MOLECULAR PHARMACOLOGY DIVISION SESSIONS AT EB 2001

COLLOQUIUM: G PROTEIN COUPLED RECEPTORS – Day 1

Separate, advanced registration required. No on-site registration.

(Sponsored by the Division for Molecular Pharmacology)

(Supported by education grants from ASPET's Division for Molecular Pharmacology, AstraZeneca R & D, I.R.I.S., Merck Research Laboratories, Novartis, Roche Bioscience, Sepracor, SmithKline Beecham, and SmithKline Beecham U.K.)

Fri. 7:15 AM-Rosen Plaza Hotel, Room TBD

Organized by: R.A. Bond and G. Milligan

7:15 Continental breakfast.

7:55 Introduction. R.A. Bond. Univ. of Houston.

8:00 Orphan GPCRs: how to identify them. S. Wilson. SmithKline Beecham Pharmaceut.

8:35 Discussion.

8:40 Engineering the GPCR ligand binding site. T. Schwartz. Univ. of Copenhagen.

9:15 Discussion.

9:20 Molecular mechanisms involved in GPCR activation and G protein coupling selectivity. J. Wess.
NIDDK, NIH.

9:55 Discussion.

10:00 Coffee break.

10:30 Receptor oligomerization. M. Bouvier. Univ. of Montreal.

11:05 Discussion.

11:10 The road to high resolution GPCR structures. B. Springer. 3-Dimensional Pharmaceut., Inc.

11:45 Discussion

11:50 Lunch.

1:30 Prostaniod receptor regulation. G.A. Fitzgerald. Univ. of Pennsylvania.

2:05 Discussion.

2:10 GPCR-G protein interactions. G. Milligan. Univ. of Glasgow.

2:45 Discussion.

2:50 Phosphorylatin and regulation of GPCRs by casein kinase 1 alpha. A. Tobin. Univ. of Leicester.

3:25 Discussion.

3:30 Break.

4:10 Regulation of TRH receptors. P.M. Hinkle. Univ. of Rochester Med. Ctr.

4:45 Discussion.

4:50 Arrestins and GPCR regulation. M.G. Caron. Duke Univ. Med. Ctr.

5:25 Discussion.

COLLOQUIUM: G PROTEIN COUPLED RECEPTORS – Day 2

Separate, advanced registration required. No on-site registration.

Sat. 7:45 AM-Rosen Plaza Hotel, Room TBD

Organized by R.A. Bond and G. Milligan

7:45 Continental breakfast.

8:30 Efficacy: what's it all about. T.P. Kenakin. Glaxo Wellcome Res., Research Triangle Park, NC.

9:05 Discussion.

9:10 Regulating ligand efficacy. F. Leeb-Lundberg. Univ. of Texas Hlth. Sci. Ctr., San Antonio.

9:45 Discussion.

9:50 Ligand-directed trafficking of GPCRs to different pathways. W.P. Clarke. Univ. of Texas Hlth. Sci.

Ctr., San Antonio.

10:25 Discussion.

10:30 Coffee break.

11:00 Receptor dimerization. Y.C. Patel. McGill Univ. Fac. of Med.

11:35 Discussion.

11:40 Protein-protein interactions involving the GABAb receptor. J. White. Glaxo Wellcome, Stevenage,
U.K.

12:15 Discussion.

12:20 Lunch.

1:30 Selective effects of RGS. T. Wilkie. Univ. of Texas Southwestern Med. Ctr.

2:05 Discussion.

2:10 Proteins which interact with GPCRs G protein. S.M. Lanier. Med. Univ. of South Carolina.

2:45 Discussion.

2:50 Break.

3:20 Young investigator talks.

BURROUGHS WELLCOME FUND LECTURE:

Sunday 12:15-1:15 PM (Room 307 C/D)

M.S. Boguski Rosetta Inpharmatics, Inc.

SYMPOSIUM: GUANYLIN PEPTIDES AND CYCLIC GMP SIGNALING MECHANISMS

(Sponsored by the Division for Molecular Pharmacology)

Sun. 2:00 PM-Orange County Convention Center, Room 306 A/B

Chaired: L.R. Forte

2:00 Introduction. L.R. Forte. Univ. of Missouri.

2:10 Uroguanylin, cyclic GMP and colon cancer. L.R. Forte. Univ. of Missouri Sch. of Med.

2:35 Discussion.

2:40 Role of guanylate cyclase-C as an intestinal receptor for guanylin peptides. R.A. Giannella. Univ. of
Cincinnati Col. of Med.

3:05 Discussion.

3:10 Regulation of the renal expression of guanylin and uroguanylin. M. Kuhn. Univ. of Muenster,
Germany.

3:35 Discussion.

3:40 Guanylin peptides regulate urinary NaCl excretion via cyclic GMP. M.C. Fonteles. Ceara State Univ.,

4:05 Discussion.

