Search Results - "Lim, Herman"

The chemokine receptor CCR8 is not a high-affinity receptor for the human chemokine CCL18 by Hussain, Khansa, Lim, Herman D, Devkota, Shankar Raj, Kemp-Harper, Barbara K, Lane, J Robert, Canals, Meritxell, Pease, James E, Stone, Martin J

“…The primate-specific chemokine CCL18 is a potent chemoattractant for T cells and is expressed at elevated levels in several inflammatory diseases. However, the…”
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Systematic Assessment of Chemokine Signaling at Chemokine Receptors CCR4, CCR7 and CCR10 by Lim, Herman D, Lane, J Robert, Canals, Meritxell, Stone, Martin J

“…Chemokines interact with chemokine receptors in a promiscuous network, such that each receptor can be activated by multiple chemokines. Moreover, different…”
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A Thieno[2,3- d]pyrimidine Scaffold Is a Novel Negative Allosteric Modulator of the Dopamine D 2 Receptor by Fyfe, Tim J, Zarzycka, Barbara, Lim, Herman D, Kellam, Barrie, Mistry, Shailesh N, Katrich, Vsevolod, Scammells, Peter J, Lane, J Robert, Capuano, Ben

“…Recently, a novel negative allosteric modulator (NAM) of the D -like dopamine receptors 1 was identified through virtual ligand screening. This ligand…”
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A Thieno[2,3‑d]pyrimidine Scaffold Is a Novel Negative Allosteric Modulator of the Dopamine D2 Receptor by Fyfe, Tim J, Zarzycka, Barbara, Lim, Herman D, Kellam, Barrie, Mistry, Shailesh N, Katrich, Vsevolod, Scammells, Peter J, Lane, J. Robert, Capuano, Ben

“…Recently, a novel negative allosteric modulator (NAM) of the D2-like dopamine receptors 1 was identified through virtual ligand screening. This ligand…”
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Structure-guided engineering of tick evasins for targeting chemokines in inflammatory diseases by Bhusal, Ram Prasad, Aryal, Pramod, Devkota, Shankar Raj, Pokhrel, Rina, Gunzburg, Menachem J, Foster, Simon R, Lim, Herman D, Payne, Richard J, Wilce, Matthew C J, Stone, Martin J

“…As natural chemokine inhibitors, evasin proteins produced in tick saliva are potential therapeutic agents for numerous inflammatory diseases. Engineering…”
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Key determinants of selective binding and activation by the monocyte chemoattractant proteins at the chemokine receptor CCR2 by Huma, Zil E, Sanchez, Julie, Lim, Herman D, Bridgford, Jessica L, Huang, Cheng, Parker, Bradyn J, Pazhamalil, Jiann G, Porebski, Benjamin T, Pfleger, Kevin D G, Lane, J Robert, Canals, Meritxell, Stone, Martin J

“…Chemokines and their receptors collectively orchestrate the trafficking of leukocytes in normal immune function and inflammatory diseases. Different chemokines…”
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Distinct inactive conformations of the dopamine D2 and D3 receptors correspond to different extents of inverse agonism by Lane, J Robert, Abramyan, Ara M, Adhikari, Pramisha, Keen, Alastair C, Lee, Kuo-Hao, Sanchez, Julie, Verma, Ravi Kumar, Lim, Herman D, Yano, Hideaki, Javitch, Jonathan A, Shi, Lei

“…By analyzing and simulating inactive conformations of the highly homologous dopamine D and D receptors (D R and D R), we find that eticlopride binds D R in a…”
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Molecular and biochemical pharmacology of the histamine H 4 receptor by Leurs, Rob, Chazot, Paul L, Shenton, Fiona C, Lim, Herman D, De Esch, Iwan JP

“…The elucidation of the human genome has had a major impact on histamine receptor research. The identification of the human H 4 receptor by several groups has…”
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Modulating Crystallinity of Poly(3-hexylthiophene) via Microphase Separation of Poly(3-hexylthiophene)–Polyisoprene Block Copolymers by Lim, Herman, Chao, Chi-Yang, Su, Wei-Fang

“…A series of poly­(3-hexylthiophene)-block-polyisoprene (P3HT-b-PI) diblock copolymers (DBCP) and polyisoprene-block-poly­(3-hexylthiophene)-block-polyisoprene…”
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Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole by Klein Herenbrink, Carmen, Verma, Ravi, Lim, Herman D, Kopinathan, Anitha, Keen, Alastair, Shonberg, Jeremy, Draper-Joyce, Christopher J, Scammells, Peter J, Christopoulos, Arthur, Javitch, Jonathan A, Capuano, Ben, Shi, Lei, Lane, J. Robert

“…Partial agonists of the dopamine D2 receptor (D2R) have been developed to treat the symptoms of schizophrenia without causing the side effects elicited by…”
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Fragment Based Design of New H4 Receptor−Ligands with Anti-inflammatory Properties in Vivo by Smits, Rogier A, Lim, Herman D, Hanzer, Agnes, Zuiderveld, Obbe P, Guaita, Elena, Adami, Maristella, Coruzzi, Gabriella, Leurs, Rob, de Esch, Iwan J. P

