Prominent publications by Xiabin Chen

KOL Index score: 8910

INTRODUCTION: Tyrosine kinase 2 (Tyk2) is a non-receptor tyrosine-protein kinase, an enzyme that in humans is encoded by the TYK2 gene. Tyk2, together with three other family subtypes, namely, Jak1, Jak2, and Jak3, belong to the JAK family. Before 2014, far more publications and patents appeared in public domain attributing to the development of selective Jak2 and Jak3 inhibitors than those for selective Tyk2 and Jak1 inhibitors.

AREAS COVERED: This review sought to give an overview of ...

Known for Tyk2 Inhibitors |  Patent Review |  Potential Therapeutic Agents |  Tyrosine Kinase |  Rheumatoid Arthritis
KOL Index score: 7298

Cocaine is a widely abused drug without an FDA (Food and Drug Administration)-approved medication. It has been recognized that an ideal anti-cocaine medication would accelerate cocaine metabolism producing biologically inactive metabolites via a route similar to the primary cocaine-metabolizing pathway, i.e. human BChE (butyrylcholinesterase)-catalysed hydrolysis. However, the native human BChE has a low catalytic activity against cocaine. We recently designed and discovered a BChE ...

Known for Human Butyrylcholinesterase |  Cocaine Hydrolase |  Vivo Characterization |  Catalytic Activity |  Animal Models
KOL Index score: 7118

Gene transfer of a human cocaine hydrolase (hCocH) derived from butyrylcholinesterase (BChE) by 5 mutations (A199S/F227A/S287G/A328W/Y332G) has shown promise in animal studies for treatment of cocaine addiction. To predict the physiological fate and immunogenicity of this enzyme in humans, a comparable enzyme was created and tested in a conspecific host. Thus, similar mutations (A199S/S227A/S287G/A328W/Y332G) were introduced into mouse BChE to obtain a mouse CocH (mCocH). The cDNA was ...

Known for Gene Transfer |  Mouse Bche |  Cocaine Hydrolase |  Viral Vectors |  Adenoassociated Virus
KOL Index score: 6202

Cocaine is one of the most addictive drugs without a U.S. Food and Drug Administration (FDA)-approved medication. Enzyme therapy using an efficient cocaine-metabolizing enzyme is recognized as the most promising approach to cocaine overdose treatment. The actual enzyme, known as RBP-8000, under current clinical development for cocaine overdose treatment is our previously designed T172R/G173Q mutant of bacterial cocaine esterase (CocE). The T172R/G173Q mutant is effective in hydrolyzing ...

Known for Cocaine Metabolite |  Enzyme Therapy |  Human Butyrylcholinesterase |  Overdose Treatment |  Body Environment
KOL Index score: 6174

Cocaine abuse is a world-wide public health and social problem without a US Food and Drug Administration-approved medication. An ideal anticocaine medication would accelerate cocaine metabolism, producing biologically inactive metabolites by administration of an efficient cocaine-specific exogenous enzyme. Our recent studies have led to the discovery of the desirable, highly efficient cocaine hydrolases (CocHs) that can efficiently detoxify and inactivate cocaine without affecting normal ...

Known for Cocaine Metabolism |  Molecular Rats |  Catalytic Efficiency |  Single Dose |  Long Period
KOL Index score: 5853

Development of a truly effective medication for treatment of cocaine abuse has been a grand challenge. There is no FDA-approved therapeutic agent specific for cocaine addiction or overdose. An enzyme therapy using an efficient cocaine-metabolizing enzyme could be a promising treatment strategy for cocaine overdose and addiction. One of our previously designed cocaine hydrolases (CocHs), known as CocH1, was fused with human serum albumin (HSA) to prolong the biological half-life. The ...

Known for Cocaine Toxicity |  Coch1 Hsa |  Clinical Potential |  Enzyme Therapy |  Grand Challenge
KOL Index score: 5597

β-elemene is a noncytotoxic Class II antitumor drug extracted from the traditional Chinese medicine Curcuma wenyujin Y. H. Chen et C. Ling. β-elemene exerts its effects by inhibiting cell proliferation, arresting the cell cycle, inducing cell apoptosis, exerting antiangiogenesis and antimetastasis effects, reversing multiple-drug resistance (MDR), and enhancing the immune system. Elemene injection and oral emulsion have been used to treat various tumors, including cancer of the lung, ...

