Molecular Modification Research Articles

A multiaxial molecular ferroelectric with record high TC designed by intermolecular interaction modulation.

Through precise and ingenious molecular modification, we successfully obtained a multiaxial ferroelectric, [FEtDabco]ZnI3 (N-fluoroethyl-N'-ZnI3-1,4-diazabicyclo[2.2.2]octonium), with a record high Tc (540 K) among molecular ferroelectrics, which is promising for application under extreme thermal conditions.

Molecular Manipulation of the miR399/PHO2 Expression Module Alters the Salt Stress Response of Arabidopsis thaliana.

In Arabidopsis thaliana (Arabidopsis), the microRNA399 (miR399)/PHOSPHATE2 (PHO2) expression module is central to the response of Arabidopsis to phosphate (PO4) stress. In addition, miR399 has been demonstrated to also alter in abundance in response to salt stress. We therefore used a molecular modification approach to alter miR399 abundance to investigate the requirement of altered miR399 abundance in Arabidopsis in response to salt stress. The generated transformant lines, MIM399 and MIR399 plants, with reduced and elevated miR399 abundance respectively, displayed differences in their phenotypic and physiological response to those of wild-type Arabidopsis (Col-0) plants following exposure to a 7-day period of salt stress. However, at the molecular level, elevated miR399 abundance, and therefore, altered PHO2 target gene expression in salt-stressed Col-0, MIM399 and MIR399 plants, resulted in significant changes to the expression level of the two PO4 transporter genes, PHOSPHATE TRANSPORTER1;4 (PHT1;4) and PHT1;9. Elevated PHT1;4 and PHT1;9 PO4 transporter levels in salt stressed Arabidopsis would enhance PO4 translocation from the root to the shoot tissue which would supply additional levels of this precious cellular resource that could be utilized by the aerial tissues of salt stressed Arabidopsis to either maintain essential biological processes or to mount an adaptive response to salt stress.

Gold nanoring core-shell satellites with abundant built-in hotspots and great analyte penetration: An immunoassay platform for the SERS/fluorescence-based detection of carcinoembryonic antigen

We designed an ingenious plasmonic core-shell-satellite nanostructure (HPGNPs@mSiO2-AuNR) including a hollow porous gold nanoshell (HPGNP) core, a protective silica shell with mesoporous (mSiO2) interlayer, and a high level of gold nanoring (AuNR) satellite coverage by in situ etching. The HPGNP core modified with 4-mercaptobenzoic acid (4-MBA) possessed relatively strong local-field enhancement. The mSiO2 coating acted as a continuous interior nanogap and protective shell, and the variable external satellites in the morphology had tunable optical responses and designed “hotspot” regions. Specifically, AuNR satellites exhibited superior plasmonic properties, intense core-satellite plasmon coupling with the HPGNP core, and favorable biocompatibility. Meanwhile, the nanoassemblies had larger surface-to-volume ratios for molecular modification and were penetrable for analyte. With their abundant built-in hotspots and less hindrance for analyte penetration into the hollow interior, the labeled nanoassemblies were successfully used in SERS/fluorescence sensing system for carcinoembryonic antigen (CEA) detection. These immunoprobes with high SERS activity could be used in SERS-based immunoassay for CEA detection with a linear response ranging from 1 pg/mL to 1000 pg/mL. CEA detection in the fluorescence sensing system showed that the fluorescence quenching efficiency gradually decreased as the CEA level increased, with a linear response of 0.5–400 pg/mL. This SERS/fluorescence-based immunoassay had the same CEA detection limit of 0.1 pg/mL. The fine-engineered penetrable nanoassemblies with Au ring satellites can provide an insight into the rational and optimal design of multifunctional nanostructures. They can also broaden the field of vision for the design of multifunctional sensing probes in biochemical detection.

Alphastatin-C a new inhibitor of endothelial cell activation is a pro-arteriogenic agent in vivo and retards B16-F10 melanoma growth in a preclinical model.

