Emerging degrader technologies engaging lysosomal pathways
Targeted protein degradation (TPD) provides unprecedented opportunities for drug
discovery. While the proteolysis-targeting chimera (PROTAC) technology has already …
discovery. While the proteolysis-targeting chimera (PROTAC) technology has already …
Applications and prospects of cryo-EM in drug discovery
KF Zhu, C Yuan, YM Du, KL Sun, XK Zhang… - Military Medical …, 2023 - Springer
Drug discovery is a crucial part of human healthcare and has dramatically benefited human
lifespan and life quality in recent centuries, however, it is usually time-and effort-consuming …
lifespan and life quality in recent centuries, however, it is usually time-and effort-consuming …
Mechanistic understanding of human SLFN11
FJ Metzner, SJ Wenzl, M Kugler, S Krebs… - Nature …, 2022 - nature.com
Abstract Schlafen 11 (SLFN11) is an interferon-inducible antiviral restriction factor with tRNA
endoribonuclease and DNA binding functions. It is recruited to stalled replication forks in …
endoribonuclease and DNA binding functions. It is recruited to stalled replication forks in …
Developing an anticancer platinum (II) compound based on the uniqueness of human serum albumin
Z Zhang, J Zhang, T Yang, S Li, G Xu… - Journal of Medicinal …, 2023 - ACS Publications
To develop the next-generation Pt drug with remarkable activity and low toxicity to maximally
inhibit tumor growth, we optimized a Pt (II) thiosemicarbazone compound (C4) with …
inhibit tumor growth, we optimized a Pt (II) thiosemicarbazone compound (C4) with …
Structural, molecular, and functional insights into Schlafen proteins
Schlafen (SLFN) genes belong to a vertebrate gene family encoding proteins with high
sequence homology. However, each SLFN is functionally divergent and differentially …
sequence homology. However, each SLFN is functionally divergent and differentially …
Velcrin-induced selective cleavage of tRNALeu(TAA) by SLFN12 causes cancer cell death
Velcrin compounds kill cancer cells expressing high levels of phosphodiesterase 3A
(PDE3A) and Schlafen family member 12 (SLFN12) by inducing complex formation between …
(PDE3A) and Schlafen family member 12 (SLFN12) by inducing complex formation between …
Facilitating the development of molecular glues: opportunities from serendipity and rational design
W Jiang, Y Jiang, Y Luo, W Qiao, T Yang - European Journal of Medicinal …, 2024 - Elsevier
Molecular glues can specifically induce interactions between two or more proteins to
modulate biological functions and have been proven to be a powerful therapeutic modality …
modulate biological functions and have been proven to be a powerful therapeutic modality …
Molecular glues: capable protein-binding small molecules that can change protein–protein interactions and interactomes for the potential treatment of human cancer …
F Li, IAM Aljahdali, X Ling - International Journal of Molecular Sciences, 2022 - mdpi.com
Molecular glue (MG) compounds are a type of unique small molecule that can change the
protein–protein interactions (PPIs) and interactomes by degrading, stabilizing, or activating …
protein–protein interactions (PPIs) and interactomes by degrading, stabilizing, or activating …
Recent advances in automated structure-based de novo drug design
As the number of determined and predicted protein structures and the size of druglike 'make-
on-demand'libraries soar, the time-consuming nature of structure-based computer-aided …
on-demand'libraries soar, the time-consuming nature of structure-based computer-aided …
Schlafen 12 restricts HIV-1 latency reversal by a codon-usage dependent post-transcriptional block in CD4+ T cells
M Kobayashi-Ishihara, K Frazão Smutná… - Communications …, 2023 - nature.com
Latency is a major barrier towards virus elimination in HIV-1-infected individuals. Yet, the
mechanisms that contribute to the maintenance of HIV-1 latency are incompletely …
mechanisms that contribute to the maintenance of HIV-1 latency are incompletely …