Christopher Langmead

Dr

20012020

Research output per year

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Research Output

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

1 Citation (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

1 Citation (Scopus)

New Advances in Targeting the Resolution of Inflammation: Implications for Specialized Pro-Resolving Mediator GPCR Drug Discovery

Park, J., Langmead, C. & Riddy, D., 20 Jan 2020, In : ACS Pharmacology & Translational Science. 3, 1, p. 88-106 19 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

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
File
2 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
File
6 Citations (Scopus)

The importance of sex differences in pharmacology research

Gogos, A., Langmead, C., Sullivan, J. C. & Lawrence, A. J., 1 Nov 2019, In : British Journal of Pharmacology. 176, 21, p. 4087-4089 3 p.

Research output: Contribution to journalEditorialOther

Open Access
File
1 Citation (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
File
9 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
File
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

6 Citations (Scopus)

G protein-coupled receptors as anabolic drug targets in osteoporosis

Diepenhorst, N., Rueda, P., Cook, A. E., Pastoureau, P., Sabatini, M. & Langmead, C. J., 1 Apr 2018, In : Pharmacology and Therapeutics. 184, p. 1-12 12 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

4 Citations (Scopus)

G protein–coupled receptors targeting insulin resistance, obesity, and type 2 diabetes mellitus

Riddy, D. M., Delerive, P., Summers, R. J., Sexton, P. & Langmead, C. J., 1 Jan 2018, In : Pharmacological Reviews. 70, 1, p. 39-67 29 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

27 Citations (Scopus)

Molecular pharmacology of GPCRs

Langmead, C. J. & Summers, R. J., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4005-4008 4 p.

Research output: Contribution to journalEditorialOther

Open Access
File
3 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
File
12 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

2 Citations (Scopus)

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

11 Citations (Scopus)

Isoform-specific bias of histamine H3 receptor agonists

Riddy, D., Cook, A. E., Diepenhorst, N., Bosnyak, S., Brady, R., La Cour, C. M., Mocaer, E., Summers, R., Charman, W., Sexton, P. M., Christopoulos, A. & Langmead, C., 2016.

Research output: Contribution to conferencePoster

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

11 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
File
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

47 Citations (Scopus)

From orphans to orexins: An arousing fifteen years

Langmead, C. J., Jan 2014, In : British Journal of Pharmacology. 171, 2, p. 281-282 2 p.

Research output: Contribution to journalEditorialOtherpeer-review

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

23 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

228 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)

Ligand properties and behaviours in an allosteric age

Langmead, C. J., Dec 2012, In : Trends in Pharmacological Sciences. 33, 12, p. 621-622 2 p.

Research output: Contribution to journalLetterOtherpeer-review

5 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

594 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)

Progress in structure based drug design for G protein-coupled receptors

Congreve, M., Langmead, C. J., Mason, J. S. & Marshall, F. H., 2011, In : Journal of Medicinal Chemistry. 54, 13, p. 4283 - 4311 29 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

171 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

13 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)

Matching models to data: A receptor pharmacologist's guide

Hall, D. A. & Langmead, C. J., Nov 2010, In : British Journal of Pharmacology. 161, 6, p. 1276-1290 15 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

13 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)