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Ji-Hye Yun et al.
Biochimica et biophysica acta, 1848(6), 1294-1302 (2015-03-11)
The melanocortin receptors (MCRs) are members of the G protein-coupled receptor (GPCR) 1 superfamily with seven transmembrane (TM) domains. Among them, the melanocortin-4 receptor (MC4R) subtype has been highlighted recently by genetic studies in obese humans. In particular, in a
Xiangyu Liu et al.
Cell, 177(5), 1243-1251 (2019-05-14)
The crystal structure of the β2-adrenergic receptor (β2AR) bound to the G protein adenylyl cyclase stimulatory G protein (Gs) captured the complex in a nucleotide-free state (β2AR-Gsempty). Unfortunately, the β2AR-Gsempty complex does not provide a clear explanation for G protein
Fabian Garces et al.
Investigative ophthalmology & visual science, 59(6), 2305-2315 (2018-05-31)
Stargardt disease (STGD1), the most common early-onset recessive macular degeneration, is caused by mutations in the gene encoding the ATP-binding cassette transporter ABCA4. Although extensive genetic studies have identified more than 1000 mutations that cause STGD1 and related ABCA4-associated diseases
Kanako Terakado Kimura et al.
Nature structural & molecular biology, 26(2), 121-128 (2019-02-07)
Many drugs target the serotonin 2A receptor (5-HT2AR), including second-generation antipsychotics that also target the dopamine D2 receptor (D2R). These drugs often produce severe side effects due to non-selective binding to other aminergic receptors. Here, we report the structures of
Xiaofen Liu et al.
PLoS biology, 17(4), e3000096-e3000096 (2019-04-23)
The Orai channel is characterized by voltage independence, low conductance, and high Ca2+ selectivity and plays an important role in Ca2+ influx through the plasma membrane (PM). How the channel is activated and promotes Ca2+ permeation is not well understood.
Nathan Robertson et al.
Nature, 553(7686), 111-114 (2018-01-05)
The complement system is a crucial component of the host response to infection and tissue damage. Activation of the complement cascade generates anaphylatoxins including C5a and C3a. C5a exerts a pro-inflammatory effect via the G-protein-coupled receptor C5a anaphylatoxin chemotactic receptor
Marius M Kostelic et al.
Journal of the American Society for Mass Spectrometry, 30(8), 1416-1425 (2019-04-12)
Native mass spectrometry (MS) has become an important tool for the analysis of membrane proteins. Although detergent micelles are the most commonly used method for solubilizing membrane proteins for native MS, nanoscale lipoprotein complexes such as nanodiscs are emerging as
Guangya Xiang et al.
International journal of pharmaceutics, 356(1-2), 29-36 (2008-02-09)
Folate receptors (FRs) have been identified as cellular surface markers for cancer and leukemia. Liposomes containing lipophilic derivatives of folate have been shown to effectively target FR-expressing cells. Here, we report the synthesis of a novel lipophilic folate derivative, folate-polyethylene
Yanyong Kang et al.
Nature, 558(7711), 553-558 (2018-06-15)
G-protein-coupled receptors comprise the largest family of mammalian transmembrane receptors. They mediate numerous cellular pathways by coupling with downstream signalling transducers, including the hetrotrimeric G proteins Gs (stimulatory) and Gi (inhibitory) and several arrestin proteins. The structural mechanisms that define
Nan Ding et al.
International journal of nanomedicine, 6, 2513-2520 (2011-11-11)
Receptor-targeted delivery of imaging and therapeutic agents can lead to enhanced efficacy for both. Multimodality imaging offers unique advantages over traditional single modality imaging. Tumor marker folate receptor (FR)-targeted fluorescent paramagnetic bimodal liposomes were synthesized to co-deliver paramagnetic and fluorescence
Jun Xu et al.
Molecular cell, 75(1), 53-65 (2019-05-20)
The M2 muscarinic acetylcholine receptor (M2R) is a prototypical GPCR that plays important roles in regulating heart rate and CNS functions. Crystal structures provide snapshots of the M2R in inactive and active states, but the allosteric link between the ligand
Ya Zhu et al.
Acta pharmacologica Sinica, 40(4), 563-568 (2018-06-27)
The chemokine receptor CCR5 is an important anti-HIV (human immunodeficiency virus) drug target owning to its pivotal role in HIV-1 viral entry as a co-receptor. Here, we present a 2.9 Å resolution crystal structure of CCR5 bound to PF-232798, a second-generation
M W Fariss et al.
Cancer research, 54(13), 3346-3351 (1994-07-01)
In the present study we have established that the antitumor activity of alpha-tocopheryl succinate (TS, vitamin E succinate) and cholesteryl succinate (CS) result from the action of the intact TS and CS compounds and not from the release of alpha-tocopherol
Marscha Hirschi et al.
Nature, 550(7676), 411-414 (2017-10-12)
The modulation of ion channel activity by lipids is increasingly recognized as a fundamental component of cellular signalling. The transient receptor potential mucolipin (TRPML) channel family belongs to the TRP superfamily and is composed of three members: TRPML1-TRPML3. TRPMLs are
Neuza Domingues et al.
Biochimica et biophysica acta, 1862(2), 210-220 (2016-10-31)
Cholesteryl hemiesters are oxidation products of polyunsaturated fatty acid esters of cholesterol. Their oxo-ester precursors have been identified as important components of the "core aldehydes" of human atheromata and in oxidized lipoproteins (Ox-LDL). We had previously shown, for the first
Xianqiang Song et al.
