Christopher Langmead

Dr

20012020

Research output per year

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Research Output

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Article
2020

Acetylcholine Muscarinic M4 Receptors as a Therapeutic Target for Alcohol Use Disorder: Converging Evidence From Humans and Rodents

Walker, L. C., Berizzi, A. E., Chen, N. A., Rueda, P., Perreau, V. M., Huckstep, K., Srisontiyakul, J., Govitrapong, P., Xiaojian, J., Lindsley, C. W., Jones, C. K., Riddy, D. M., Christopoulos, A., Langmead, C. J. & Lawrence, A. J., 28 Feb 2020, (Accepted/In press) In : Biological Psychiatry. 12 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Negative allosteric modulators of the human calcium-sensing receptor bind to overlapping and distinct sites within the 7-transmembrane domain

Josephs, T. M., Keller, A. N., Khajehali, E., DeBono, A., Langmead, C. J., Conigrave, A. D., Capuano, B., Kufareva, I., Gregory, K. J. & Leach, K., Apr 2020, In : British Journal of Pharmacology. 177, 8, p. 1917-1930 14 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)
2019

Crystal structure of the M5 muscarinic acetylcholine receptor

Vuckovic, Z., Gentry, P. R., Berizzi, A. E., Hirata, K., Varghese, S., Thompson, G., van der Westhuizen, E. T., Burger, W. A. C., Rahmani, R., Valant, C., Langmead, C. J., Lindsley, C. W., Baell, J. B., Tobin, A. B., Sexton, P. M., Christopoulos, A. & Thal, D. M., 17 Dec 2019, In : Proceedings of the National Academy of Sciences of the United States of America. 116, 51, p. 26001-26007 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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3 Citations (Scopus)

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H3 receptor antagonists

Riddy, D. M., Cook, A. E., Shackleford, D. M., Pierce, T. L., Mocaer, E., Mannoury la Cour, C., Sors, A., Charman, W. N., Summers, R. J., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Jan 2019, In : Neuropharmacology. 144, p. 244-255 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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7 Citations (Scopus)
2018

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes S

Bradley, S. J., Molloy, C., Bundgaard, C., Mogg, A. J., Thompson, K. J., Dwomoh, L., Sanger, H. E., Crabtree, M. D., Brooke, S. M., Sexton, P. M., Felder, C. C., Christopoulos, A., Broad, L. M., Tobin, A. B. & Langmead, C. J., 1 Jun 2018, In : Molecular Pharmacology. 93, 6, p. 645-656 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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10 Citations (Scopus)

Comparative genotypic and phenotypic analysis of human peripheral blood monocytes and surrogate monocyte-like cell lines commonly used in metabolic disease research

Riddy, D. M., Goy, E., Delerive, P., Summers, R. J. & Langmead, C. J., 1 May 2018, In : PLoS ONE. 13, 5, 19 p., e0197177.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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5 Citations (Scopus)

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold

Bender, A. M., Cho, H. P., Nance, K. D., Lingenfelter, K. S., Luscombe, V. B., Gentry, P. R., Voigtritter, K., Berizzi, A. E., Sexton, P. M., Langmead, C. J., Christopoulos, A., Locuson, C. W., Bridges, T. M., Chang, S., O'Neill, J. C., Zhan, X., Niswender, C. M., Jones, C. K., Conn, P. J. & Lindsley, C. W., 18 Jul 2018, In : ACS Chemical Neuroscience. 9, 7, p. 1572-1581 10 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity

Diepenhorst, N. A., Leach, K., Keller, A. N., Rueda, P., Cook, A. E., Pierce, T. L., Nowell, C., Pastoureau, P., Sabatini, M., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4095-4108 14 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Muscarinic M5 receptors modulate ethanol seeking in rats

Berizzi, A. E., Perry, C. J., Shackleford, D. M., Lindsley, C. W., Jones, C. K., Chen, N. A., Sexton, P. M., Christopoulos, A., Langmead, C. J. & Lawrence, A. J., 1 Jun 2018, In : Neuropsychopharmacology. 43, 7, p. 1510-1517 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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13 Citations (Scopus)

