Article
Structural basis for potent and broad inhibition of HIV-1 RT by thiophene[3,2-d]pyrimidine non-nucleoside inhibitors.
eLife - 25 Jul 2018
Yang Yang, Kang Dongwei, Nguyen Laura A, Smithline Zachary B, Pannecouque Christophe, Zhan Peng, Liu Xinyong, Steitz Thomas A
Abstract excerpt
Rapid generation of drug-resistant mutations in HIV-1 reverse transcriptase (RT), a prime target for anti-HIV therapy, poses a major impediment to effective anti-HIV treatment. Our previous efforts have led to the development of two novel non-nucleoside reverse transcriptase inhibitors (NNRTIs) with piperidine-substituted thiophene[3,2-d]pyrimidine scaffolds, compounds K-5a2 and 25a, which demonstrate highly...
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