LB50053: A 5-Hydroxytryptamine1A Agent with a High Binding Affinity and a Potency Evoking a K+ Current

Pharmacology ◽  
2002 ◽  
Vol 65 (4) ◽  
pp. 175-181
Author(s):  
Han-Seop Kim ◽  
Taesup Cho ◽  
Changho Lee ◽  
Hyun Joo ◽  
Seung Kim ◽  
...  
Keyword(s):  
Binding Affinity ◽  
High Binding ◽  
High Binding Affinity

scholarly journals Herb-target virtual screening and network pharmacology for prediction of molecular mechanism of Danggui Beimu Kushen Wan for prostate cancer

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Hong Li ◽  
Andrew Hung ◽  
Angela Wei Hong Yang
Keyword(s):  
Prostate Cancer ◽  
Binding Affinity ◽  
Molecular Mechanisms ◽  
Biological Activities ◽  
Tight Binding ◽  
Experimental Studies ◽  
Network Pharmacology ◽  
High Morbidity ◽  
High Binding ◽  
High Binding Affinity

AbstractProstate cancer (PCa) is a cancer that occurs in the prostate with high morbidity and mortality. Danggui Beimu Kushen Wan (DBKW) is a classic formula for patients with difficult urination including PCa. This study aimed to investigate the molecular mechanisms of DBKW for PCa. We obtained DBKW compounds from our previous reviews. We identified potential targets for PCa from literature search, currently approved drugs and Open Targets database and filtered them by protein–protein interaction network analysis. We selected 26 targets to predict three cancer-related pathways. A total of 621 compounds were screened via molecular docking using PyRx and AutoDock Vina against 21 targets for PCa, producing 13041 docking results. The binding patterns and positions showed that a relatively small number of tight-binding compounds from DBKW were predicted to interact strongly and selectively with three targets. The top five high-binding-affinity compounds were selected to generate a network, indicating that compounds from all three herbs had high binding affinity against the 21 targets and may have potential biological activities with the targets. DBKW contains multi-targeting agents that could act on more than one pathway of PCa simultaneously. Further studies could focus on validating the computational results via experimental studies.

A fluorescent probe for butyrylcholinesterase activity in human serum based on a fluorophore with specific binding affinity for human serum albumin

2019 ◽  
Vol 55 (97) ◽  
pp. 14574-14577 ◽  
Author(s):  
Soyeon Yoo ◽  
Min Su Han
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Human Serum ◽  
Fluorescent Probe ◽  
Binding Affinity ◽  
Specific Binding ◽  
Turn On ◽  
High Binding ◽  
Butyrylcholinesterase Activity ◽  
High Binding Affinity

We report a novel turn-on sensing probe for the detection of butyrylcholinesterase activity in human serum using a fluorophore with high binding affinity for HSA.

scholarly journals Peptide-binding induced inhibition of chemokine CXCL12

RSC Advances ◽  
2017 ◽  
Vol 7 (34) ◽  
pp. 21298-21307
Author(s):  
Hongyang Duan ◽  
Ling Zhu ◽  
Jiaxi Peng ◽  
Mo Yang ◽  
Hanyi Xie ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Peptide Binding ◽  
Inhibitory Effect ◽  
High Binding ◽  
Significant Inhibitory Effect ◽  
Chemokine Cxcl12 ◽  
Cxcr4 Axis ◽  
High Binding Affinity

A designed peptide (W4) has a significant inhibitory effect on the CXCL12/CXCR4 axis by targeting CXCL12 with high binding affinity.

Synthesis of Oligo(3-hydroxybutanoate)(OHB)-Containing Peptides with High Binding Affinity to a Class-I-MHC Protein

1998 ◽  
Vol 81 (5-8) ◽  
pp. 1181-1200 ◽  
Author(s):  
Dieter Seebach ◽  
Sorana Poenaru ◽  
Gerd Folkers ◽  
Didier Rognan
Keyword(s):  
Binding Affinity ◽  
Class I ◽  
Class I Mhc ◽  
High Binding ◽  
High Binding Affinity

Benzenebistriazole-strapped calix[4]pyrrole: a neutral anion receptor with CH and NH donor groups that exhibits high sulfate binding affinity and selectivity in aqueous solutions

2020 ◽  
Vol 56 (65) ◽  
pp. 9364-9367
Author(s):  
Ying-Chun He ◽  
Yan-Mei Yan ◽  
Hong-Bo Tong ◽  
Zhen-Xing Ren ◽  
Jun-Hong Wang ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Aqueous Solutions ◽  
Binding Affinity ◽  
Anion Receptor ◽  
High Binding ◽  
High Sulfate ◽  
High Binding Affinity

Benzenebistriazole-strapped calix[4]pyrrole with high binding affinity and selectivity for sulfate in an aqueous solution has been synthesized.

scholarly journals A Bifunctional Adsorber Particle for the Removal of Hydrophobic Uremic Toxins from Whole Blood of Renal Failure Patients

Toxins ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 389 ◽  
Author(s):  
Marieke Sternkopf ◽  
Sven Thoröe-Boveleth ◽  
Tobias Beck ◽  
Kirsten Oleschko ◽  
Ansgar Erlenkötter ◽  
...  
Keyword(s):  
Adsorption Capacity ◽  
Binding Affinity ◽  
Whole Blood ◽  
Uremic Toxins ◽  
In Vivo Studies ◽  
Uremic Toxin ◽  
High Binding ◽  
High Binding Affinity

Hydrophobic uremic toxins accumulate in patients with chronic kidney disease, contributing to a highly increased cardiovascular risk. The clearance of these uremic toxins using current hemodialysis techniques is limited due to their hydrophobicity and their high binding affinity to plasma proteins. Adsorber techniques may be an appropriate alternative to increase hydrophobic uremic toxin removal. We developed an extracorporeal, whole-blood bifunctional adsorber particle consisting of a porous, activated charcoal core with a hydrophilic polyvinylpyrrolidone surface coating. The adsorption capacity was quantified using analytical chromatography after perfusion of the particles with an albumin solution or blood, each containing mixtures of hydrophobic uremic toxins. A time-dependent increase in hydrophobic uremic toxin adsorption was depicted and all toxins showed a high binding affinity to the adsorber particles. Further, the particle showed a sufficient hemocompatibility without significant effects on complement component 5a, thrombin-antithrombin III complex, or thrombocyte concentration in blood in vitro, although leukocyte counts were slightly reduced. In conclusion, the bifunctional adsorber particle with cross-linked polyvinylpyrrolidone coating showed a high adsorption capacity without adverse effects on hemocompatibility in vitro. Thus, it may be an interesting candidate for further in vivo studies with the aim to increase the efficiency of conventional dialysis techniques.

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