Targeting cancer with small-molecule pan-KRAS degraders

J Popow, W Farnaby, A Gollner, C Kofink, G Fischer… - Science, 2024 - science.org
Mutations in the Kirsten rat sarcoma viral oncogene homolog (KRAS) protein are highly
prevalent in cancer. However, small-molecule concepts that address oncogenic KRAS …

Cleavage-independent activation of ancient eukaryotic gasdermins and structural mechanisms

Y Li, Y Hou, Q Sun, H Zeng, F Meng, X Tian, Q He… - Science, 2024 - science.org
Gasdermins (GSDMs) are pore-forming proteins that execute pyroptosis for immune
defense. GSDMs are two-domain proteins activated by proteolytic removal of the inhibitory …

Gut microbial β-glucuronidases influence endobiotic homeostasis and are modulated by diverse therapeutics

JB Simpson, ME Walker, JJ Sekela, SM Ivey… - Cell Host & Microbe, 2024 - cell.com
Hormones and neurotransmitters are essential to homeostasis, and their disruptions are
connected to diseases ranging from cancer to anxiety. The differential reactivation of …

VISTA checkpoint inhibition by pH-selective antibody SNS-101 with optimized safety and pharmacokinetic profiles enhances PD-1 response

T Thisted, FD Smith, A Mukherjee, Y Kleschenko… - Nature …, 2024 - nature.com
VISTA, an inhibitory myeloid-T-cell checkpoint, holds promise as a target for cancer
immunotherapy. However, its effective targeting has been impeded by issues such as rapid …

Photosensitization enables Pauson-Khand–type reactions with nitrenes

F Li, WF Zhu, C Empel, O Datsenko, A Kumar, Y Xu… - Science, 2024 - science.org
The Pauson-Khand reaction has in the past 50 years become one of the most common
cycloaddition reactions in chemistry. Coupling two unsaturated bonds with carbon …

Spike structures, receptor binding, and immune escape of recently circulating SARS-CoV-2 Omicron BA. 2.86, JN. 1, EG. 5, EG. 5.1, and HV. 1 sub-variants

L Li, K Shi, Y Gu, Z Xu, C Shu, D Li, J Sun, M Cong, X Li… - Structure, 2024 - cell.com
Summary The recently emerged BA. 2.86, JN. 1, EG. 5, EG. 5.1, and HV. 1 variants have a
growth advantage. In this study, we explore the structural bases of receptor binding and …

Drug repurposing screen identifies lonafarnib as respiratory syncytial virus fusion protein inhibitor

SM Sake, X Zhang, MK Rajak… - Nature …, 2024 - nature.com
Respiratory syncytial virus (RSV) is a common cause of acute lower respiratory tract
infection in infants, older adults and the immunocompromised. Effective directly acting …

Post-translational modifications in the Protein Data Bank

LC Schofield, JS Dialpuri, GN Murshudov… - Biological …, 2024 - journals.iucr.org
Proteins frequently undergo covalent modification at the post-translational level, which
involves the covalent attachment of chemical groups onto amino acids. This can entail the …

XDSGUI: a graphical user interface for XDS, SHELX and ARCIMBOLDO

W Brehm, J Triviño, JM Krahn, I Usón… - Applied …, 2023 - journals.iucr.org
XDSGUI is a lightweight graphical user interface (GUI) for the XDS, SHELX and
ARCIMBOLDO program packages that serves both novice and experienced users in …

AlphaFold two years on: Validation and impact

O Kovalevskiy, J Mateos-Garcia… - Proceedings of the …, 2024 - pnas.org
Two years on from the initial release of AlphaFold, we have seen its widespread adoption as
a structure prediction tool. Here, we discuss some of the latest work based on AlphaFold …