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Article ; Online: Targeting the m

Burgess, Hannah M / Depledge, Daniel P / Thompson, Letitia / Srinivas, Kalanghad Puthankalam / Grande, Rebecca C / Vink, Elizabeth I / Abebe, Jonathan S / Blackaby, Wesley P / Hendrick, Alan / Albertella, Mark R / Kouzarides, Tony / Stapleford, Kenneth A / Wilson, Angus C / Mohr, Ian

Genes & development

2021 Volume 35, Issue 13-14, Page(s) 1005–1019

Abstract: ... ...

Abstract	N
MeSH term(s)	Adenosine/analogs & derivatives ; Adenosine/genetics ; Adenosine/metabolism ; Cell Line ; Coronavirus Infections/metabolism ; Coronavirus Infections/virology ; Coronavirus OC43, Human/physiology ; Gene Expression Regulation/drug effects ; Host-Pathogen Interactions/drug effects ; Humans ; Methyltransferases/antagonists & inhibitors ; Methyltransferases/metabolism ; Nucleocapsid Proteins ; RNA Processing, Post-Transcriptional/genetics ; RNA, Viral/metabolism ; RNA-Binding Proteins/metabolism ; SARS-CoV-2/physiology ; Virus Replication/drug effects ; Virus Replication/genetics
Chemical Substances	Nucleocapsid Proteins ; RNA, Viral ; RNA-Binding Proteins ; YTHDF1 protein, human ; YTHDF3 protein, human ; N-methyladenosine (CLE6G00625) ; Methyltransferases (EC 2.1.1.-) ; METTL3 protein, human (EC 2.1.1.62) ; Adenosine (K72T3FS567)
Language	English
Publishing date	2021-06-24
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	806684-x
ISSN	1549-5477 ; 0890-9369
ISSN (online)	1549-5477
ISSN	0890-9369
DOI	10.1101/gad.348320.121
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Zs.A 2292: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular Jg. 1995 - 2021: Lesesall (2.OG) ab Jg. 2022: Lesesaal (EG)
Zs.MG 54: Show issues

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Article ; Online: Role of Conserved Tyrosine Lid Residues in the Activation of the M

Pham, Vi / Habben Jansen, Maria Clazina Cornelia / Thompson, Geoff / Heitman, Laura H / Christopoulos, Arthur / Thal, David M / Valant, Celine

Molecular pharmacology

2023 Volume 104, Issue 3, Page(s) 92–104

Abstract: The development of subtype selective small molecule drugs for the muscarinic acetylcholine receptor (mAChR) family has been challenging. The design of more selective ligands can be improved by understanding the structure and function of key amino acid ... ...

Abstract	The development of subtype selective small molecule drugs for the muscarinic acetylcholine receptor (mAChR) family has been challenging. The design of more selective ligands can be improved by understanding the structure and function of key amino acid residues that line ligand binding sites. Here we study the role of three conserved key tyrosine residues [Y104
MeSH term(s)	Humans ; Ligands ; Muscarinic Agonists/pharmacology ; Tyrosine ; Receptors, Muscarinic ; Allosteric Site ; Allosteric Regulation/physiology ; Receptor, Muscarinic M1 ; Receptor, Muscarinic M2/genetics ; Receptor, Muscarinic M2/metabolism
Chemical Substances	Ligands ; Muscarinic Agonists ; Tyrosine (42HK56048U) ; Receptors, Muscarinic ; Receptor, Muscarinic M1 ; Receptor, Muscarinic M2
Language	English
Publishing date	2023-06-22
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	124034-1
ISSN	1521-0111 ; 0026-895X
ISSN (online)	1521-0111
ISSN	0026-895X
DOI	10.1124/molpharm.122.000661
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Zs.A 525: Show issues

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Article ; Online: Challenges to mapping and defining m

Horner, Stacy M / Thompson, Matthew G

RNA (New York, N.Y.)

2024 Volume 30, Issue 5, Page(s) 482–490

Abstract: ... beyond the primary sequence, such as RNA structures and RNA modifications, including N6-methyladenosine (m ...

Abstract	Viral RNA molecules contain multiple layers of regulatory information. This includes features beyond the primary sequence, such as RNA structures and RNA modifications, including N6-methyladenosine (m
MeSH term(s)	Humans ; RNA, Viral/genetics ; RNA, Viral/metabolism ; Virus Replication/genetics ; RNA/genetics ; Viruses/genetics ; Virus Diseases
Chemical Substances	RNA, Viral ; RNA (63231-63-0)
Language	English
Publishing date	2024-04-16
Publishing country	United States
Document type	Journal Article
ZDB-ID	1241540-6
ISSN	1469-9001 ; 1355-8382
ISSN (online)	1469-9001
ISSN	1355-8382
DOI	10.1261/rna.079959.124
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Zs.A 4777: Show issues

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Article ; Online: Identification of a Novel Allosteric Site at the M

Burger, Wessel A C / Gentry, Patrick R / Berizzi, Alice E / Vuckovic, Ziva / van der Westhuizen, Emma T / Thompson, Geoff / Yeasmin, Mahmuda / Lindsley, Craig W / Sexton, Patrick M / Langmead, Christopher J / Tobin, Andrew B / Christopoulos, Arthur / Valant, Celine / Thal, David M

ACS chemical neuroscience

2021 Volume 12, Issue 16, Page(s) 3112–3123

Abstract: The M ...