4:10 Abstract 4101. Changes in receptor guanylate cyclase signaling molecules induced by partial hepatectomy in the rat. A.M. Schrader. Univ of Missouri.

4:20 Discussion.

4:25 Abstract 8325. Stimulation of intestinal chloride secretion: serosal actions of guanylin. J.-H. Seok. Univ. of Missouri.

4:35 Discussion.

4:40 General discussion.

SYMPOSIUM: G PROTEIN REGULATION OF ENDOTHELIAL FUNCTION

(Sponsored by the Division for Molecular Pharmacology)

Mon. 9:00 AM-Orange County Convention Center, Room 307 A/B

Co-chairs: A.B. Malik and T.Voyno-Yasenetskaya

9:00 Introduction. A.B. Malik. Univ. of Illinois, Chicago.

9:10 Role of heterotrimeric G13 protein in regulation of endothelial cell function. T. Voyno-Yasenetskaya.
Univ. of Illinois, Chicago.

9:40 Discussion.

9:50 Sorting out the G protein pathways mediating thrombin's action on endothelial cells. H.E. Hamm.
Northwestern Univ. Med. Sch.

10:20 Discussion.

10:30 Protease-activated receptors in vascular biology. S.R. Coughlin. UCSF.

11:00 Discussion.

11:10 G protein-receptor signaling in angiogenesis and biology of cyclooxygenase-2. T.T. Hla. Univ. of
Connecticut

11:40 Discussion.

SYMPOSIUM: CURRENT PROGRESS OF ESTERASES: FROM MOLECULES TO FUNCTIONS

(Sponsored by the Division for Drug Metabolism and the Division for Molecular Pharmacology)

Tues. 9:00 AM-Orange County Convention Center, Room 307 C/D

Chaired: T. Satoh

9:00 Introduction. T. Satoh. Chiba Univ. & Biomed. Res. Inst., Chiba, Japan.

9:10 Structural and functional diversity in the _-_ hydrolase fold family of proteins: from neurotransmitter
hydrolysis to

9:30 Discussion.

9:35 Biological effects of over expression of insect and mammalian esterases. B.D. Hammock. Univ. of
California, Davis.

9:55 Discussion.

10:00 Human and rat carboxylesterases: ester substrate specificity and tissue-specific expression. W.F.

10:20 Discussion.

10:25 Molecular cloning and expression of liver, intestine and brain carboxylesterase isozymes: role in
metabolic activation of drugs. M. Hosokawa. Chiba Univ., Japan

10:45 Discussion.

10:50 Evolution and enzymatic properties of the mammalian paraoxonases. B.N. LaDu. Univ. of Michigan Med. Sch.

11:10 Discussion.

11:15 Conclusion. T. Satoh. Chiba Univ. & Biomed. Res. Inst., Chiba, Japan.

MOLECULAR PHARMACOLOGY DIVISION SYMPOSIUM: MACROMOLECULAR SIGNALING
COMPLEXES

Tues. 2:00 PM-Orange County Convention Center, Room 307 C/D

Chaired: T.M. Wilkie

2:00 Targeting of PKA, PKC, and protein phosphatases to cellular microdomains. J.D. Scott. Oregon Hlth.

2:25 Discussion.

2:35 Abstract 842. Protein kinase A-anchoring protein 110, AKAP110: a novel effector molecule of G13 protein. J.

2:45 Discussion.

2:48 MAP kinase binding and activation of dual-specificity phosphatases: a mechanism for enzymatic specificity. S.

3:13 Discussion.

3:23 Break.

3:33 G protein/RGS control of Ca2+ signaling and cell proliferation. T.M. Wilkie. Univ. of Texas Southwestern Med. Ctr.

3:58 Discussion.

4:08 Spatial and temporal coordination in signal transduction pathways. T. Meyer. Stanford Univ. Sch. of Med.

4:33 Discussion.

SYMPOSIUM: CAPACITATIVE CALCIUM ENTRY

(Sponsored by the Division for Molecular Pharmacology)

Wed. 9:00 AM-Orange County Convention Center, Room 307 C/D

Chaired: J.W. Putney

9:00 Overview of capacitative calcium entry. J.W. Putney. NIEHS, Research Triangle Park, NC.

9:20 Coupling mechanisms to activate store-operated channels. D.L. Gill. Univ. of Maryland Sch. of Med. 

9:50 Discussion.

10:00 Structure and function of TRPs and associated proteins. V. Flockerzi. Univ. of Saarlandes, Homburg, Germany.

10:30 Discussion.

10:40 Regulation of TRP channels by IP3R and Ca/CaM. L. Birnbaumer. UCLA Sch. of Med.

11:10 Discussion.

11:20 Gating of store-operated Ca influx channels by Ca release channels. S. Muallem. Univ. of Texas Southwestern Med. Ctr.