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Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles.
Author: ChenWenmin, DaelemansDirk, De ClercqErik, GaoPing, GinexTiziana, HuangBoshi, JiangXiangyi, KangDongwei, LiZhenyu, LiuXinyong, LuqueFrancisco Javier, PannecouqueChristophe, TianYe, VílchezDavid, ZhanPeng, ZhangJian, ZhaoTong
Original Abstract of the Article :
Diarylpyrimidine derivatives (DAPYs) exhibit robust anti-HIV-1 potency, although they have been compromised by E138K variant and severe side-effects and been suffering from poor water solubility. In the present work, hydrophilic morpholine or methylsulfonyl and sulfamide-substituted piperazine/piper...See full text at original site
Dr.Camel's Paper Summary Blogラクダ博士について
ラクダ博士は、Health Journal が論文の内容を分かりやすく解説するために作成した架空のキャラクターです。
難解な医学論文を、専門知識のない方にも理解しやすいように、噛み砕いて説明することを目指しています。
* ラクダ博士による解説は、あくまで論文の要点をまとめたものであり、原論文の完全な代替となるものではありません。詳細な内容については、必ず原論文をご参照ください。
* ラクダ博士は架空のキャラクターであり、実際の医学研究者や医療従事者とは一切関係がありません。
* 解説の内容は Health Journal が独自に解釈・作成したものであり、原論文の著者または出版社の見解を反映するものではありません。
引用元:
https://doi.org/10.1021/acs.jmedchem.8b01729
データ提供:米国国立医学図書館(NLM)
Diarylpyrimidine Derivatives: A New Oasis in the Desert of HIV Treatment
HIV, like a persistent drought in the desert, continues to pose a global health challenge. This study, like a tireless caravan seeking a solution, explores the development of new anti-HIV medications, specifically diarylpyrimidine derivatives (DAPYs). The researchers, like skilled desert engineers, carefully design and test these medications, targeting the HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. The study highlights the potential of DAPYs to overcome the challenges posed by HIV drug resistance, offering hope for individuals living with HIV.
A New Route to Treatment: DAPYs' Potential
The study reveals that DAPYs, like a newly discovered water source in the desert, exhibit robust anti-HIV activity against both wild-type and E138K mutant virus. The researchers, like astute desert explorers, identify a promising lead compound (11c), which demonstrates excellent potency and favorable safety profiles, paving the way for further development and optimization of these medications.
Staying Hydrated in the Fight Against HIV: Tips for Patients
Remember, living with HIV, like navigating a harsh desert landscape, requires careful management and adherence to treatment plans. Stay informed about the latest advancements in HIV treatment and work closely with your healthcare provider to develop a personalized plan that meets your specific needs. DAPYs, like a refreshing oasis, offer hope for a more effective and tolerable treatment option, giving individuals living with HIV a chance to thrive.
Dr. Camel's Conclusion
This study, like a shimmering oasis in the desert, provides a glimmer of hope in the fight against HIV. The development of DAPYs, like the discovery of a precious water source, offers a new avenue for treatment, potentially improving outcomes and quality of life for individuals living with HIV. The journey towards a cure continues, and the unwavering dedication of researchers and healthcare professionals provides solace and strength to those affected by this global health challenge.
Date :
- Date Completed 2020-03-03
- Date Revised 2020-03-03
Further Info :
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