Most characterized angiogenic modulators are proteolytic fragments of structural plasma and/or matrix components. Herein, we have identified a novel anti-angiogenic peptide generated by the in vitro hydrolysis of the C-terminal moiety of the fibrinogen alpha chain, produced by the snake venom metalloprotease bothropasin (SVMP), a hemorrhagic proteinase in Bothrops jararaca venom. The 14-amino acids peptide (alphastatin-C) is a potent antagonist of basic fibroblast growth factor, induced endothelial cell (HUVEC-CS) proliferation, migration and capillary tube formation in matrigel. It also inhibits cell adhesion to fibronectin. The basis of the antagonism between bFGF and alphastatin-C is elucidated by the inhibition of various bFGF induced signaling pathways and their molecular components modification, whenever the combination of the stimuli is provided, in comparison to the treatment with bFGF only. To corroborate to the potential therapeutic use of alphastatin-C, we have chosen to perform in vivo assays in two distinct angiogenic settings. In chick model, alphastatin-C inhibits chorioallantoic membrane angiogenesis. In mouse, it efficiently reduces tumor number and volume in a melanoma model, due to the impairment of tumor neovascularization in treated mice. In contrast, we show that the alphastatin-C peptide induces arteriogenesis, increasing pial collateral density in neonate mice. alphastatin-C is an efficient new antiangiogenic FGF-associated agent in vitro, it is an inhibitor of embryonic and tumor vascularization in vivo while, it is an arteriogenic agent. The results also suggest that SVMPs can be used as in vitro biochemical tools to process plasma and/or matrix macromolecular components unraveling new angiostatic peptides.

An overview of pharmacological activities of acridine derivatives

The derivatives of acridine can be served as a lead molecule of an antibacterial, anti-viral antiprotozoal, anti-viral, antitubercular, anti-fungal, anti-malarial and anti-cancer agents. Even though the usage of acridine becomes limited due to its side effects, so many potent and safe compounds can be derived through molecular modification in the acridine ring. Since the resistance of pathogens and tumour cells has become more common nowadays, it necessitates the search of new drug candidates. Since the treatment and management of Alzheimer's disease is such a complicated and proper drug regimen is not designed so far, The cholinesterase activity of acridines can be used to derive novel compounds from treating Alzheimer's disease. The mosquito larvicidal activity of acridines is considered as an advantage as vector control to reduce the spreading rate of malaria. Unfortunately, the versatility of the acridine molecule is not entirely explored still. If new approaches may overcome the drawbacks of the acridines such as resistance of pathogens and tumour cells in synthesis and formulation acridine analogues will become a useful drug candidate for the treatment of diseases mentioned above. So this article aims to seek the attention of researchers in the acridine to utilise it’s a wide range of biological activities in the development of novel drug molecules for the various diseases in the future.

Modified organophosphorus fire retardant with low toxicity/high flame retardancy using the pharmacophore model associated with Mamdani fuzzy inference approach.

The bi-directional selective low toxicity/high flame retardancy organophosphorus fire retardants (OPFRs) derivatives were designed by a comprehensive effect 3D quantitative structure-activity relationship (QSAR) pharmacophore model, and the toxicity and flame retardancy mechanism of OPFR derivatives were explored. The 3D-QSAR comprehensive pharmacophore model was constructed using the toxicity/flame retardancy comprehensive evaluation values of OPFRs for molecular modifications, which were obtained by the Mamdani fuzzy inference approach. The environment-friendly OPFR derivatives (CDPP-F, CDPP-NO2, TPHP-F, TDCIPP-CH2CH3, and TDCIPP-Br) with high flame retardancy showed significantly reduced multi-toxicity effects (biotoxicity, reproductive toxicity, and neurotoxicity) in the comprehensive model. The spatial overlapping volumes of the toxicity/flame retardancy comprehensive effect model with the toxic effect and with flame retardant effect were 1 : 1. The trend (1 : 1) was similar to the degree of improvement of toxicity and flame retardancy of the OPFR derivatives. The toxicity and flame retardancy were decreased by more than 50%. This indicated that the spatial overlapping volumes in the comprehensive model with the toxic and flame retardant mono-models have significant effects. Based on the 2D-QSAR model, molecular docking, and density functional theory, it was found that, in molecular modification, the introduction of electronegative groups to improve the electronic parameters (q+) can reduce the toxicity of OPFRs. An increase in the bond length and bond angle of the molecular side chain increased the steric parameter (MR) that improved the molecular flame retardancy of OPFRs.