Abstract	The M
MeSH term(s)	Allosteric Regulation ; Allosteric Site ; Binding Sites ; Molecular Docking Simulation ; Receptor, Muscarinic M1/genetics ; Receptor, Muscarinic M4 ; Receptors, Muscarinic/genetics
Chemical Substances	Receptor, Muscarinic M1 ; Receptor, Muscarinic M4 ; Receptors, Muscarinic
Language	English
Publishing date	2021-08-05
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1948-7193
ISSN (online)	1948-7193
DOI	10.1021/acschemneuro.1c00383
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Biased Profile of Xanomeline at the Recombinant Human M

McDonald, Jack K / van der Westhuizen, Emma T / Pham, Vi / Thompson, Geoff / Felder, Christian C / Paul, Steven M / Thal, David M / Christopoulos, Arthur / Valant, Celine

ACS chemical neuroscience

2022 Volume 13, Issue 8, Page(s) 1206–1218

Abstract: ... in particular, the M ...

Abstract	Many Food and Drug Administration (FDA)-approved drugs are structural analogues of the endogenous (natural) ligands of G protein-coupled receptors (GPCRs). However, it is becoming appreciated that chemically distinct ligands can bind to GPCRs in conformations that lead to different cellular signaling events, a phenomenon termed biased agonism. Despite this, the rigorous experimentation and analysis required to identify biased agonism are often not undertaken in most clinical candidates and go unrealized. Recently, xanomeline, a muscarinic acetylcholine receptor (mAChR) agonist, has entered phase III clinical trials for the treatment of schizophrenia. If successful, xanomeline will be the first novel FDA-approved antipsychotic drug in almost 50 years. Intriguingly, xanomeline's potential for biased agonism at the mAChRs and, in particular, the M
MeSH term(s)	Acetylcholine/metabolism ; Acetylcholine/pharmacology ; Animals ; CHO Cells ; Calcium ; Cricetinae ; Cricetulus ; Humans ; Ligands ; Muscarinic Agonists/pharmacology ; Muscarinic Agonists/therapeutic use ; Pyridines ; Receptor, Muscarinic M1/agonists ; Receptor, Muscarinic M4/agonists ; Receptors, G-Protein-Coupled ; Receptors, Muscarinic ; Thiadiazoles/chemistry
Chemical Substances	Ligands ; Muscarinic Agonists ; Pyridines ; Receptor, Muscarinic M1 ; Receptor, Muscarinic M4 ; Receptors, G-Protein-Coupled ; Receptors, Muscarinic ; Thiadiazoles ; xanomeline (9ORI6L73CJ) ; Acetylcholine (N9YNS0M02X) ; Calcium (SY7Q814VUP)
Language	English
Publishing date	2022-04-05
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1948-7193
ISSN (online)	1948-7193
DOI	10.1021/acschemneuro.1c00827
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Programmable protein expression using a genetically encoded m

Marayati, Bahjat F / Thompson, Matthew G / Holley, Christopher L / Horner, Stacy M / Meyer, Kate D

Nature biotechnology

2024

Abstract: ... The ... ...

Abstract	The N
Language	English
Publishing date	2024-01-02
Publishing country	United States
Document type	Journal Article
ZDB-ID	1311932-1
ISSN	1546-1696 ; 1087-0156
ISSN (online)	1546-1696
ISSN	1087-0156
DOI	10.1038/s41587-023-01978-3
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Zs.A 2167: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular Jg. 1995 - 2021: Lesesall (1.OG) ab Jg. 2022: Lesesaal (EG)
Zs.MO 137: Show issues
Zs.MG 43: Show issues

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Article ; Online: Crystal structure of the M

Vuckovic, Ziva / Gentry, Patrick R / Berizzi, Alice E / Hirata, Kunio / Varghese, Swapna / Thompson, Geoff / van der Westhuizen, Emma T / Burger, Wessel A C / Rahmani, Raphaël / Valant, Celine / Langmead, Christopher J / Lindsley, Craig W / Baell, Jonathan B / Tobin, Andrew B / Sexton, Patrick M / Christopoulos, Arthur / Thal, David M

Proceedings of the National Academy of Sciences of the United States of America

2019 Volume 116, Issue 51, Page(s) 26001–26007

Abstract: The human M ...