“…Using a previously reported flexible alignment model we have designed, synthesized, and evaluated a series of compounds at the human histamine H4 receptor…”
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Proof of Concept Study for Designed Multiple Ligands Targeting the Dopamine D2, Serotonin 5‑HT2A, and Muscarinic M1 Acetylcholine Receptors by Szabo, Monika, Lim, Herman D, Klein Herenbrink, Carmen, Christopoulos, Arthur, Lane, J. Robert, Capuano, Ben

“…Herein we describe the hybridization of a benzoxazinone M1 scaffold with D2 privileged structures derived from putative and clinically relevant antipsychotics…”
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Several down, a few to go: histamine H3 receptor ligands making the final push towards the market? by Kuhne, Sebastiaan, Wijtmans, Maikel, Lim, Herman D, Leurs, Rob, de Esch, Iwan J P

“…The histamine H(3) receptor (H(3)R) plays a pivotal role in a plethora of therapeutic areas. Blocking the H(3)R with antagonists/inverse agonists has been…”
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Characterization of the Histamine H4 Receptor Binding Site. Part 1. Synthesis and Pharmacological Evaluation of Dibenzodiazepine Derivatives by Smits, Rogier A, Lim, Herman D, Stegink, Bart, Bakker, Remko A, de Esch, Iwan J. P, Leurs, Rob

“…A series of dibenzodiazepine derivatives was synthesized to probe the binding site of the recently discovered histamine H4 receptor (H4R). Optimization of the…”
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Molecular Determinants of Ligand Binding Modes in the Histamine H4 Receptor: Linking Ligand-Based Three-Dimensional Quantitative Structure–Activity Relationship (3D-QSAR) Models to in Silico Guided Receptor Mutagenesis Studies by Istyastono, Enade P, Nijmeijer, Saskia, Lim, Herman D, van de Stolpe, Andrea, Roumen, Luc, Kooistra, Albert J, Vischer, Henry F, de Esch, Iwan J. P, Leurs, Rob, de Graaf, Chris

“…The histamine H4 receptor (H4R) is a G protein-coupled receptor (GPCR) that plays an important role in inflammation. Similar to the homologous histamine H3…”
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Molecular determinants of ligand binding to H4R species variants by Lim, Herman D, de Graaf, Chris, Jiang, Wen, Sadek, Payman, McGovern, Patricia M, Istyastono, Enade P, Bakker, Remko A, de Esch, Iwan J P, Thurmond, Robin L, Leurs, Rob

“…The histamine H(4) receptor (H(4)R) is the latest identified histamine receptor to emerge as a potential drug target for inflammatory diseases. Animal models…”
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Phenylalanine 169 in the second extracellular loop of the human histamine H4 receptor is responsible for the difference in agonist binding between human and mouse H4 receptors by Lim, Herman D, Jongejan, Aldo, Bakker, Remko A, Haaksma, Eric, de Esch, Iwan J P, Leurs, Rob

“…Using the natural variation in histamine H(4) receptor protein sequence, we tried to identify amino acids involved in the binding of H(4) receptor agonists. To…”
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Cloning and characterization of dominant negative splice variants of the human histamine H4 receptor by van Rijn, Richard M, van Marle, André, Chazot, Paul L, Langemeijer, Ellen, Qin, Yongjun, Shenton, Fiona C, Lim, Herman D, Zuiderveld, Obbe P, Sansuk, Kamonchanok, Dy, Michel, Smit, Martine J, Tensen, Cornelis P, Bakker, Remko A, Leurs, Rob

“…The H(4)R (histamine H(4) receptor) is the latest identified member of the histamine receptor subfamily of GPCRs (G-protein-coupled receptors) with potential…”
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A novel series of histamine H4 receptor antagonists based on the pyrido[3,2-d]pyrimidine scaffold: Comparison of hERG binding and target residence time with PF-3893787 by Andaloussi, Mounir, Lim, Herman D., van der Meer, Tiffany, Sijm, Maarten, Poulie, Chris B.M., de Esch, Iwan J.P., Leurs, Rob, Smits, Rogier A.

“…In this work we describe the optimization of a lead compound based on the quinazoline template to give a new series of potent pyrido[3,2-d]pyrimidines as…”
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Pharmacological characterization of the new histamine H 4 receptor agonist VUF 8430 by Lim, Herman D, Adami, Maristella, Guaita, Elena, Werfel, Thomas, Smits, Rogier A, De Esch, Iwan JP, Bakker, Remko A, Gutzmer, Ralf, Coruzzi, Gabriella, Leurs, Rob

“…Background and purpose:  We compare the pharmacological profiles of a new histamine H 4 receptor agonist 2‐(2‐guanidinoethyl)isothiourea (VUF 8430) with that…”
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