The emerging role of mass spectrometry-based proteomics in drug discovery

F Meissner, J Geddes-McAlister, M Mann… - Nature Reviews Drug …, 2022 - nature.com
Proteins are the main targets of most drugs; however, system-wide methods to monitor
protein activity and function are still underused in drug discovery. Novel biochemical …

Targeted Covalent Modification Strategies for Drugging the Undruggable Targets

T Tamura, M Kawano, I Hamachi - Chemical Reviews, 2025 - ACS Publications
The term “undruggable” refers to proteins or other biological targets that have been
historically challenging to target with conventional drugs or therapeutic strategies because …

Synthesis of portimines reveals the basis of their anti-cancer activity

J Tang, W Li, TY Chiu, F Martínez-Peña, Z Luo… - Nature, 2023 - nature.com
Marine-derived cyclic imine toxins, portimine A and portimine B, have attracted attention
because of their chemical structure and notable anti-cancer therapeutic potential …

Enhanced mapping of small-molecule binding sites in cells

JM Wozniak, W Li, P Governa, LY Chen… - Nature Chemical …, 2024 - nature.com
Photoaffinity probes are routinely utilized to identify proteins that interact with small
molecules. However, despite this common usage, resolving the specific sites of these …

Evaluation of fully-functionalized diazirine tags for chemical proteomic applications

LP Conway, AM Jadhav, RA Homan, W Li… - Chemical …, 2021 - pubs.rsc.org
The use of photo-affinity reagents for the mapping of noncovalent small molecule–protein
interactions has become widespread. Recently, several 'fully-functionalized'(FF) chemical …

Structural and functional annotation of solute carrier transporters: implication for drug discovery

V Dvorak, G Superti-Furga - Expert Opinion on Drug Discovery, 2023 - Taylor & Francis
ABSTRACT Introduction Solute carriers (SLCs) represent the largest group of membrane
transporters in the human genome. They play a central role in controlling the …

Modes‐of‐action of antifungal compounds: Stressors and (target‐site‐specific) toxins, toxicants, or toxin–stressors

D Noel, JE Hallsworth, E Gelhaye… - Microbial …, 2023 - Wiley Online Library
Fungi and antifungal compounds are relevant to the United Nation's Sustainable
Development Goals. However, the modes‐of‐action of antifungals—whether they are …

Lysophosphatidylserine: A Signaling Lipid with Implications in Human Diseases

A Chakraborty, SS Kamat - Chemical Reviews, 2024 - ACS Publications
Lysophosphatidylserine (lyso-PS) has emerged as yet another important signaling
lysophospholipid in mammals, and deregulation in its metabolism has been directly linked to …

The 5-formyl-tetrahydrofolate proteome links folates with C/N metabolism and reveals feedback regulation of folate biosynthesis

W Li, Q Liang, RC Mishra, R Sanchez-Muñoz… - The Plant …, 2021 - academic.oup.com
Folates are indispensable for plant development, but their molecular mode of action remains
elusive. We synthesized a probe,“5-F-THF-Dayne,” comprising 5-formyl-tetrahydrofolate …

Novel Covalent Probe Selectively Targeting Glutathione Peroxidase 4 In Vivo: Potential Applications in Pancreatic Cancer Therapy

Z Tang, J Li, L Peng, F Xu, Y Tan, X He… - Journal of Medicinal …, 2024 - ACS Publications
Glutathione peroxidase 4 (GPX4) emerges as a promising target for the treatment of therapy-
resistant cancer through ferroptosis. Thus, there is a broad interest in the development of …