Directed evolution of a D-mandelate dehydrogenase toward D-o-chloromandelic acid and insight into the molecular basis for its catalytic performance

Halogenated mandelate and its derivatives are important scaffolds in chemical industry. However, the natural D-mandelate dehydrogenase (DMDH) showed relatively low catalytic activity toward D-o-chloromandelic acid, which largely limits the efficiency of dehydrogenation processes. To improve catalytic activity of Lactobacillus brevis D-mandelate dehydrogenase (LbDMDH) toward halogenated substrate, a D-mandelate dehydrogenase mutant LbDMDHN253S with higher catalytic activity toward D-o-chloromandelic acid was successfully obtained by directed evolution, which was about 29 times of LbDMDH. In addition, the temperature optimum of LbDMDHN253S is 50 °C, and closer to the optimal growth temperature for Escherichia coli, indicating that it may be more advantageous in whole cell catalysis using living cells as catalysts. Meanwhile, the Kcat value toward D-o-chloromandelic acid of LbDMDHN253S is 2.08 s−1, which is significantly higher than the one (0.09 s−1) of LbDMDH, indicating that LbDMDHN253S displayed higher catalytic efficiency toward D-o-chloromandelic acid. Then, we preliminarily explained the molecular basis for its catalytic performance by in silico design methods. All of these results established a solid foundation for molecular modification of DMDHs and the other industrial enzymes.

Organic Molecule Modified Phosphotungstate with Helical Structure for Electrochemical Detection of Dopamine

To overcome the water solubility and aggregation of heteropoly acids (HPAs), and to promote its application in the electrochemical biosensors, organic molecular modification strategy was employed by simple hydrothermal synthesis. Herein, an unprecedented phosphotungstate (PTA)‐based three‐dimensional supramolecular framework with helical structure, [(bix)2(H3PW12O40)·H2O] [PTA‐bix, bix = 1,3‐bis(imidazol‐1‐ylmethyl) benzene], was synthesized and characterized. And the PTA‐bix modified glassy carbon electrode shows the high sensitivity and catalytic activity for detecting the neurotransmitter dopamine (DA) with the linear detection range from 1 μM to 100 μM, and the detection limit of differential pulse voltammetry (DPV) is 0.85 μM. The concept behinds the new architecture to modify electrodes should promote the further development of HPA hybrid crystal material‐based biosensors.

Evaluation of green synthetic depressants for sulfide flotation: Synthesis, characterization and floatation performance to pyrite and chalcopyrite

Native starch has a complex molecular structure that limits its ability as a selective depressant in sulfide flotation separations. This research study was conducted primarily to develop a series of starch-based molecules of different molecular weights with the aim of obtaining the most selective depressant of pyrite in chalcopyrite flotation. Five low molecular weight molecules were produced by the oxidative treatment of starch using H2O2 as the oxidant and FeSO4·7H2O as the catalyst. Oxidation treatment resulted in molecular modification of starch, producing low molecular weight molecules of grafted polar groups with increased reaction time. The molecules developed were investigated by microflotation to obtain the most selective and effective depressant for pyrite than chalcopyrite. The optimal and most selective depressant was named tricarboxystarch (sodium salt), also known as TCSS, based on the results of characterization measurements. The inhibitory effect of tricarboxystarch on pyrite was far more selective and effective than native starch. Good selective separation between pyrite and chalcopyrite was achieved by adding tricarboxystarch to a low pH solution. Tricarboxystarch contained three –COOH and several –OH groups in the skeleton, providing excellent depression of pyrite. This study is a basic research that sheds new light on the development and optimization of organic polymers for flotation technology.

Storage stability of fish gelatin films by molecular modification or direct incorporation of oxidized linoleic acid: Comparative studies

Changes in properties of films fabricated with oxidized linoleic acid (OLA)-modified gelatin (OMG) and those prepared with OLA-added gelatin (OAG) were investigated during storage for 8 weeks, in comparison to the control film (without modification or OLA addition). OMG and OAG films showed lower water-vapor permeability (WVP) throughout 8 weeks of storage (p < 0.05) compared to control gelatin films. Additionally, a slight decrease in WVP was found in control and OMG films with an increase in storage time. Regarding mechanical properties, tensile strength (TS) and elastic modulus (EM) increased during storage, while elongation at break (EAB) decreased (p < 0.05). During storage, OMG and control films showed similar appearances, with slight changes in yellowness and transparency; however, OAG films showed a marked increase in yellowness, opacity and rancid smell at week 8 of storage. These changes were associated with the increase in lipid oxidation as ascertained by significantly higher thiobarbituric acid reactive substances (TBARS) and volatile compounds observed for OAG films during storage up to 8 weeks. As a consequence, transition temperatures, including glass transition, melting and degradation temperatures of films stored at week 8 were higher than those at week 0. In addition, control and OMG films showed greater thermal stability than OAG films at week 0 and 8. Therefore, the addition of OLA had a relevant impact on the properties of fish gelatin films during extended storage, depending on the method used for OLA incorporation.

