Untangling the web of 5-lipoxygenase-derived products from a molecular and structural perspective: the battle between pro-and anti-inflammatory lipid mediators

NC Gilbert, ME Newcomer, O Werz - Biochemical pharmacology, 2021 - Elsevier
Arachidonic acid (AA) is the precursor to leukotrienes (LT), potent mediators of the
inflammatory response. In the 35+ years since cysteinyl-LTs were reported to mediate …

Structures of leukotriene biosynthetic enzymes and development of new therapeutics

JZ Haeggström, ME Newcomer - Annual review of …, 2023 - annualreviews.org
Leukotrienes are potent immune-regulating lipid mediators with patho-genic roles in
inflammatory and allergic diseases, particularly asthma. These autacoids also contribute to …

Structural identification of lysophosphatidylcholines as activating ligands for orphan receptor GPR119

P Xu, S Huang, S Guo, Y Yun, X Cheng, X He… - Nature Structural & …, 2022 - nature.com
Lysophosphatidylcholine (LPC) is an essential mediator in human lipid metabolism and is
associated with a variety of diseases, but the exact identity of LPC receptors remains …

Biasing AlphaFold2 to predict GPCRs and kinases with user-defined functional or structural properties

D Sala, PW Hildebrand, J Meiler - Frontiers in Molecular Biosciences, 2023 - frontiersin.org
Determining the three-dimensional structure of proteins in their native functional states has
been a longstanding challenge in structural biology. While integrative structural biology has …

Structural basis of leukotriene B4 receptor 1 activation

N Wang, X He, J Zhao, H Jiang, X Cheng, Y Xia… - Nature …, 2022 - nature.com
Abstract Leukotriene B4 receptor 1 (BLT1) plays crucial roles in the acute inflammatory
responses and is a valuable target for anti-inflammation treatment, however, the mechanism …

Recent advances in function and structure of two leukotriene B4 receptors: BLT1 and BLT2

M Nakamura, T Shimizu - Biochemical Pharmacology, 2022 - Elsevier
Abstract Leukotriene B 4 (LTB 4) is generated by the enzymatic oxidation of arachidonic
acid, which is then released from the cell membrane and acts as a potent activator of …

Therapeutic target of leukotriene B4 receptors, BLT1 and BLT2: Insights from basic research

M Nakamura, T Shimizu - Biochimie, 2023 - Elsevier
Abstract Leukotriene B 4 (LTB 4) is a lipid mediator rapidly generated from arachidonic acid
in response to various stimuli. This lipid mediator exerts its biological activities by binding to …

Recent advances in structure, function, and pharmacology of class A lipid GPCRs: opportunities and challenges for drug discovery

RNV Krishna Deepak, RK Verma, YD Hartono… - Pharmaceuticals, 2021 - mdpi.com
Great progress has been made over the past decade in understanding the structural,
functional, and pharmacological diversity of lipid GPCRs. From the first determination of the …

[HTML][HTML] Structural diversity of leukotriene G-protein coupled receptors

A Luginina, A Gusach, E Lyapina, P Khorn… - Journal of Biological …, 2023 - Elsevier
Dihydroxy acid leukotriene (LTB 4) and cysteinyl leukotrienes (LTC 4, LTD 4, and LTE 4) are
inflammatory mediators derived from arachidonic acid via the 5-lipoxygenase pathway …

Stepwise phosphorylation of BLT1 defines complex assemblies with β‐arrestin serving distinct functions

R Tatsumi, S Aihara, S Matsune, J Aoki… - The FASEB …, 2023 - Wiley Online Library
G protein‐coupled receptors (GPCRs) utilize complex cellular systems to respond to diverse
ligand concentrations. By taking BLT1, a GPCR for leukotriene B4 (LTB4), as a model, our …