Abstract	The human M
MeSH term(s)	Allosteric Regulation ; Allosteric Site ; Binding Sites ; Crystallization ; Drug Design ; Humans ; Kinetics ; Ligands ; Models, Molecular ; Protein Conformation ; Receptor, Muscarinic M5/chemistry ; Receptor, Muscarinic M5/genetics ; Receptor, Muscarinic M5/metabolism ; Receptors, Muscarinic/chemistry ; X-Ray Diffraction
Chemical Substances	Ligands ; Receptor, Muscarinic M5 ; Receptors, Muscarinic
Language	English
Publishing date	2019-11-26
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	209104-5
ISSN	1091-6490 ; 0027-8424
ISSN (online)	1091-6490
ISSN	0027-8424
DOI	10.1073/pnas.1914446116
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Zs.A 1148: Show issues

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Article ; Online: Bitopic Binding Mode of an M

Bradley, Sophie J / Molloy, Colin / Bundgaard, Christoffer / Mogg, Adrian J / Thompson, Karen J / Dwomoh, Louis / Sanger, Helen E / Crabtree, Michael D / Brooke, Simon M / Sexton, Patrick M / Felder, Christian C / Christopoulos, Arthur / Broad, Lisa M / Tobin, Andrew B / Langmead, Christopher J

Molecular pharmacology

2018 Volume 93, Issue 6, Page(s) 645–656

Abstract: The realization of the therapeutic potential of targeting the M ...

Abstract	The realization of the therapeutic potential of targeting the M
MeSH term(s)	Acetylcholine/metabolism ; Allosteric Regulation/drug effects ; Allosteric Site/drug effects ; Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Animals ; Benzimidazoles/pharmacology ; Binding Sites/drug effects ; CHO Cells ; Cell Line ; Clinical Trials as Topic ; Cricetinae ; Cricetulus ; Humans ; Learning/drug effects ; Male ; Memory/drug effects ; Mice ; Mice, Inbred C57BL ; Muscarinic Agonists/pharmacology ; Protein Binding/drug effects ; Rats ; Rats, Wistar ; Receptor, Muscarinic M1/metabolism ; Receptors, Muscarinic/metabolism
Chemical Substances	Benzimidazoles ; GSK 1034702 ; Muscarinic Agonists ; Receptor, Muscarinic M1 ; Receptors, Muscarinic ; benzimidazol-2-one (43135-91-7) ; Acetylcholine (N9YNS0M02X)
Language	English
Publishing date	2018-04-25
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	124034-1
ISSN	1521-0111 ; 0026-895X
ISSN (online)	1521-0111
ISSN	0026-895X
DOI	10.1124/mol.118.111872
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Zs.A 525: Show issues

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Article ; Online: Dual Inhibitors of Main Protease (M

Mondal, Santanu / Chen, Yongzhi / Lockbaum, Gordon J / Sen, Sudeshna / Chaudhuri, Sauradip / Reyes, Archie C / Lee, Jeong Min / Kaur, Arshia N / Sultana, Nadia / Cameron, Michael D / Shaffer, Scott A / Schiffer, Celia A / Fitzgerald, Katherine A / Thompson, Paul R

Journal of the American Chemical Society

2022 Volume 144, Issue 46, Page(s) 21035–21045

Abstract: ... economy, the development of direct acting antivirals is of paramount importance. Main protease (M ...

Abstract	Given the current impact of SARS-CoV2 and COVID-19 on human health and the global economy, the development of direct acting antivirals is of paramount importance. Main protease (M
MeSH term(s)	Animals ; Mice ; Humans ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; Antiviral Agents/chemistry ; Coronavirus 3C Proteases ; Cathepsin L/chemistry ; Cathepsin L/metabolism ; RNA, Viral ; SARS-CoV-2 ; Protease Inhibitors/pharmacology ; Protease Inhibitors/therapeutic use ; Protease Inhibitors/chemistry ; Peptide Hydrolases ; Proteomics ; Viral Nonstructural Proteins/chemistry ; Molecular Docking Simulation ; Hepatitis C, Chronic ; COVID-19 Drug Treatment
Chemical Substances	Antiviral Agents ; Coronavirus 3C Proteases (EC 3.4.22.28) ; Cathepsin L (EC 3.4.22.15) ; RNA, Viral ; Protease Inhibitors ; Peptide Hydrolases (EC 3.4.-) ; Viral Nonstructural Proteins
Language	English
Publishing date	2022-11-10
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural
ZDB-ID	3155-0
ISSN	1520-5126 ; 0002-7863
ISSN (online)	1520-5126
ISSN	0002-7863
DOI	10.1021/jacs.2c04626
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Z 4' 55/32: Show issues
Z 7.3: Show issues

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Article: MK-7622: A First-in-Class M

Beshore, Douglas C / N Di Marco, Christina / Chang, Ronald K / Greshock, Thomas J / Ma, Lei / Wittmann, Marion / Seager, Matthew A / Koeplinger, Kenneth A / Thompson, Charles D / Fuerst, Joy / Hartman, George D / Bilodeau, Mark T / Ray, William J / Kuduk, Scott D

ACS medicinal chemistry letters

2018 Volume 9, Issue 7, Page(s) 652–656

Abstract: Identification of ligands that selectively activate the M ...

Abstract	Identification of ligands that selectively activate the M
Language	English
Publishing date	2018-04-30
Publishing country	United States
Document type	Journal Article
ISSN	1948-5875
ISSN	1948-5875
DOI	10.1021/acsmedchemlett.8b00095
Database	MEDical Literature Analysis and Retrieval System OnLINE

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