukin-1/metabolismABSTRACT
Crop classification is one of the most important agricultural applications of remote sensing. Many studies have investigated crop classification using SAR data, while few studies have focused on the classification of dryland crops by the new Gaofen-3 (GF3) SAR data. In this paper, taking Hengshui city as the study area, the performance of the Freeman-Durden, Sato4, Singh4 and multi-component decomposition methods for dryland crop type classification applications are evaluated, and the potential of full-polarimetric GF3 data in dryland crop type classification are also investigated. The results show that the multi-component decomposition method produces the most accurate overall classifications (88.37%). Compared with the typical polarization decomposition techniques, the accuracy of the classification results using the new decomposition method is improved. In addition, the Freeman method generally yields the third-most accurate results, and the Sato4 (87.40%) and Singh4 (87.34%) methods yield secondary results. The overall classification accuracy of the GF3 data is very positive. These results demonstrate the great promising potential of GF3 SAR data for dryland crop monitoring applications.
Subject(s)
Agriculture , Crops, Agricultural , Agriculture/methods , Spectrum AnalysisABSTRACT
Infections especially tuberculosis caused by various bacteria including mycobacteria result in millions of lives every year, but the control of bacterial infections is challenged by the limitation of effective pharmaceuticals against drug-resistant pathogens. Nitroimidazoles belong to a group of nitroheterocyclic compounds that have broad-spectrum activity against a series of organisms such as mycobacteria, anaerobic Gram-positive and Gram-negative bacteria, and some of them have already been used in clinics or under clinical trials for the treatment of infectious diseases. In this review, we made an overview of the recent advances in nitroimidazole-containing compounds with antibacterial and antitubercular activity in the recent 20 years.
Subject(s)
Anti-Bacterial Agents/pharmacology , Bacterial Infections/drug therapy , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Nitroimidazoles/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Humans , Microbial Sensitivity Tests , Molecular Structure , Nitroimidazoles/chemical synthesis , Nitroimidazoles/chemistryABSTRACT
Plant phenology is the best indicator of terrestrial ecosystem response to climate change and it becomes a hot issue in the study of global change. The forest in northeast of China plays an important part in global forest ecosystem. In this paper, yearly integrated Normalized Difference Vegetation Index (NDVI) of forest vegetation in northeast China was calculated based on Spot Vegetation datasets from 2001-2010, which has been filtered using Savtiky-Galoy method. And then, the yearly integrated NDVI profile was fitted using a logistic model. Two key parameters of forest phenology (start of season, SOS; end of season, EOS) were extracted according to the greatest rate of curvature of fitted cumulative NDVI and the length of forest phenology (length of season, LOS) was also analyzed. The main conclusions of this paper are (1) SOS mainly occurs in the 110th-140th day and EOS in 260th and 290th day. SOS displays a marked delayed from south to north while EOS gradually advances. However, the changes of SOS and EOS in ten years are not obvious. (2) Corresponding to the SOS and EOS, LOS of forest in study area mainly occurs in the 120th-160th day; however, it is spatially heterogeneous. LOS of forest in Greater Khingan Mountains is shorter (about 120-140 day) than forests in Xiao Hinggan Ling and Changbai Mountains (about 160 day). The results in this paper are concordant with records of phenology in situ measurements and previous researches in the same area. It indicates that forest phenophases using method in this paper from Spot Vegetation dataset is feasible.
Subject(s)
Forests , Remote Sensing Technology , Trees , China , Climate Change , SeasonsABSTRACT
Leaf area index (LAI) is an important structural parameter of vegetation canopy, the correct estimation of which has been the focus in the remote sensing community. As a kind of hyperspectral and multi-angle remote sensing data with higher resolution (17 m), PROBA/CHRIS has significant application value in LAI inversion. In the present paper, the analytical two-layer canopy reflectance model (ACRM) was used to simulate a series of reflectances with different LAI values. Based on this, a new vegetation index was built and successfully applied to LAI inversion of PROBA/CHRIS image data. Our results indicated that: compared with the spectral index NDVI and multi-angle index HDS, the new index could make better use of spectrum and multi-angle messages and have a better correlation with LAI of the study area; moreover, the correlation coefficient R2 reached up to 0.734 7. And in order to obtain the figure of LAI distribution of the study area, we used the optimal fit equation between LAI and HDVI to estimate LAI, and the accuracy of the RMSE was 0.619 8.
Subject(s)
Chlorophyll/analysis , Photosynthesis/physiology , Plant Leaves/chemistry , Remote Sensing Technology , Spectrum Analysis/methods , Environmental Monitoring/methods , Models, Theoretical , Satellite Communications , Spectrum Analysis/instrumentationABSTRACT
The title compound, C(12)H(20)N(2)O, was obtained by the reaction of N-(oxiran-2-ylmeth-yl)aniline and propan-2-amine. In the crystal, mol-ecules are linked by O-Hâ¯N and N-Hâ¯O hydrogen bonds into chains parallel to the b axis.
ABSTRACT
In the crystal structure of the title amino alcohol derivitive, C(12)H(19)NO(2), mol-ecules are linked by N-Hâ¯O hydrogen bonds. The mol-ecular structure exhibits an intra-molecular O-Hâ¯N hydrogen bond.
ABSTRACT
In the title compound, C(24)H(34)O(3)S, the dihedral angle between the benzene rings is 84.62â (8)°. In the crystal, inter-molecular C-Hâ¯O hydrogen bonds link mol-ecules into zigzag chains running parallel to the c axis. The C atoms of two isopropyl groups are disordered over two sets of sites with occupancy ratios of 0.858â (9):0.142â (9) and 0.61â (5):0.39â (5).
ABSTRACT
The mol-ecule of the title compound, C(10)H(6)O(4)S(2), has crystallographically imposed twofold symmetry. The dihedral angle formed by the furan rings is 80.90â (8)°. In the crystal, mol-ecules are linked by weak C-Hâ¯O hydrogen bonds into chains running parallel to the a axis [C-S-S-C torsion angle = 82.04 (11)°].
ABSTRACT
In the crystal structure of the title amino alcohol derivative, C(9)H(24)N(2)O(2+)·2Cl(-), the cations and anions are linked by inter-molecular O-Hâ¯Cl and N-Hâ¯Cl hydrogen bonds into a three-dimensional network.
ABSTRACT
The title compound, C(14)H(21)Cl(3)O(9)·2H(2)O, is a disaccharide constructed from a galactose and a fructose. In the mol-ecular structure, the tetra-hydro-furan five-membered ring and tetra-hydro-pyran six-membered ring assume envelope and chair conformations, respectively. An extensive O-Hâ¯O hydrogen-bonding network occurs in the crystal structure.