Constitutive Activity in Receptors and Other Proteins, Part A

This volume of Methods in Enzymology covers the current methodology for the detection and assessment of constitutively active proteins. The chapters written by expert authors who are leaders in the field, provide hints and tricks not available in primary research publications.It is extensively referenced, with useful figures and tables throughout the volume.

Section I-- Identification and Measurement of Constitutive Activity

1. Constitutive activity at the cannabinoid CB₁ receptor and behavioral responses

Katherine E. Hanlon and Todd W. Vanderah

2. Detecting constitutive activity and protean agonism at the cannabinoid-2 receptor.

Massimiliano Beltramo, Rossella Brusa, Isabella Mancini, Paola Scandroglio, Massimiliano. Beltramo

3. Modulation of constitutive activity of the ghrelin receptor by use of pharmacological tools as well as mutagenesis

Birgitte Holst and Jacek Mokrosiński

4. Assessment of constitutive activity and internalization of GPR54 (Kiss1-r).

Macarena Pampillo and Andy Videsh Babwah

5. Assessment of Constitutive Activity in EP Prostanoid Receptors

Hiromichi Fujino, Toshihiko Murayama, and John W. Regan

6. α_1D-Adrenergic receptors: constitutive activity and reduced expression at the plasma membrane

J Adolfo Garcia-Sáinz, M. Teresa Romero-Ávila and Luz del Carmen Medina

7. Constitutive activity of the histamine H₁ receptor

Saskia Nijmeijer, Rob Leurs and Henry F Vischer

8. Constitutive activity of somatostatin receptor subtypes

Anat Ben-Shlomo, Kolja Wawrowsky and Shlomo Melmed

9. Assessment of homologous internalization of constitutively active N111G mutant of AT₁ receptor

Mohiuddin Ahmed Bhuiyan and Takafumi Nagatomo

10. Methods to detect cell surface expression and constitutive activity of GPR6

Balakrishna M. Prasad, Bettye Hollins and Nevin A. Lambert

11. β₃-adrenoceptor agonists and (antagonists as) inverse agonists: history, perspective, constitutive activity and stereospecific binding.

Maria Grazia Perrone and Antonio Scilimati

12. Constitutive Activity of the Lutropin Receptor and its Allosteric Modulation by Receptor Heterodimerization

Deborah L. Segaloff

13. Assessing Constitutive Activity of Extracellular Calcium-Sensing Receptors in Vitro and in Bone

Wenhan Chang, Melita Dvorak, and Dolores Shoback

14. Constitutive Activity of Neural Melanocortin Receptors.

Ya-Xiong Tao, Hui Huang, Zhi-Qiang Wang, Fan Yang, Jessica N. Williams, and Gregory V. Nikiforovich

15. Measurement of Constitutive Activity of BMP Type I receptors

Peter ten Dijke

16. Probing the CA among dopamine D1 and D5 receptors and their mutants

Bianca Plouffe, Jean-Philippe D’Aoust, Vincent Laquerre, Binhui Liang and Mario Tiberi

17. Identification of Gain-of-Function Variants of the Human Prolactin Receptor

Vincent Goffin, Roman L. Bogorad, and Philippe Touraine

18. Investigations of Activated ACVR1/ALK2, a Bone Morphogenetic Protein (BMP) Type I Receptor that Causes Fibrodysplasia Ossificans Progressiva

Frederick. Kaplan, Petra Seemann, Julia Haupt, Meiqi Xu, Vitali Lounev, Mary Mullins, Eileen M. Shore

19. Identification and evaluation of constitutively active thyroid stimulating hormone receptor mutations

Joaquin Lado-Abeal, Leah R. Quisenberry, and Isabel Castro-Piedras

20. Assessment of constitutive activity of a G protein-coupled receptor, Cpr2, in Cryptococcus neoformans by heterologous and homologous methods

Chaoyang Xue, Yina Wang, and Yen-Ping Hsueh

21. In vitro and in vivo assessment of mu opioid receptor constitutive activity.

Edward J. Bilsky, Denise Giuvelis, Melissa D. Osborn, Christina M. Dersch, Heng Xu and Richard B. Rothman

22. Constitutively active µ-opioid methods

Mark. Connor and John Traynor

23. Protein Kinase Ck2 is a Constitutively-Active Enzyme That Promotes Cell Survival: Strategies To Identify Ck2 Substrates and Manipulate Its Activity In Mammalian Cells

Jacob P. Turowec, James S. Duncan, Ashley C. French, Laszlo Gyenis, Nicole A. St. Denis, Greg J. Vilk, and David W. Litchfield

24. Assessment of Ck2 Constitutive Activity In Cancer Cells

Maria Ruzzene, Giovanni Di Maira, Kendra Tosoni, and Lorenzo A. Pinna

25. Structural basis of the constitutive activity of protein kinase CK2

Birgitte B. Olsen, Barbara Guerra, Karsten Niefind and Olar-Georg Issinger font error

26. Measuring the Constitutive Activation of c-Jun N-terminal Kinase Isoforms

Ryan T. Nitta, Shawn S. Badal, and Albert J. Wong

27. Measurement of constitutive MAPK and PI3K/AKT signaling activity in human cancer cell lines.

Keiran S.M. Smalley

28. Constitutive activity of GPR40/FFA1: Intrinsic or assay dependent?

Leigh A Stoddart and Graeme Milligan

29. Constitutive activity of TRP channels: methods for measuring the activity and its outcome

Baruch Minke

30. Measurement of Orexin (Hypocretin) and Substance P Effects On Constitutively Active Inward Rectifier K+ Channels in Brain Neurons

Yasuko Nakajima and Shigehiro Nakajima

31. Characterization of G protein receptor kinase 4 and measuring its constitutive activity in vivo

Bradley T. Andresen

32. Voltage-clamp based methods for the detection of constitutively active acetylcholine-gated I_K,ACh channels in the diseased heart

Niels Voigt, Samy Makary, Stanley Nattel, Dobromir Dobrev

33. Assaying Wave and WASH complex constitutive activities towards the Arp2/3 complex.

Emmanuel DERIVERY and Alexis GAUTREAU