Structure-Activity Relationships of Pan-Gαq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators

Berizzi, A. E., Bender, A. M., Lindsley, C. W., Conn, P. J., Sexton, P. M., Langmead, C. J. & Christopoulos, A., 18 Jul 2018, In : ACS Chemical Neuroscience. 9, 7, p. 1818-1828 11 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)
2017

High throughput, quantitative analysis of human osteoclast differentiation and activity

Diepenhorst, N., Nowell, C., Rueda, P., Henriksen, K., Pierce, T., Cook, A., Pastoureau, P., Sabatini, M., Charman, W., Christopoulos, A., Summers, R., Sexton, P. & Langmead, C., 15 Feb 2017, In : Analytical Biochemistry. 519, p. 51-56 6 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

Isoform-specific biased agonism of histamine H3 receptor agonists

Riddy, D. M., Cook, A. E., Diepenhorst, N. A., Bosnyak, S., Brady, R., La Cour, C. M., Mocaer, E., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Feb 2017, In : Molecular Pharmacology. 91, 2, p. 87-99 13 p.

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)
2016

Molecular mechanisms of action of M5 muscarinic acetylcholine receptor allosteric modulators

Berizzi, A. E., Gentry, P. R., Rueda, P., Hoedt, S. D., Sexton, P. M., Langmead, C. J. & Christopoulos, A., 1 Oct 2016, In : Molecular Pharmacology. 90, 4, p. 427-436 10 p.

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)

Murine GPRC6A mediates cellular responses to L-amino acids, but not osteocalcin variants

Rueda, P., Harley, E., Lu, Y., Stewart, G. D., Fabb, S., Diepenhorst, N., Cremers, B., Rouillon, M-H., Wehrle, I., Geant, A., Lamarche, G., Leach, K., Charman, W. N., Christopoulos, A., Summers, R. J., Sexton, P. M. & Langmead, C. J., 1 Jan 2016, In : PLoS ONE. 11, 1, p. 1-19 19 p., e0146846.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
27 Citations (Scopus)
Open Access
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9 Citations (Scopus)
2015

Discovery of HTL6641, a dual orexin receptor antagonist with differentiated pharmacodynamic properties

Christopher, J. A., Aves, S. J., Brown, J., Errey, J. C., Klair, S. S., Langmead, C. J., Mace, O. J., Mould, R., Patel, J. C., Tehan, B. G., Zhukov, A., Marshall, F. H. & Congreve, M., 1 May 2015, In : MedChemComm. 6, 5, p. 947-955 9 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)
2014

Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands

Mould, R., Brown, J., Marshall, F. H. & Langmead, C. J., Jan 2014, In : British Journal of Pharmacology. 171, 2, p. 351-363 13 p.

Research output: Contribution to journalArticleResearchpeer-review

48 Citations (Scopus)

Functional and structural perspectives on allosteric modulation of GPCRs

Langmead, C. J. & Christopoulos, A., 2014, In : Current Opinion in Cell Biology. 27, 1, p. 94 - 101 8 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

International union of basic and clinical pharmacology. XC. Multisite pharmacology: Recommendations for the nomenclature of receptor allosterism and allosteric ligands

Christopoulos, A., Changeux, J-P., Catterall, W. A., Fabbro, D., Burris, T. P., Cidlowski, J. A., Olsen, R. W., Peters, J. A., Neubig, R., Pin, J. P., Sexton, P., Kenakin, T. P., Ehlert, F. J., Spedding, M. & Langmead, C. J., 2014, In : Pharmacological Reviews. 66, 4, p. 918 - 947 30 p.