Nature, 556(7702), 515-519 (2018-04-20)
The NMDA (N-methyl-D-aspartate) receptor transduces the binding of glutamate and glycine, coupling it to the opening of a calcium-permeable ion channel 1 . Owing to the lack of high-resolution structural studies of the NMDA receptor, the mechanism by which ion-channel blockers
Yi Zheng et al.
Nature, 540(7633), 458-461 (2016-12-08)
CC chemokine receptor 2 (CCR2) is one of 19 members of the chemokine receptor subfamily of human class A G-protein-coupled receptors. CCR2 is expressed on monocytes, immature dendritic cells, and T-cell subpopulations, and mediates their migration towards endogenous CC chemokine
Mi Wang et al.
Drug development and industrial pharmacy, 38(9), 1134-1141 (2011-12-21)
The purpose of this study was to investigate preparation, characterization and tumor-targeted effect of pH-sensitive niosomes, composed of a nonionic surfactant mixed with cholesteryl hemisuccinate (CHEMS), a derivative of cholesterol (CHOL), as a pH-sensitive molecule. CHEMS was synthesized with CHOL
Michael A Goren et al.
Nature communications, 5, 5115-5115 (2014-10-09)
Opsin, the rhodopsin apoprotein, was recently shown to be an ATP-independent flippase (or scramblase) that equilibrates phospholipids across photoreceptor disc membranes in mammalian retina, a process required for disc homoeostasis. Here we show that scrambling is a constitutive activity of
Monique B Ewonkem et al.
Chemistry and physics of lipids, 212, 96-110 (2018-02-07)
Based on ricinoleic acid, two asymmetric bolaamphiphiles with unsymmetrical hydrophobic skeletons and two different hydrophilic head groups were designed and synthesized. The first bola compound had acetylcholine (ACh) and maleimide (MAL) head groups while the second was derived from the
Jiangtao Guo et al.
Nature, 552(7684), 205-209 (2017-12-07)
TRPM4 is a calcium-activated, phosphatidylinositol-4,5-bisphosphate (PtdIns(4,5)P
Benjamin Klasczyk et al.
The journal of physical chemistry. B, 114(46), 14941-14946 (2010-10-28)
Cholesterol hemisuccinate (CHEMS) is a protonable lipid that is frequently used for the construction of pH-responsive delivery systems. Such systems have a stable, lamellar phase at pH 7, but can form a fusogenic, hexagonal phase at pH 5. This behavior
Mohammed Jamshad et al.
Bioscience reports, 35(2) (2015-02-28)
G-protein coupled receptors (GPCRs) constitute the largest class of membrane proteins and are a major drug target. A serious obstacle to studying GPCR structure/function characteristics is the requirement to extract the receptors from their native environment in the plasma membrane
Y Yamamoto et al.
Plant physiology, 67(6), 1069-1072 (1981-06-01)
Cholesteryl hemisuccinate has been incorporated into pea chloroplast thylakoids to investigate the relationship between fluidity and functioning of this membrane system. Levels of sterol which increased the apparent viscosity of the membrane, estimated by fluorescence polarization measurements using the lipophilic
Jongwon Shim et al.
International journal of pharmaceutics, 388(1-2), 251-256 (2010-01-12)
We have studied how the transdermal delivery of lidocaine hydrochloride (LHC) is affected by the morphology of lipid carriers, liposomes and micelles, having the same lipid composition of 1-stearoyl-sn-glycero-3-phosphocholine (LPC) and cholesteryl hemisuccinate (CHEMS). In vitro drug permeation study, carried
Zachary Lee Johnson et al.
Cell, 172(1-2), 81-89 (2018-01-02)
The multidrug resistance protein MRP1 is an ATP-driven pump that confers resistance to chemotherapy. Previously, we have shown that intracellular substrates are recruited to a bipartite binding site when the transporter rests in an inward-facing conformation. A key question remains: how
Yuma Yamada et al.
Mitochondrion, 52, 67-74 (2020-02-26)
The delivery of nucleic acids targeting mutant mtDNA represent a potential strategy for addressing a variety of mitochondria-related diseases. We previously developed a MITO-Porter, a nano carrier that is capable of delivering nanoparticles of nucleic acids to mitochondria of human
Yu-Hsin Chiu et al.
Nature communications, 8, 14324-14324 (2017-01-31)
Pannexin 1 (PANX1) subunits form oligomeric plasma membrane channels that mediate nucleotide release for purinergic signalling, which is involved in diverse physiological processes such as apoptosis, inflammation, blood pressure regulation, and cancer progression and metastasis. Here we explore the mechanistic
Nicholas M I Taylor et al.
Nature, 546(7659), 504-509 (2017-05-30)
ABCG2 is a constitutively expressed ATP-binding cassette (ABC) transporter that protects many tissues against xenobiotic molecules. Its activity affects the pharmacokinetics of commonly used drugs and limits the delivery of therapeutics into tumour cells, thus contributing to multidrug resistance. Here
Seungkirl Ahn et al.
Molecular pharmacology, 94(2), 850-861 (2018-05-18)
Conventional drug discovery efforts at the β2-adrenoceptor (β2AR) have led to the development of ligands that bind almost exclusively to the receptor's hormone-binding orthosteric site. However, targeting the largely unexplored and evolutionarily unique allosteric sites has potential for developing more
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