Transcriptome based functional identification and application of regulator AbrB on alkaline protease synthesis in Bacillus licheniformis 2709

Bacillus licheniformis 2709 is the major alkaline protease producer, which has great potential value of industrial application, but how the high-producer can be regulated rationally is still not completely understood. It's meaningful to understand the metabolic processes during alkaline protease production in industrial fermentation medium. Here, we collected the transcription database at various enzyme-producing stages (preliminary stage, stable phase and decline phase) to specifically research the synthesized and regulatory mechanism of alkaline protease in B. licheniformis. The RNA-sequencing analysis showed differential expression of numerous genes related to several processes, among which genes correlated with regulators were concerned, especially the major differential gene abrB on enzyme (AprE) synthesis was investigated. It was further verified that AbrB is a repressor of AprE by plasmid-mediated over-expression due to the severely descending enzyme activity (11,300 U/mL to 2695 U/mL), but interestingly it is indispensable for alkaline protease production because the enzyme activity of the null abrB mutant was just about 2279 U/mL. Thus, we investigated the aprE transcription by eliminating the theoretical binding site (TGGAA) of AbrB protein predicated by computational strategy, which significantly improved the enzyme activity by 1.21-fold and gene transcription level by 1.77-fold in the mid-log phase at a cultivation time of 18 h. Taken together, it is of great significance to improve the production strategy, control the metabolic process and oriented engineering by rational molecular modification of regulatory network based on the high throughput sequencing and computational prediction.

Activity Screening and Structure Modification of Trigonelline as New Anticancer Drug for Non Small Cell Lung Cancer Through In Silico

The biggest case of death in 2018 is caused by lung cancer. Non-small cell lung cancer (NSCLC) is most common. One of the cause lung cancer is the over expression of EGFR. Erlotinib is the first line of anticancer for NSCLC with EGFR mutations. However, erlotinib can cause side effects such as liver damage therefore new safe anticancer is needed. Trigonelline is an alkaloid compound from coffee beans that had anticancer activity in pancreatic cancer cells by inhibiting Nrf2 in vitro and in vivo at concentrations of 0.1-1 µM. Development of cancer cells by Nrf2 is regulated by EGFR. In this study screening and modification of trigonelline structure was carried out to obtain compounds that have anticancer activity on NSCLC against EGFR computationally. The research procedures carried out are modification of ten trigonelline derived structures, the molecular docking and prediction of physicochemical profiles from trigonelline and its modification also their ADMET. Based on results, KF9 has the lowest free energy of binding which was -8,88 kcal/mol and binds to Met769 which has biological activity with receptor. KF9 has good physiochemical profile and absorption, distribution, also toxicity parameters. KF9 has potential to become a new anticancer drug for NSCLC.Keywords: Coffee, Drug discovery and Drug development, Molecular structure modification, Nonsmall cell lung cancer, Trigonelline

Application of a 2D-QSAR with a sine normalization method for the biodegradation of fluoroquinolones to poison cyanobacteria.

Cyanobacteria are photosynthetic autotrophic aquatic prokaryotes. One of the methods for controlling cyanobacterial blooms is to destroy the phycobiliproteins required for photosynthesis. In this study, to improve the biodegradation of the fluoroquinolones through inhibit cyanobacteria, the molecular docking scores of 32 fluoroquinolones (FQs) with four categories of phycobiliproteins from cyanobacteria were calculated after sine normalization to characterize the binding ability between them. A two-dimensional quantitative structure-activity relationship (2D-QSAR) model was constructed based on the comprehensive scores. Danofloxacin (DAN) with the highest comprehensive score was chosen for molecular modification. When docking with four categories of phycobiliproteins from cyanobacteria, the docking values of DAN-11 and DAN-16 were increased up to 35.75%. Moreover, their functional characteristics and environmentally friendly predictive values were improved. When the DAN-11 and DAN-16 molecules docked with the other cyanobacterial phycobiliproteins, indicating that the designed DAN derivatives had general applicability to poison cyanobacteria, the weak interaction forces might increase the binding ability between the DAN derivatives and the receptor phycobiliprotein compared with the target molecule.

Molecular modification approach on kojic acid derivatives as antioxidants related to ascorbic acid.

