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The Drug-Induced Interface That Drives HIV-1 Integrase Hypermultimerization and Loss of Function
Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are an emerging class of small molecules that disrupt viral maturation by inducing the aberrant multimerization of IN. Here, we present cocrystal structures of HIV-1 IN with two potent ALLINIs, namely,
Matthew R. Singer+14 more
doaj +1 more source
As an important antiviral target, HIV-1 integrase plays a key role in the viral life cycle, and five integrase strand transfer inhibitors (INSTIs) have been approved for the treatment of HIV-1 infections so far.
Yu-Chan Wang+8 more
doaj +1 more source
Summary Zanthoxylum armatum and Zanthoxylum bungeanum, known as ‘Chinese pepper’, are distinguished by their extraordinary complex genomes, phenotypic innovation of adaptive evolution and species‐special metabolites. Here, we report reference‐grade genomes of Z. armatum and Z. bungeanum.
Lisong Hu+20 more
wiley +1 more source
Soft Rot Pectobacteriaceae (SRP; Pectobacterium spp. and Dickeya spp., formerly known as pectinolytic Erwinia spp.) are necrotrophic bacterial pathogens infecting a large number of plant species worldwide, including agriculturally-important crops ...
Robert Czajkowski
doaj +1 more source
Quantum-Chemistry based design of halobenzene derivatives with augmented affinities for the HIV-1 viral G4/C16 base-pair [PDF]
The HIV-1 integrase (IN) is a major target for the design of novel anti-HIV inhibitors. Among these, three inhibitors which embody a halobenzene ring derivative (HR) in their structures are presently used in clinics. High-resolution X-ray crystallography of the complexes of the IN-viral DNA transient complex bound to each of the three inhibitors showed
arxiv +1 more source
Using the class 1 integron-integrase gene as a proxy for anthropogenic pollution
Around all human activity, there are zones of pollution with pesticides, heavy metals, pharmaceuticals, personal care products and the microorganisms associated with human waste streams and agriculture.
M. Gillings+5 more
semanticscholar +1 more source
Relationship between HIV integrase polymorphisms and integrase inhibitor susceptibility: An in silico analysis [PDF]
Integrase (IN) plays an essential role in HIV-1 replication, by mediating integration of the viral genome into the host cell genome. IN is a potential target of antiretroviral (ARV) therapeutic drugs such as ALLINI, Raltegravir (RAL), and Elvitegravir (EVG).
Hotma Martogi Lorensi Hutapea+2 more
openaire +4 more sources
More than 10 million people worldwide are infected with the retrovirus human T-cell lymphotropic virus type 1 (HTLV-1). Infection phenotypes can range from asymptomatic to severe adult T-cell leukemia/lymphoma (ATLL) and HTLV-1-associated myelopathy ...
Michał S. Barski+2 more
doaj +1 more source
Background: With the introduction of integrase strand transfer inhibitor (INSTI)-based antiretroviral therapy, persons living with HIV have a potent new treatment option.
Jamison Norwood+10 more
semanticscholar +1 more source
Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase
One of the major factors contributing to HIV-1 drug resistance is suboptimal adherence to combination antiretroviral therapy (cART). Currently, recommended cART for HIV-1 treatment is a three-drug combination, whereas the pre-exposure prophylaxis (PrEP ...
Kamal Singh+2 more
doaj +1 more source