Triazole As Potent Anti-Cancer Agent- A Pharmacophoric Scaffold

: Triazole is the main five-membered Nitrogen-containing basic heterocyclic ring system reported for their biological activities and compounds with multiple pharmacophores, which fetch together acquaintance of a target with sympathetic types of the molecule that might interact with the target. In addition, healthy, adaptable, and scalable chemistry must be employed to achieve the task. This characteristic feature of triazole would make a good template for a lead cohort library. The current review article focuses on recent advancements in triazole moiety as an anti-cancer agent with their mechanism pathways of synthesized analogues.

Molecular-replacement phasing using predicted protein structures from AWSEM-Suite

The phase problem in X-ray crystallography arises from the fact that only the intensities, and not the phases, of the diffracting electromagnetic waves are measured directly. Molecular replacement can often estimate the relative phases of reflections starting with those derived from a template structure, which is usually a previously solved structure of a similar protein. The key factor in the success of molecular replacement is finding a good template structure. When no good solved template exists, predicted structures based partially on templates can sometimes be used to generate models for molecular replacement, thereby extending the lower bound of structural and sequence similarity required for successful structure determination. Here, the effectiveness is examined of structures predicted by a state-of-the-art prediction algorithm, the Associative memory, Water-mediated, Structure and Energy Model Suite (AWSEM-Suite), which has been shown to perform well in predicting protein structures in CASP13 when there is no significant sequence similarity to a solved protein or only very low sequence similarity to known templates. The performance of AWSEM-Suite structures in molecular replacement is discussed and the results show that AWSEM-Suite performs well in providing useful phase information, often performing better than I-TASSER-MR and the previous algorithm AWSEM-Template.

ETHNOBOTANICAL SURVEY OF MEDICINAL PLANTS USED IN THE TREATMENT OF CANCER IN DUTSIN-MA LOCAL GOVERNMENT AREA OF KATSINA STATE, NIGERIA

Ethnopharmacological surveys showed that herbal remedies and their products are mostly preferred type of alternative and complementary medicine (ACM) globally. In Dutsin-Ma Local Government Area (LGA) like other places herbal remedies are popularly employed against many ailment including tumor and cancer. Therefore, this study aimed to report and document the ethnobotanical survey of the plants used in the management of tumor and cancer in Dutsin-Ma Local Government Area of Katsina State, Nigeria. Traditional medicine practitioners (TMPs) living within the area of study were cross-examined by employing questionnaires forms and key informant survey. Forty-two (42) different plant species were discovered to be employed against cancer and tumor management. The results obtained showed the parts of plant used for the herbs include; roots (4), bark (10), whole plant (13), seeds (5), fruits (3), stem (1) and leaves (6). The plant families Leguminosae caesalpinoideae and Leguminosae mimosoideae appeared more in the ethno-surveyed plant list though other families are involved. Many of these plants are mix together as storehouses for active compounds which may be good template for cancer and tumor management. The preparation of the remedies include; grinding to powder form then dispersing in either water or milk for drinking, or either mix with shear butter or water and administered on the affected part of the body. The reports showed that the herbal remedies indentified are effective for the treatment of cancer in Dutsin-Ma local government area. Hence, it is imperative for ethnobotanists and chemists to establish the toxicity and efficacy of these

Evolution-inspired design of multicolored photoswitches from a single cyanobacteriochrome scaffold