Research output: Contribution to journalArticleResearchpeer-review

119 Citations (Scopus)

Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment

Hutchings, C. J., Cseke, G., Osborne, G., Woolard, J., Zhukov, A., Koglin, M., Jazayeri, A., Pandya-Pathak, J., Langmead, C. J., Hill, S. J., Weir, M. & Marshall, F. H., Jan 2014, In : mAbs. 6, 1, p. 246-261 16 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)
2013

Pharmacology and structure of isolated conformations of the adenosine A2A receptor define ligand efficacy

Bennett, K. A., Tehan, B., Lebon, G., Tate, C. G., Weir, M., Marshall, F. H. & Langmead, C. J., May 2013, In : Molecular Pharmacology. 83, 5, p. 949-958 10 p.

Research output: Contribution to journalArticleResearchpeer-review

40 Citations (Scopus)

Supra-physiological efficacy at GPCRs: superstition or super agonists?

Langmead, C. J. & Christopoulos, A., 2013, In : British Journal of Pharmacology. 169, 2, p. 353 - 356 4 p.

Research output: Contribution to journalArticleOtherpeer-review

20 Citations (Scopus)
2012

Discovery of 1,2,4-triazine derivatives as adenosine A2A antagonists using structure based drug design

Congreve, M., Andrews, S. P., Dore, A. S., Hollenstein, K., Hurrell, E., Langmead, C. J., Mason, J. S., Ng, I. W., Tehan, B. G., Zhukov, A., Weir, M. & Marshall, F. H., 2012, In : Journal of Medicinal Chemistry. 55, 5, p. 1898 - 1903 6 p.

Research output: Contribution to journalArticleResearchpeer-review

231 Citations (Scopus)

Identification of novel adenosine A2A receptor antagonists by virtual screening

Langmead, C. J., Andrews, S. P., Congreve, M., Errey, J. C., Hurrell, E., Marshall, F. H., Mason, J. S., Richardson, C. M., Robertson, N., Zhukov, A. & Weir, M., 2012, In : Journal of Medicinal Chemistry. 55, 5, p. 1904 - 1909 6 p.

Research output: Contribution to journalArticleResearchpeer-review

99 Citations (Scopus)
2011

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

Lebon, G., Warne, T., Edwards, P. C., Bennett, K. A., Langmead, C. J., Leslie, A. G. W. & Tate, C. G., 23 Jun 2011, In : Nature. 474, 7352, p. 521-526 6 p.

Research output: Contribution to journalArticleResearchpeer-review

598 Citations (Scopus)

Determining allosteric modulator mechanism of action: Integration of radioligand binding and functional assay data

Langmead, C. J., 2011, In : Methods in Molecular Biology. 746, p. 195-209 15 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Quantitative analysis reveals multiple mechanisms of allosteric modulation of the mGlu5 receptor in rat astroglia

Bradley, S. J., Langmead, C. J., Watson, J. M. & Challiss, R. A. J., May 2011, In : Molecular Pharmacology. 79, 5, p. 874-885 12 p.

Research output: Contribution to journalArticleResearchpeer-review

35 Citations (Scopus)

The muscarinic M4 receptor is the functionally predominant subtype in rat and mouse striatum as demonstrated using [35S] GTPγS binding

Chapman, K. L., Vaswani, D., Hendry, N., Langmead, C. J., Kew, J. N. C. & Watson, J. M., 10 Feb 2011, In : European Journal of Pharmacology. 652, 1-3, p. 1-6 6 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)

The properties of thermostabilised G protein-coupled receptors (StaRs) and their use in drug discovery

Robertson, N., Jazayeri, A., Errey, J. C., Baig, A. H., Hurrell, E., Zhukov, A., Langmead, C. J., Weir, M. & Marshall, F. H., 2011, In : Neuropharmacology. 60, 1, p. 36 - 44 9 p.

Research output: Contribution to journalArticleResearchpeer-review

110 Citations (Scopus)

The use of GPCR structures in drug design

Congreve, M., Langmead, C. J. & Marshall, F. H., 2011, In : Advances in Pharmacology. 62, p. 1 - 36 36 p.

