[HTML][HTML] Stapled peptides inhibitors: a new window for target drug discovery

AM Ali, J Atmaj, N Van Oosterwijk, MR Groves… - Computational and …, 2019 - Elsevier
Protein-protein interaction (PPI) is a hot topic in clinical research as protein networking has a
major impact in human disease. Such PPIs are potential drugs targets, leading to the need …

Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors

L Zhang, D Lin, X Sun, U Curth, C Drosten… - Science, 2020 - science.org
The coronavirus disease 2019 (COVID-19) pandemic caused by severe acute respiratory
syndrome–coronavirus 2 (SARS-CoV-2) is a global health emergency. An attractive drug …

α-Ketoamides as broad-spectrum inhibitors of coronavirus and enterovirus replication: structure-based design, synthesis, and activity assessment

L Zhang, D Lin, Y Kusov, Y Nian, Q Ma… - Journal of medicinal …, 2020 - ACS Publications
The main protease of coronaviruses and the 3C protease of enteroviruses share a similar
active-site architecture and a unique requirement for glutamine in the P1 position of the …

SARS-CoV-2 Mpro inhibitors and activity-based probes for patient-sample imaging

W Rut, K Groborz, L Zhang, X Sun… - Nature chemical …, 2021 - nature.com
In December 2019, the first cases of infection with a novel coronavirus, SARS-CoV-2, were
diagnosed. Currently, there is no effective antiviral treatment for COVID-19. To address this …

A single sulfatase is required to access colonic mucin by a gut bacterium

AS Luis, C Jin, GV Pereira, RWP Glowacki, SR Gugel… - Nature, 2021 - nature.com
Humans have co-evolved with a dense community of microbial symbionts that inhabit the
lower intestine. In the colon, secreted mucus creates a barrier that separates these …

Design principles for cyclin K molecular glue degraders

Z Kozicka, DJ Suchyta, V Focht, G Kempf… - Nature chemical …, 2024 - nature.com
Molecular glue degraders are an effective therapeutic modality, but their design principles
are not well understood. Recently, several unexpectedly diverse compounds were reported …

Structural snapshots of TRPV1 reveal mechanism of polymodal functionality

K Zhang, D Julius, Y Cheng - Cell, 2021 - cell.com
Many transient receptor potential (TRP) channels respond to diverse stimuli and
conditionally conduct small and large cations. Such functional plasticity is presumably …

Structural mechanism of cGAS inhibition by the nucleosome

GR Pathare, A Decout, S Glück, S Cavadini… - Nature, 2020 - nature.com
The DNA sensor cyclic GMP–AMP synthase (cGAS) initiates innate immune responses
following microbial infection, cellular stress and cancer. Upon activation by double-stranded …

Visualization of chemical modifications in the human 80S ribosome structure

SK Natchiar, AG Myasnikov, H Kratzat, I Hazemann… - Nature, 2017 - nature.com
Chemical modifications of human ribosomal RNA (rRNA) are introduced during biogenesis
and have been implicated in the dysregulation of protein synthesis, as is found in cancer …

Structural basis for selective binding of m6A RNA by the YTHDC1 YTH domain

C Xu, X Wang, K Liu, IA Roundtree, W Tempel… - Nature chemical …, 2014 - nature.com
Abstract N 6-methyladenosine (m6A) is the most abundant internal modification of nearly all
eukaryotic mRNAs and has recently been reported to be recognized by the YTH domain …