Cyanobacteriochromes (CBCRs) are small, bistable linear tetrapyrrole (bilin)-binding light sensors which are typically found as modular components in multidomain cyanobacterial signaling proteins. The CBCR family has been categorized into many lineages that roughly correlate with their spectral diversity, but CBCRs possessing a conserved DXCF motif are found in multiple lineages. DXCF CBCRs typically possess two conserved Cys residues: a first Cys that remains ligated to the bilin chromophore and a second Cys found in the DXCF motif. The second Cys often forms a second thioether linkage, providing a mechanism to sense blue and violet light. DXCF CBCRs have been described with blue/green, blue/orange, blue/teal, and green/teal photocycles, and the molecular basis for some of this spectral diversity has been well established. We here characterize AM1_1499g1, an atypical DXCF CBCR that lacks the second cysteine residue and exhibits an orange/green photocycle. Based on prior studies of CBCR spectral tuning, we have successfully engineered seven AM1_1499g1 variants that exhibit robust yellow/teal, green/teal, blue/teal, orange/yellow, yellow/green, green/green, and blue/green photocycles. The remarkable spectral diversity generated by modification of a single CBCR provides a good template for multiplexing synthetic photobiology systems within the same cellular context, thereby bypassing the time-consuming empirical optimization process needed for multiple probes with different protein scaffolds.

Resolving the Mystery of Ring Opening in the Synthesis of Benzo[d][1, 3]oxazin-4-one and Quinazolin-4(3H)-one

Quinazoline is the six-membered heterocyclic ring system reported for its versatile biological activities. This characteristic feature of quinazoline makes it a good template for a lead generation library. Ring opening is one of the major concerns in the synthesis of quinazolin-4(3H)-one that results in diamide formation. Here, alternative fusion strategy is reported, which is a time-saving and costeffective method to overcome the ring opening problem associated with the synthesis of benzo[ d][1,3]oxazin-4-one and quinazolin-4(3H)-one.

A Template Generation and Improvement Approach for Finger-Vein Recognition

Finger-vein biometrics have been extensively investigated for person verification. One of the open issues in finger-vein verification is the lack of robustness against variations of vein patterns due to the changes in physiological and imaging conditions during the acquisition process, which results in large intra-class variations among the finger-vein images captured from the same finger and may degrade the system performance. Despite recent advances in biometric template generation and improvement, current solutions mainly focus on the extrinsic biometrics (e.g., fingerprints, face, signature) instead of intrinsic biometrics (e.g., vein). This paper proposes a weighted least square regression based model to generate and improve enrollment template for finger-vein verification. Driven by the primary target of biometric template generation and improvement, i.e., verification error minimization, we assume that a good template has the smallest intra-class distance with respect to the images from the same class in a verification system. Based on this assumption, the finger-vein template generation is converted into an optimization problem. To improve the performance, the weights associated with similarity are computed for template generation. Then, the enrollment template is generated by solving the optimization problem. Subsequently, a template improvement model is proposed to gradually update vein features in the template. To the best of our knowledge, this is the first proposed work of template generation and improvement for finger-vein biometrics. The experimental results on two public finger-vein databases show that the proposed schemes minimize the intra-class variations among samples and significantly improve finger-vein recognition accuracy.

An unbiased spectral line survey observation toward the low-mass star-forming region L1527

An unbiased spectral line survey toward a solar-type Class 0/I protostar, IRAS 04368+2557, in L1527 has been carried out in the 3 mm band with the Nobeyama 45 m telescope. L1527 is known as a warm carbon-chain chemistry (WCCC) source, which harbors abundant unsaturated organic species such as CnH (n = 3, 4, 5, …) in a warm and dense region near the protostar. The observation covers the frequency range from 80 to 116 GHz. A supplementary observation has also been conducted in the 70 GHz band to observe fundamental transitions of deuterated species. In total, 69 molecular species are identified, among which 27 species are carbon-chain species and their isomers, including their minor isotopologues. This spectral line survey provides us with a good template of the chemical composition of the WCCC source.

Part A Annotated Guide, 2 The Concept of Insider Dealing

This chapter turns to the controversial issue of insider dealing. It offers a general background for the analytical discussion of the single provisions of the Market Abuse Regulation, before taking a broad view at the evolution of the phenomenon and the legal discourse surrounding it. To that end, this chapter adopts an historical perspective, and compares and contrasts different regulatory approaches (in the US and Europe, which offer a good template for most existing regulatory models). The economic and ethical basis invoked to support—or criticize—the prohibition of insider trading is then discussed. Finally, this chapter also discusses a few open questions or regulatory challenges that might be relevant in the next few years.