Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine
Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …
small-molecule probes. These molecular tools have been widely applied for interrogating …
Activity-based protein profiling: Recent advances in medicinal chemistry
H Deng, Q Lei, Y Wu, Y He, W Li - European journal of medicinal chemistry, 2020 - Elsevier
Activity-based protein profiling (ABPP) has become an emerging chemical proteomic
approach to illustrate the interaction mechanisms between compounds and proteins. This …
approach to illustrate the interaction mechanisms between compounds and proteins. This …
LPCAT3 inhibitors remodel the polyunsaturated phospholipid content of human cells and protect from ferroptosis
LPCAT3 is an integral membrane acyltransferase in the Lands cycle responsible for
generating C20: 4 phospholipids and has been implicated in key biological processes such …
generating C20: 4 phospholipids and has been implicated in key biological processes such …
Three-dimensional bioprinted glioblastoma microenvironments model cellular dependencies and immune interactions
Brain tumors are dynamic complex ecosystems with multiple cell types. To model the brain
tumor microenvironment in a reproducible and scalable system, we developed a rapid three …
tumor microenvironment in a reproducible and scalable system, we developed a rapid three …
Specific binding of GPR174 by endogenous lysophosphatidylserine leads to high constitutive Gs signaling
Y Nie, Z Qiu, S Chen, Z Chen, X Song, Y Ma… - Nature …, 2023 - nature.com
Many orphan G protein-coupled receptors (GPCRs) remain understudied because their
endogenous ligands are unknown. Here, we show that a group of class A/rhodopsin-like …
endogenous ligands are unknown. Here, we show that a group of class A/rhodopsin-like …
Biomimetic synthesis and chemical proteomics reveal the mechanism of action and functional targets of phloroglucinol meroterpenoids
AK Bracken, CE Gekko, NO Suss… - Journal of the …, 2024 - ACS Publications
Natural products perennially serve as prolific sources of drug leads and chemical probes,
fueling the development of numerous therapeutics. Despite their scarcity, natural products …
fueling the development of numerous therapeutics. Despite their scarcity, natural products …
High-throughput screening for the discovery of enzyme inhibitors
MD Lloyd - Journal of Medicinal Chemistry, 2020 - ACS Publications
Enzymes are common targets in high-throughput screening and related campaigns. An
analysis of papers published between 1990 and 2018 showed that kinases were the most …
analysis of papers published between 1990 and 2018 showed that kinases were the most …
ABHD10 is an S-depalmitoylase affecting redox homeostasis through peroxiredoxin-5
S-Palmitoylation is a reversible lipid post-translational modification that has been observed
on mitochondrial proteins, but both the regulation and functional consequences of …
on mitochondrial proteins, but both the regulation and functional consequences of …
Lysophosphatidylserine: A Signaling Lipid with Implications in Human Diseases
Lysophosphatidylserine (lyso-PS) has emerged as yet another important signaling
lysophospholipid in mammals, and deregulation in its metabolism has been directly linked to …
lysophospholipid in mammals, and deregulation in its metabolism has been directly linked to …
Positron emission tomography imaging of the endocannabinoid system: opportunities and challenges in radiotracer development
The endocannabinoid system (ECS) is involved in a wide range of biological functions and
comprises cannabinoid receptors and enzymes responsible for endocannabinoid synthesis …
comprises cannabinoid receptors and enzymes responsible for endocannabinoid synthesis …