New antiretroviral inhibitors and HIV-1 drug resistance: more focus on 90% HIV-1 isolates?

E Ndashimye, PS Reyes, EJ Arts - FEMS Microbiology Reviews, 2023 - academic.oup.com
Combined HIV antiretroviral therapy (cART) has been effective except if drug resistance
emerges. As cART has been rolled out in low-income countries, drug resistance has …

Predicted effects of the introduction of long-acting injectable cabotegravir pre-exposure prophylaxis in sub-Saharan Africa: a modelling study

J Smith, L Bansi-Matharu, V Cambiano, D Dimitrov… - The Lancet …, 2023 - thelancet.com
Background Long-acting injectable cabotegravir pre-exposure prophylaxis (PrEP) is
recommended by WHO as an additional option for HIV prevention in sub-Saharan Africa, but …

New designs for HIV-1 integrase inhibitors: a patent review (2018-present)

Y Taoda, S Sugiyama, T Seki - Expert Opinion on Therapeutic …, 2023 - Taylor & Francis
Introduction Combination antiretroviral therapy (cART) has dramatically reduced morbidity
and mortality of HIV-1-infected patients. Integrase strand transfer inhibitors (INSTIs) play an …

[HTML][HTML] Genotypic correlates of resistance to the HIV-1 strand transfer integrase inhibitor cabotegravir

SY Rhee, N Parkin, PR Harrigan, S Holmes, RW Shafer - Antiviral research, 2022 - Elsevier
Cabotegravir (CAB) is an integrase strand transfer inhibitor (INSTI) formulated as a long-
acting injectable drug approved for pre-exposure prophylaxis and use with a long acting …

Emergence of compensatory mutations reveals the importance of electrostatic interactions between HIV-1 integrase and genomic RNA

C Shema Mugisha, T Dinh, A Kumar, K Tenneti… - MBio, 2022 - Am Soc Microbiol
ABSTRACT HIV-1 integrase (IN) has a noncatalytic function in virion maturation through its
binding to the viral RNA genome (gRNA). Class II IN substitutions inhibit IN-gRNA binding …

Allosteric integrase inhibitor influences on HIV-1 integration and roles of LEDGF/p75 and HDGFL2 host factors

PK Singh, W Li, GJ Bedwell, HJ Fadel, EM Poeschla… - Viruses, 2022 - mdpi.com
Allosteric integrase (IN) inhibitors (ALLINIs), which are promising preclinical compounds that
engage the lens epithelium-derived growth factor (LEDGF)/p75 binding site on IN, can …

The C-Terminal domain of RNase H and the C-terminus amino acid residue regulate virus release and autoprocessing of a defective HIV-1 possessing M50I and …

T Imamichi, Q Chen, M Hao, W Chang, J Yang - Viruses, 2022 - mdpi.com
Previously, we reported that an HIV-1 variant containing Met-to-Ile change at codon 50 and
Val-to-Ile mutation at codon 151 of integrase (IN), HIV (IN: M50I/V151I), was an impaired …

[HTML][HTML] Tenofovir and Doravirine Are Potential Reverse-Transcriptase Analogs in Combination with the New Reverse-Transcriptase Translocation Inhibitor (Islatravir) …

AD Nka, Y Bouba, WR Tsapi Lontsi… - Viruses, 2025 - mdpi.com
Islatravir (ISL) is a novel antiretroviral that inhibits HIV-1 reverse transcriptase translocation.
The M184V mutation, known to reduce ISL's viral susceptibility in vitro, could arise from …

A Combination of M50I and V151I polymorphic mutations in HIV-1 subtype B integrase results in defects in autoprocessing

J Yang, M Hao, MA Khan, MT Rehman, HC Highbarger… - Viruses, 2021 - mdpi.com
We have recently reported that a recombinant HIV-1NL4. 3 containing Met-to-Ile change at
codon 50 of integrase (IN)(IN: M50I) exhibits suppression of the virus release below 0.5% of …

HIV-1 subtype F integrase polymorphisms external to the catalytic core domain contribute to severe loss of replication capacity in context of the integrase inhibitor …

PC Aulicino, Z Momin, M Rozenszajn… - Journal of …, 2022 - academic.oup.com
Background In prior studies, HIV-1 BF recombinants with subtype F integrases failed to
develop resistance to raltegravir through the Q148H mutational pathway. We aimed to …