Research output: Contribution to journalArticleResearchpeer-review

36 Citations (Scopus)
2010

2′ Biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR

Budzik, B., Garzya, V., Shi, D., Foley, J. J., Rivero, R. A., Langmead, C. J., Watson, J. M., Wu, Z., Forbes, I. T. & Jin, JI., 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 12, p. 3540-3544 5 p.

Research output: Contribution to journalArticleResearchpeer-review

14 Citations (Scopus)

2′ Biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling

Budzik, B., Garzya, V., Shi, D., Walker, G., Lauchart, Y., Lucas, A. J., Rivero, R. A., Langmead, C. J., Watson, J. M., Wu, Z., Forbes, I. T. & Jin, JI., 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 12, p. 3545-3549 5 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

In vitro and in vivo comparison of two non-peptide tachykinin NK3 receptor antagonists: Improvements in efficacy achieved through enhanced brain penetration or altered pharmacological characteristics

Dawson, L. A., Langmead, C. J., Dada, A., Watson, J. M., Wu, Z., de la Flor, R., Jones, G. A., Cluderay, J. E., Southam, E., Murkitt, G. S., Hill, M. D., Jones, D. N. C., Davies, C. H., Hagan, J. J. & Smith, P. W., 10 Feb 2010, In : European Journal of Pharmacology. 627, 1-3, p. 106-114 9 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

N-desmethylclozapine (NDMC) is an antagonist at the human native muscarinic M1 receptor

Thomas, D. R., Dada, A., Jones, G. A., Deisz, R. A., Gigout, S., Langmead, C. J., Werry, T. D., Hendry, N., Hagan, J. J., Davies, C. H. & Watson, J. M., 1 Jun 2010, In : Neuropharmacology. 58, 8, p. 1206-1214 9 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

Novel N-substituted benzimidazolones as potent, selective, CNS-penetrant, and orally active M1 mAChR agonists

Budzik, B., Garzya, V., Shi, D., Walker, G., Woolley-Roberts, M., Pardoe, J., Lucas, A., Tehan, B., Rivero, R. A., Langmead, C. J., Watson, J. M., Wu, Z., Forbes, I. T. & Jin, JI., 9 Sep 2010, In : ACS Medicinal Chemistry Letters. 1, 6, p. 244-248 5 p.

Research output: Contribution to journalArticleResearchpeer-review

37 Citations (Scopus)

Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor

Avlani, V. A., Langmead, C. J., Guida, E., Wood, M. D., Tehan, B. G., Herdon, H. J., Watson, J. M., Sexton, P. & Christopoulos, A., 2010, In : Molecular Pharmacology. 78, 1, p. 94 - 104 11 p.

Research output: Contribution to journalArticleResearchpeer-review

52 Citations (Scopus)

Performance of mouse neural stem cells as a screening reagent: Characterization of PAC1 activity in medium-throughput functional assays

Lodge, A. P., Langmead, C. J., Daniel, G., Anderson, G. W. & Werry, T. D., 2010, In : Journal of Biomolecular Screening. 15, 2, p. 159-168 10 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)
2009

Contrasting effects of allosteric and orthosteric agonists on M1 muscarinic acetylcholine receptor internalization and down-regulation

Thomas, R. L., Langmead, C. J., Wood, M. D. & Challiss, R. A. J., Dec 2009, In : Journal of Pharmacology and Experimental Therapeutics. 331, 3, p. 1086-1095 10 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)

Evaluation of expression and function of the H+/myo-inositol transporter HMIT

Di Daniel, E., Mok, M. H. S., Mead, E., Mutinelli, C., Zambello, E., Caberlotto, L., Pell, T. J., Langmead, C. J., Shah, A. J., Duddy, G., Kew, J. N. C. & Maycox, P. R., 16 Jul 2009, In : BMC Cell Biology. 10, 54.

