Abstract: The present invention relates to the technical field of biological medicine, and particularly to a heat shock protein 90 (HSP90)-mediated targeting chimera (HEMTAC) small-molecule degradation agent and an application thereof. It is found through research in the present invention that the HEMTAC small-molecule degradation agent can induce formation of an HSP90-HEMTAC-targeted protein ternary complex, the targeted protein is spatially positioned at a position which is beneficial for being mistakenly recognized as an “abnormal” protein by the HSP90, is then introduced into a ubiquitin-proteasome system, and causes degradation of the targeted protein. HEMTACs are released to participate in the next degradation cycle. Therefore, the HEMTACs have a catalytic effect in targeted protein ubiquitin induction and degradation, can be used for treating diseases related to tumors, inflammations, immunity and the like, and have a good prospect for practical application.

Abstract: The present disclosure encompasses oligonucleotide aptamers selectively binding a target glycosylated polypeptide or protein, and having biased affinity for the glycan through a boronic acid linked to a nucleosidic base of a nucleotide(s). The disclosure further encompasses methods for isolating an aptamer(s) selectively binding a target glycosylated polypeptide, where, from a population of randomized oligonucleotides that have at least one nucleotide having a boronic acid label linked to a base, is selected a first subpopulation of aptamers binding to the target glycosylated polypeptide or protein. This subpopulation is then amplified without using boronic acid-modified TTP, and amplification products not binding to a target glycosylated polypeptide or protein are selected. The second subpopulation of aptamers is then amplified using boronic acid-modified TTP to provide a population of boronic acid-modified aptamers capable of selectively binding to a glycosylation site of a target polypeptide or protein.

Abstract: The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.

Abstract: The present disclosure encompasses oligonucleotide aptamers selectively binding a target glycosylated polypeptide or protein, and having biased affinity for the glycan through a boronic acid linked to a nucleosidic base of a nucleotide(s). The disclosure further encompasses methods for isolating an aptamer(s) selectively binding a target glycosylated polypeptide, where, from a population of randomized oligonucleotides that have at least one nucleotide having a boronic acid label linked to a base, is selected a first subpopulation of aptamers binding to the target glycosylated polypeptide or protein. This subpopulation is then amplified without using boronic acid-modified TTP, and amplification products not binding to a target glycosylated polypeptide or protein are selected. The second subpopulation of aptamers is then amplified using boronic acid-modified TTP to provide a population of boronic acid-modified aptamers capable of selectively binding to a glycosylation site of a target polypeptide or protein.

Abstract: Boronic acid-modified DNA-based aptamers can be selected to recognize fibrinogen through binding at a glycosylation site and thus are useful for probing the effect of glycosylation pattern changes on the ability for fibrinogen to mediate blood coagulation. In addition, the aptamers of the disclosure also have anticoagulation effects due to their binding to fibrinogen and its cleavage product fibrin. The present disclosure, therefore, encompasses methods for inhibiting fibrin coagulation with an aptamer capable of specifically binding to a glycosylation site of fibrinogen or fibrin. The disclosure further provides oligonucleotide aptamers comprising at least one nucleotide having a boronic acid thereon, where the aptamer is capable of selectively binding to a glycosylation site of fibrinogen, or the derivative thereof.

Abstract: The present invention provides a chroman compound of formula (I) and its pharmaceutical salt, methods of its preparation and its pharmaceutical applications. Wherein: X is O or S; n is for 2, 3 or 4; R1 is 6-substituted or 7-substituted halogen, C1-4alkyl, C1-4alkoxyl, benzyloxy, carbamoyl; R2 is nitrogen-containing five-membered or six-membered substituted heterocyclic ring selected from piperidinyl, morpholinyl, N-methyl-piperazinyl, N-(2-ethoxyl)piperazinyl, pyrrolyl, pyrazolyl or imidazolyl. The compounds are useful to prepare medicaments for treating cardiovascular diseases, their preparation employs mild reaction conditions, the raw material are plenty and easy to be obtained, and the operation and post-treatment in the preparation are simple.

Abstract: The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.

Abstract: The present invention provided a chroman compound, the method of its preparation and pharmaceutical applications. The compound are represented by formula (I) and its pharmaceutical salt, where in :x is for O or S; n is for 2, 3 or 4; R1 is 6-situ or 7-situ halogen, C1-4alkyl, C1-4alkyoxyl, benzyloxy, acylamino; R2 is nitrogen-containing pentatomic or hexahydric substituted heterocyclic ring. The compound is useful to prepare anti-arrhythmic drugs, the reaction conditions of the method are mild, the raw material are plenty and easy to be obtained, and the operation and post-treatment are simple.