Coumarin-based derivatives with potential anti-HIV activity

Z Xu, Q Chen, Y Zhang, C Liang - Fitoterapia, 2021 - Elsevier
Acquired immunodeficiency syndrome (AIDS), as a result of human immunodeficiency virus
(HIV) infection which leads to severe suppression of immune functions, is an enormous …

The life of pi star: exploring the exciting and forbidden worlds of the benzophenone photophore

G Dorman, H Nakamura, A Pulsipher… - Chemical …, 2016 - ACS Publications
The widespread applications of benzophenone (BP) photochemistry in biological chemistry,
bioorganic chemistry, and material science have been prominent in both academic and …

Protein chemistry combined with mass spectrometry for protein structure determination

EV Petrotchenko, CH Borchers - Chemical Reviews, 2021 - ACS Publications
The advent of soft-ionization mass spectrometry for biomolecules has opened up new
possibilities for the structural analysis of proteins. Combining protein chemistry methods with …

Multimode, cooperative mechanism of action of allosteric HIV-1 integrase inhibitors

JJ Kessl, N Jena, Y Koh, H Taskent-Sezgin… - Journal of Biological …, 2012 - ASBMB
The multifunctional HIV-1 enzyme integrase interacts with viral DNA and its key cellular
cofactor LEDGF to effectively integrate the reverse transcript into a host cell chromosome …

New class of HIV-1 integrase (IN) inhibitors with a dual mode of action

M Tsiang, GS Jones, A Niedziela-Majka, E Kan… - Journal of Biological …, 2012 - ASBMB
tert-Butoxy-(4-phenyl-quinolin-3-yl)-acetic acids (tBPQA) are a new class of HIV-1 integrase
(IN) inhibitors that are structurally distinct from IN strand transfer inhibitors but analogous to …

Non-catalytic site HIV-1 integrase inhibitors disrupt core maturation and induce a reverse transcription block in target cells

M Balakrishnan, SR Yant, L Tsai, C O'Sullivan… - PloS one, 2013 - journals.plos.org
HIV-1 integrase (IN) is the target for two classes of antiretrovirals: i) the integrase strand-
transfer inhibitors (INSTIs) and ii) the non-catalytic site integrase inhibitors (NCINIs). NCINIs …

Target identification by diazirine photo‐cross‐linking and click chemistry

AL MacKinnon, J Taunton - Current protocols in chemical …, 2009 - Wiley Online Library
Target identification is often the rate‐determining step in deciphering the mechanism of
action of biologically active small molecules. Photo‐affinity labeling (PAL) represents a …

Discovery of small-molecule HIV-1 fusion and integrase inhibitors oleuropein and hydroxytyrosol: Part I. Integrase inhibition

S Lee-Huang, PL Huang, D Zhang, JW Lee… - Biochemical and …, 2007 - Elsevier
We have identified oleuropein (Ole) and hydroxytyrosol (HT) as a unique class of HIV-1
inhibitors from olive leaf extracts effective against viral fusion and integration. We used …

A historical sketch of the discovery and development of HIV-1 integrase inhibitors

A Savarino - Expert opinion on investigational drugs, 2006 - Taylor & Francis
The long process of HIV-1 integrase inhibitor discovery and development can be attributed
to both the complexity of HIV-1 integration and poor 'integration'of these researches into …

Integrase, LEDGF/p75 and HIV replication

EM Poeschla - Cellular and molecular life sciences, 2008 - Springer
HIV integrates a DNA copy of its genome into a host cell chromosome in each replication
cycle. The essential DNA cleaving and joining chemistry of integration is known, but there is …