Known for Cancer Therapy |  Drug Delivery |  Elemene Injection |  Cell Cycle |  Solid Lipid Nanoparticles
KOL Index score: 4951

Cocaine esterase (CocE) is known as the most efficient natural enzyme for cocaine hydrolysis. The major obstacle to the clinical application of wild-type CocE is the thermoinstability with a half-life of only ∼12 min at 37 °C. The previously designed T172R/G173Q mutant (denoted as enzyme E172-173) with an improved in vitro half-life of ∼6 h at 37 °C is currently in clinical trial Phase II for cocaine overdose treatment. Through molecular modeling and dynamics simulation, we designed and ...

Known for 37 °c |  Crosssubunit Disulfide Bonds |  Pegylated E196 |  Catalytic Efficiency |  Cocaine Esterase
KOL Index score: 4400

Cocaine abuse is a worldwide public health and social problem without a US Food and Drug Administration (FDA)-approved medication. Accelerating cocaine metabolism that produces biologically inactive metabolites by administration of an efficient cocaine hydrolase (CocH) has been recognized as a promising strategy for cocaine abuse treatment. However, the therapeutic effects of CocH are limited by its short biological half-life (e.g., 8 h or shorter in rats). In this study, we designed and ...

Known for Cocaine Hydrolase |  Recombinant Proteins |  Protein Domains |  Addiction Treatment |  Biological Life
KOL Index score: 4320

It is a grand challenge to develop a truly effective medication for treatment of cocaine overdose. The current available, practical emergence treatment for cocaine overdose includes administration of a benzodiazepine anticonvulsant agent (e.g. diazepam) and/or physical cooling with an aim to relieve the symptoms. The inherent difficulties of antagonizing physiological effects of drugs in the central nervous system have led to exploring protein-based pharmacokinetic approaches using ...

Known for Cocaine Overdose |  Clinical Potential |  Grand Challenge |  Effective Medication |  Locomotor Activity
KOL Index score: 4278

Human butyrylcholinesterase (BChE) is known as a safe and effective protein for detoxification of organophosphorus (OP) nerve agents. Its rationally designed mutants with considerably improved catalytic activity against cocaine, known as cocaine hydrolases (CocHs), are recognized as the most promising drug candidates for the treatment of cocaine abuse. However, it is a grand challenge to efficiently produce active recombinant BChE and CocHs with a sufficiently long biological half-life. ...

Known for Cocaine Abuse |  Proteins Recombinant |  Promising Candidate |  Human Butyrylcholinesterase |  Grand Challenge
KOL Index score: 3965

As new metabolic pathways of cocaine were recently identified, a high performance liquid chromatography tandem mass spectrometry (LC-MS/MS) method was developed to simultaneously determine cocaine and nine cocaine-related metabolites in whole blood samples. One-step solid phase extraction was used to extract all of the ten compounds and corresponding internal standards from blood samples. All compounds and internal standards extracted were separated on an Atlantis T3 (100Å, 3μm, ...

Known for Simultaneous Determination |  Liquid Chromatography |  Tandem Mass |  Multiple Reaction Monitoring |  Cocaine Metabolites
KOL Index score: 3775

Carboxylesterase-1 (CE-1) is a crucial enzyme responsible for metabolism/activation/inactivation of xenobiotics (therapeutic agents, prodrugs, abused drugs, and organophosphorus nerve agents etc.) and also involved in many other biological processes. In this study, we performed extensive computational modeling and simulations to understand the fundamental reaction mechanism of cocaine hydrolysis catalyzed by CE-1, revealing that CE-1-catalyzed cocaine hydrolysis follows a novel reaction ...

Known for Cocaine Hydrolysis |  Drug Metabolism |  Transition States |  Catalytic Mechanism |  Oxyanion Hole
KOL Index score: 3701

Accelerating cocaine metabolism through enzymatic hydrolysis at cocaine benzoyl ester is recognized as a promising therapeutic approach for cocaine abuse treatment. Our more recently designed A199S/F227A/S287G/A328W/Y332G mutant of human BChE, denoted as cocaine hydrolase-3 (CocH3), has a considerably improved catalytic efficiency against cocaine and has been proven active in blocking cocaine-induced toxicity and physiological effects. In the present study, we have further characterized ...

