Open Access. Powered by Scholars. Published by Universities.®
- Keyword
-
- AIDS Dementia Complex (1)
- Acute toxicity (1)
- Allosteric modulator (1)
- Animals (1)
- Anti-inflammatory drugs (1)
-
- Cocaine (1)
- Dopamine (1)
- Dopamine Plasma Membrane Transport Proteins (1)
- Dopamine transporter (1)
- Drug activation (1)
- Drug discovery and development (1)
- HIV-1 Tat (1)
- Heroin (1)
- Humans (1)
- Lead optimization (1)
- MPGES-1 inhibitors (1)
- Molecular medicine (1)
- Mutation (1)
- Neurotoxicity syndromes (1)
- Tat Gene Products, Human Immunodeficiency Virus (1)
- Wild-type mice (1)
Articles 1 - 3 of 3
Full-Text Articles in Medicine and Health Sciences
Blocking Drug Activation As A Therapeutic Strategy To Attenuate Acute Toxicity And Physiological Effects Of Heroin, Ting Zhang, Xirong Zheng, Kyungbo Kim, Fang Zheng, Chang-Guo Zhan
Blocking Drug Activation As A Therapeutic Strategy To Attenuate Acute Toxicity And Physiological Effects Of Heroin, Ting Zhang, Xirong Zheng, Kyungbo Kim, Fang Zheng, Chang-Guo Zhan
Molecular Modeling and Biopharmaceutical Center Faculty Publications
Heroin is a growing national crisis in America. There is an increasing frequency of heroin overdoses. All of the currently used therapeutic approaches to treatment of heroin abuse and other opioid drugs of abuse focus on antagonizing a brain receptor (particularly µ-opiate receptors). However, it has been known that the therapeutic use of certain µ-opiate receptor antagonist may actually increase heroin overdose. Once overdosed, heroin addicts may continue to get overdosed again and again until fatal. Here we report our design and validation of a novel therapeutic strategy targeting heroin activation based on our analysis of the chemical transformation and …
Structure-Based Discovery Of Mpges-1 Inhibitors Suitable For Preclinical Testing In Wild-Type Mice As A New Generation Of Anti-Inflammatory Drugs, Kai Ding, Ziyuan Zhou, Shurong Hou, Yaxia Yuan, Shuo Zhou, Xirong Zheng, Jianzhong Chen, Charles D. Loftin, Fang Zheng, Chang-Guo Zhan
Structure-Based Discovery Of Mpges-1 Inhibitors Suitable For Preclinical Testing In Wild-Type Mice As A New Generation Of Anti-Inflammatory Drugs, Kai Ding, Ziyuan Zhou, Shurong Hou, Yaxia Yuan, Shuo Zhou, Xirong Zheng, Jianzhong Chen, Charles D. Loftin, Fang Zheng, Chang-Guo Zhan
Molecular Modeling and Biopharmaceutical Center Faculty Publications
Human mPGES-1 is recognized as a promising target for next generation of anti-inflammatory drugs without the side effects of currently available anti-inflammatory drugs, and various inhibitors have been reported in the literature. However, none of the reported potent inhibitors of human mPGES-1 has shown to be also a potent inhibitor of mouse or rat mPGES-1, which prevents using the well-established mouse/rat models of inflammation-related diseases for preclinical studies. Hence, despite of extensive efforts to design and discover various human mPGES-1 inhibitors, the promise of mPGES-1 as a target for the next generation of anti-inflammatory drugs has never been demonstrated in …
The Role Of Human Dopamine Transporter In Neuroaids, Jun Zhu, Subramaniam Ananthan, Chang-Guo Zhan
The Role Of Human Dopamine Transporter In Neuroaids, Jun Zhu, Subramaniam Ananthan, Chang-Guo Zhan
Molecular Modeling and Biopharmaceutical Center Faculty Publications
HIV-associated neurocognitive disorder (HAND) remains highly prevalent in HIV infected individuals and represents a special group of neuropathological disorders, which are associated with HIV-1 viral proteins, such as transactivator of transcription (Tat) protein. Cocaine abuse increases the incidence of HAND and exacerbates its severity by enhancing viral replication. Perturbation of dopaminergic transmission has been implicated as a risk factor of HAND. The presynaptic dopamine (DA) transporter (DAT) is essential for DA homeostasis and dopaminergic modulation of the brain function including cognition. Tat and cocaine synergistically elevate synaptic DA levels by acting directly on human DAT (hDAT), ultimately leading to dysregulation …