Research output: Contribution to journalArticleResearchpeer-review

35 Citations (Scopus)

Growth hormone secretagogues and growth hormone releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein Gαo1 by the ghrelin receptor

Bennett, K. A., Langmead, C. J., Wise, A. & Milligan, G., Oct 2009, In : Molecular Pharmacology. 76, 4, p. 802-811 10 p.

Research output: Contribution to journalArticleResearchpeer-review

27 Citations (Scopus)

Mutagenic mapping suggests a novel binding mode for selective agonists of M1 muscarinic acetylcholine receptors

Lebon, G., Langmead, C. J., Tehan, B. G. & Hulme, E. C., 2009, In : Molecular Pharmacology. 75, 2, p. 331 - 341 11 p.

Research output: Contribution to journalArticleResearchpeer-review

45 Citations (Scopus)
2008

Characterization of a CNS penetrant, selective M1 muscarinic receptor agonist, 77-LH-28-1

Langmead, C. J., Austin, N. E., Branch, C. L., Brown, J. T., Buchanan, K. A., Davies, C. H., Forbes, I. T., Fry, V. A. H., Hagan, J. J., Herdon, H. J., Jones, G. A., Jeggo, R. D., Kew, J. N. C., Mazzali, A., Melarange, R. A., Patel, N., Pardoe, J., Randall, A. D., Roberts, C. J., Roopun, A. K. & 6 others, Starr, K. R., Teriakidis, A., Wood, M. D., Whittington, M. A., Wu, Z. & Watson, J. M., 2008, In : British Journal of Pharmacology. 154, 5, p. 1104 - 1115 12 p.

Research output: Contribution to journalArticleResearchpeer-review

96 Citations (Scopus)

G protein coupling and signaling pathway activation by M1 muscarinic acetylcholine receptor orthosteric and allosteric agonists

Thomas, R. L., Mistry, R., Langmead, C. J., Wood, M. D. & Challiss, R. A. J., 2008, In : Journal of Pharmacology and Experimental Therapeutics. 327, 2, p. 365 - 374 10 p.

Research output: Contribution to journalArticleResearchpeer-review

43 Citations (Scopus)

Muscarinic acetylcholine receptors as CNS drug targets

Langmead, C. J., Watson, J. M. & Reavill, C., 2008, In : Pharmacology and Therapeutics. 117, 2, p. 232 - 243 12 p.

Research output: Contribution to journalArticleResearchpeer-review

303 Citations (Scopus)
2007

Roof and floor of the muscarinic binding pocket: Variations in the binding modes of orthosteric ligands

Goodwin, J. A., Hulme, E. C., Langmead, C. J. & Tehan, B. G., 1 Dec 2007, In : Molecular Pharmacology. 72, 6, p. 1484-1496 13 p.

Research output: Contribution to journalArticleResearchpeer-review

36 Citations (Scopus)

Screening for positive allosteric modulators: Assessment of modulator concentration-response curves as a screening paradigm

Langmead, C. J., 1 Aug 2007, In : Journal of Biomolecular Screening. 12, 5, p. 668-676 9 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors

May, L. T., Avlani, V. A., Langmead, C. J., Herdon, H. J., Wood, M. D., Sexton, P. & Christopoulos, A., 2007, In : Molecular Pharmacology. 72, 2, p. 463 - 476 14 p.

Research output: Contribution to journalArticleResearchpeer-review

95 Citations (Scopus)
2006

Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox

Langmead, C. J. & Christopoulos, A., 2006, In : Trends in Pharmacological Sciences. 27, 9, p. 475 - 481 7 p.

Research output: Contribution to journalArticleResearchpeer-review

104 Citations (Scopus)

Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2- methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M1 receptor: Direct pharmacological evidence that AC-42 is an allosteric agonist

Langmead, C. J., Fry, V. A., Forbes, I. T., Branch, C. L., Christopoulos, A., Wood, M. D. & Herdon, H. J., 2006, In : Molecular Pharmacology. 69, 1, p. 236 - 246 11 p.

Research output: Contribution to journalArticleResearchpeer-review

91 Citations (Scopus)