Known for Human Butyrylcholinesterase |  Cocaine Hydrolase |  Protein Engineering |  Tandem Mass |  Spectrometry Animals
KOL Index score: 3209

Mouse butyrylcholinesterase (mBChE) and an mBChE-based cocaine hydrolase (mCocH, i.e. the A¹⁹⁹S/S²²⁷A/S²⁸⁷G/A³²⁸W/Y³³²G mutant) have been characterized for their catalytic activities against cocaine, i.e. naturally occurring (-)-cocaine, in comparison with the corresponding human BChE (hBChE) and an hBChE-based cocaine hydrolase (hCocH, i.e. the A¹⁹⁹S/F²²⁷A/S²⁸⁷G/A³²⁸W/Y³³²G mutant). It has been demonstrated that mCocH and hCocH have improved the catalytic efficiency of mBChE and hBChE ...

Known for Cocaine Hydrolase |  Catalytic Efficiency |  Human Bche |  Mutant Proteins |  Protein Engineering


Xiabin Chen: Influence Statistics

Sample of concepts for which Xiabin Chen is among the top experts in the world.
Concept World rank
elimination clinical treatment #2
rbp8000 produce #2
rbp8000 clinically #2
rbp8000 cholinesterase #2
endogenous cholinesterases #2
marked sublethal toxicity #2
rbp8000s cholinesterase activity #2
elimination cocaine metabolite #2
supplemental evidences #2
development rbp8000 #2
rbp8000 study #2
cocaine overdose treatment #2
activity rbp8000 #2
cholinesterase activity cocaine #2
cocaine rbp8000 #2
addictive drug contaminant #2
overdose acetylthiocholine #2
cocederived rbp8000 #2
acetylthiocholine bacterial #2
1000fold 5000fold #2
1 hacc1 #3
barrier 201 #3
hydrolysis ce1 #3
isomerization isomerase #3
catalytic hacc1 #3
isomerization carboxybiotin #3
coa carboxybiotin #3
hacc1 isomerization #3
hacc1 catalyzed #3
atom cocaine #3
mechanism hacc1 #3
catalyzed hacc1 #3
cocaine carbonyl #3
transition state hacc1 #3
hacc1 catalytic #3
cocaine hydrolysis pathway #3
carboxybiotin hacc1 #3
carboxyl transfer carboxybiotin #3
ce1 catalyzed #3
isomerization obesity #3
state hacc1 #3
catalyzed ce1 #3
catalytic hacc1 isomerization #3
cocaine nh #3
carboxylesterase1 cocaine #3
isomerase carboxyl #3
design hacc1 #3
carboxybiotin ratelimiting step #3
isomerase carboxyl transfer #3
ce1catalyzed cocaine hydrolysis #3

Key People For Cocaine Hydrolase

Top KOLs in the world
Stephen W Brimijoin
axonal transport cocaine hydrolase gene transfer
Oksana Lockridge
human butyrylcholinesterase mass spectrometry active site
Yuan Ping Pang
hydroxamic acids crystal structures small molecules
Hong Sun
cocaine hydrolase milligram tissue molecular modeling
Yang Gao
cocaine hydrolase gene transfer human butyrylcholinesterase
Chang‐Guo Zhan
human butyrylcholinesterase energy barriers molecular dynamics

Xiabin Chen:Expert Impact

Concepts for whichXiabin Chenhas direct influence:Cocaine hydrolase,  Dendrobium officinale,  Cocaine abuse,  Cocaine overdose,  Human butyrylcholinesterase,  Clinical potential,  Cocaine toxicity,  Catalytic efficiency.

Xiabin Chen:KOL impact

Concepts related to the work of other authors for whichfor which Xiabin Chen has influence:Cocaine hydrolase,  Tyrosine kinase,  Lncrna hotair,  Elemene injection,  Human butyrylcholinesterase,  Curcumae radix,  Endophytic streptomyces.



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College of Pharmacy, School of Medicine, Hangzhou Normal University, Hangzhou, China; Key Laboratory of Elemene Class Anti-Cancer Chinese Medicines; Engineering Laboratory of Development and Application of Traditional Chinese Medicines; Collaborative

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