A hypothetical study by using molecular modeling for antioxidant capacity of kojic acid derivatives was performed using quantum chemistry calculations by DFT/B3LYP/6-311++G(3d,2p). Four modification approaches were considered namely simplification, functional modifications, ring regioisomerism, and hydroxylation. Molecular orbitals, single-electron transfers, hydrogen atom transfers, and spin density distributions were used for antioxidant prediction. In accordance with HOMO, LUMO, Gap, ionization potential, bond dissociation energy, and stabilization energy, the molecular simplifications of kojic acid show that enol moiety is more important for antioxidant capacity than alcohol group. Few molecular modifications on alcohol or enol position were more potent than kojic acid. The π conjugation system among ether, alkene, and hydroxyl moieties can be involved on resonance effects of better compounds. A different performance was observed on alcohol molecular modifications when compared to enol position. All lactone derivatives were more potent than kojic acid on both mechanisms, and their hydroxylated derivatives were more potent than ascorbic acid. In conclusion, the ring regioisomers and its hydroxylated derivatives have better antioxidant capacity than kojic acid. Graphical Abstract The theoretical study using molecular modeling for antioxidant capacity prediction of kojic acid was more related to enol moiety than alcohol. The regioisomerism and hybrid derivatives show that the lactone derivatives increase antioxidant capacity more than the pyrone derivatives.

Epoxy-based grouting materials with super-low viscosities and improved toughness

The main goal of this work was to prepare epoxy grouts with super-low viscosities that could be easily inserted into the micro-cracks of construction materials. The combinations of two diluents—acetone with 1,6 hexanediol diglycidylether (RDDF) or trimethylolpropane glycidylether (RDTF)—were developed for epoxy grouting materials. To clarify the effects of the combined diluents on the epoxy grouting materials, experiments to determine the viscosity and mechanical characteristics and SEM were carried out. The combined diluents could not only dramatically reduce the viscosity of the epoxy solution but could also modify the brittleness of the neat epoxy. To further describe the mechanism, Fourier-transform infrared spectroscopy, thermogravimetric analysis, and dynamic mechanical analyses were used to investigate the molecular modification of the epoxy network. The modification of the epoxy groups contributed to the properties of the epoxy grouts, accelerated the reaction with the curing agents and the ether groups, and improved the flexibilities of the epoxy grouts. Furthermore, the tests of the acute oral toxicity showed that the median lethal oral dose exceeded 5000 mg/kg and could be considered non-toxic. Epoxy grouting materials with super-low viscosities can be used for repairing micro-fractures in construction.

Study of the physico-chemical properties of vancomycin hydrochloride for determining its potential applications in formulation development

The study of physico-chemical properties of vancomycin hydrochloride is an important parameter in the pre–formulation analysis of a drug. Pre-formulation study provides important information for formulation design or support the need for molecular modification. The main objective of pre-formulation is to develop a stable and an effective drug, with a safe dosage. Therefore properties like specific conductivity, density, viscosity, velocity of sound and specific gravity are determined which further helps in determination of critical micelle concentration (CMC). Other thermodynamic parameters are calculated from CMC like change in entropy, enthalpy and Gibb’s free energy which indicated that formation of micelles is favourable and exothermic in nature. Along with this, thermo-acoustic parameters such as apparent molar volume and apparent molar compressibility have also been determined. These parameters revealed that electrostatic interactions were favourable at lower concentrations of vancomycin hydrochloride whereas hydrophobic interactions were dominant at higher concentrations. All these studies have proven useful in determining the types of interactions occurring in the system. Moreover, a stable concentration of vancomycin hydrochloride can also be determined which may aid in the topical formulation of this drug.

Rheological fingerprinting as an effective tool to guide development of personal care formulations

Conventional rheological techniques in the linear viscoelastic region provide insights about the spatial configuration of the microstructural components of personal care formulations in their 'at-rest' state. However, they fail to describe the textural experience associated with large and fast deformations during daily consumer application. In this study we present a non-conventional rheological technique-large amplitude oscillatory shear (LAOS)-for probing the transformation of a material during its application. This technique is proposed a practical tool for formulators in their efforts to design products with desired textural attributes. A non-linear rheological technique termed LAOS was utilized to capture the textural expression perceived by consumers. Lissajous plots (stress vs. strain or strain rate) provide a fingerprint of the formula and are utilized to both analyse the thickening mechanism and monitor the influence of various parameters, such as the chemistry, molecular properties, colloidal parameters and processing conditions. In this study, we showcased several approaches for modifying the texture of personal care formulations and show the influence of various parameters on the characteristics of the Lissajous curves and their relation to sensorial perception. This fingerprinting technique shows that increasing the molecular weight or hydrophobic modification boosts the elasticity and thickening efficiency of a given polymer. Differences in the chemistry of rheological ingredients also influence the characteristic Lissajous fingerprint. In high concentration surfactant systems, which tend to form worm-like micelles, their unique Lissajous fingerprints indicate structure rebuild because of fast kinetics at large but slow deformations. Analysis of lamellar gel-based hair conditioner formulations demonstrates the unique high yield stress of these types of materials, accompanied by the fast breakdown transition from a solid to viscous structure because of their crystalline lamellar gel structure. The LAOS technique presented in this article is intended to better capture the textural expression perceived by consumers. Lissajous plots-generated from the LAOS experimental data-provide a fingerprint of the tested formula and are utilized to both analyse the thickening mechanism and monitor the influence of various parameters, such as the chemistry and molecular weight of the thickener, pH of the formula medium and influence of other ingredients in the formula (surfactants, emulsifiers, etc.).

The Relationship Between Protein S-Nitrosylation and Human Diseases: A Review.

S-nitrosylation (SNO) is a covalent post-translational oxidative modification. The reaction is the nitroso group (-NO) to a reactive cysteine thiol within a protein to form the SNO. In recent years, a variety of proteins in human body have been found to undergo thiol nitrosylation under specific conditions. Protein SNO, which is closely related to cardiovascular disease, Parkinson's syndrome, Alzheimer's disease and tumors, plays an important role in regulatory mechanism of protein function in both physiological and pathological pathways, such as in cellular homeostasis and metabolism. This review discusses possible molecular mechanisms protein SNO modification, such as the role of NO in vivo and the formation mechanism of SNO, with particular emphasis on mechanisms utilized by SNO to cause certain diseases of human. Importantly, the effect of SNO on diseases is multifaceted and multi-channel, and its critical value in vivo is not well defined. Intracellular redox environment is also a key factor affecting its level. Therefore, we should pay more attention to the equilibrium relationship between SNO and denitrosylation pathway in the future researches. These findings provide theoretical support for the improvement or treatment of diseases from the point of view of SNO.

Molecular Functionalization of NiO Nanocatalyst for Enhanced Water Oxidation by Electronic Structure Engineering.

Tuning the local environment of nanomaterial‐based catalysts has emerged as an effective approach to optimize their oxygen evolution reaction (OER) performance, yet the controlled electronic modulation around surface active sites remains a great challenge. Herein, directed electronic modulation of NiO nanoparticles was achieved by simple surface molecular modification with small organic molecules. By adjusting the electronic properties of modifying molecules, the local electronic structure was rationally tailored and a close electronic structure‐activity relationship was discovered: the increasing electron‐withdrawing modification readily decreased the electron density around surface Ni sites, accelerating the reaction kinetics and improving OER activity, and vice versa. Detailed investigation by operando Raman spectroelectrochemistry revealed that the electron‐withdrawing modification facilitates the charge‐transfer kinetics, stimulates the catalyst reconstruction, and promotes abundant high‐valent γ‐NiOOH reactive species generation. The NiO−C6F5 catalyst, with the optimized electronic environment, exhibited superior performance towards water oxidation. This work provides a well‐designed and effective approach for heterogeneous catalyst fabrication under the molecular level.

Boronic Acids and Their Derivatives in Medicinal Chemistry: Synthesis and Biological Applications.

Boron containing compounds have not been widely studied in Medicinal Chemistry, mainly due to the idea that this group could confer some toxicity. Nowadays, this concept has been demystified and, especially after the discovery of the drug bortezomib, the interest for these compounds, mainly boronic acids, has been growing. In this review, several activities of boronic acids, such as anticancer, antibacterial, antiviral activity, and even their application as sensors and delivery systems are addressed. The synthetic processes used to obtain these active compounds are also referred. Noteworthy, the molecular modification by the introduction of boronic acid group to bioactive molecules has shown to modify selectivity, physicochemical, and pharmacokinetic characteristics, with the improvement of the already existing activities. Besides, the preparation of compounds with this chemical group is relatively simple and well known. Taking into consideration these findings, this review reinforces the relevance of extending the studies with boronic acids in Medicinal Chemistry, in order to obtain new promising drugs shortly.