GPCR Signaling in Cancer

GPCR Signaling in Cancer PDF

Author:

Publisher: Academic Press

Published: 2020-03-06

Total Pages: 164

ISBN-13: 0128202300

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GPCR Signaling in Cancer, Volume 145, the latest release in the Advances in Cancer Research series, highlights recent developments in the area of GPCRs and cancer biology. Chapters included in this volume cover several GPCRs and their downstream effectors as case examples to highlight their fundamental understanding and therapeutic potential. Specific chapters address the Role of GRKs and beta-arrestins in cancer, Atypical GPCRs in cancer, the Role of a chemokine receptor (CCR) 5 in cancer, Targeting G protein-coupled receptors for therapeutics in cancer, Emerging GPCR signaling pathways in cancer, and more. G protein-coupled receptors (GPCRs) constitute a large family of cell surface receptors which are involved in nearly every cellular and physiological event. These receptors can recognize a broad array of ligands and they are targeted by nearly one third of the currently prescribed drugs including anti-cancer therapeutics. Covers the latest concepts in GPCR signaling and their relevancy to cancer biology Presents new indications for anti-cancer therapeutic programs Includes sections on cross-talk and signaling networks of GPCRs and effectors in molecular oncology and therapeutics

GPCRs as Therapeutic Targets

GPCRs as Therapeutic Targets PDF

Author: Annette Gilchrist

Publisher: John Wiley & Sons

Published: 2022-09-19

Total Pages: 1610

ISBN-13: 1119564727

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Eine umfassende Betrachtung der Struktur, Pharmakologie, Funktion und Rolle von G-Protein-gekoppelten Rezeptoren Mit GPCRs as Therapeutic Targets legt die renommierte Forscherin Dr. Annette Gilchrist einen maßgeblichen, umfassenden Leitfaden für einen dynamischen, aktiven Bereich der akademischen und industriellen Arzneimittelforschung vor. Das Werk, in dem die molekulare Pharmakologie dieser wichtigen Zielklasse behandelt wird, ist ein wichtiges Referenzwerk für neue und erfahrene Forscher, die sich mit G-Protein-gekoppelten Rezeptoren beschäftigen. Es enthält außerdem aktuelle Daten zu GPCR-Strukturen und dem strukturbasierten Wirkstoffdesign. In diesem Werk wird die Rolle von GPCR bei der Behandlung von Krankheiten und für neue Ansätze in deren Erforschung analysiert. Dabei werden nicht nur Informationen über die Struktur, Pharmakologie und Funktion von GPCR dargestellt, sondern es wird auch deren Rolle bei Krankheitszuständen erörtert. Neue Methoden zur Messung der GPCR-Aktivität werden auf verständliche und ansprechende Weise präsentiert. Das Werk bietet: * Eine gründliche Einführung in die molekulare Pharmakologie G-Protein-gekoppelter Rezeptoren mit aktuellen Angaben zu GPCR-Strukturen und dem strukturbasierten Wirkstoffdesign * Ausführliche Erörterungen der entstehenden Pharmakologie von GPCR, des intrazellulären Transports und der subzellulären GPCR-Signalübertragung * Umfassende Betrachtung der allosterischen Modulation, Rezeptordimerisierung, Deorphanisierung und Ubiquitinierung * Ausführliche Besprechung der Rolle von GPCR bei der Behandlung von Krebs, Substanzmissbrauch, zerebrovaskulären Erkrankungen und Stoffwechselkrankheiten Als ideales Referenzwerk für Forscher in den Bereichen Biochemie, Zellbiologie und Pharmakologie sollte GPCRs as Therapeutic Targets auch in den Bibliotheken von Fachleuten der Medizinischen Chemie, Strukturbiologie und klinischen Pharmakologie einen Platz finden.

G-protein Coupled Receptor Mediated Signaling Pathways in Chemoresistant Melanoma and Ovarian Cancer

G-protein Coupled Receptor Mediated Signaling Pathways in Chemoresistant Melanoma and Ovarian Cancer PDF

Author: Molly Koertel Altman

Publisher:

Published: 2014

Total Pages: 416

ISBN-13:

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Cellular signaling pathways are involved in numerous physiological processes such as reproduction, growth, and the development of cancer and chemoresistance. G-protein coupled receptors (GPCRs) are master regulators of many signaling pathways as they are expressed in numerous tissues types throughout the body. GPCRs are being investigated in cancer development particularly through their roles in angiogenesis, metastasis, and inflammation-associated cancer. Growth factors that bind and activate GPCRs to mediate signaling pathways involved in growth and survival include lysophosphatidic acid (LPA). In our studies, both in vitro and in vivo methods were used to test the importance of several signaling pathways in chemoresistant cancer cell survival and tumor biology. In our studies, we found that specific Regulators of G-protein signaling (RGS) proteins are involved in modulating growth and survival pathways in ovarian cancer. Specifically, we showed that silencing of RGS10 and RGS17 proteins increases viability of ovarian cancer cells, and we further examined the role of modulating RGS10 expression on cell differentiation, proliferation, and survival pathways. We also showed that the inhibition of autotaxin the enzyme that produces LPA is a potential therapeutic target for melanoma and how LPA mediated receptor pathways can be manipulated to overcome chemoresistance in cancer. Our most valuable observation was that our novel compounds were able to reduce tumor progression in vivo in a primary xenograft model of melanoma in correlation with a reduction in markers of angiogenesis. Our data serves to help better understand signaling pathways involved in the development of chemoresistance.

G Protein-coupled Receptor Expression and Function in Cancer and the Cancer Associated Microenvironment

G Protein-coupled Receptor Expression and Function in Cancer and the Cancer Associated Microenvironment PDF

Author: Thalia McCann

Publisher:

Published: 2015

Total Pages: 101

ISBN-13: 9781339097022

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G protein-coupled receptors (GPCRs) are the largest superfamily of membrane receptors and are targeted by more than 30% of FDA-approved drugs. Although there has been limited study of GPCRs in cancer, they may be strategic targets in treating both tumor cells and the supportive microenvironment that is implicated in malignancies such as chronic lymphocytic leukemia (CLL) and pancreatic ductal adenocarcinoma (PDAC). In this thesis research, TaqMan® GPCR arrays were used as an unbiased approach to characterize the GPCR profile of CLL cells and NKtert bone marrow cells, as well as PDAC cells and pancreatic- cancer associated fibroblasts (CAFs). The results revealed that targeting two highly expressed Gs-linked GPCRs, VIPR1 and MC2R, in combination with the dual PDE inhibitor IR284, increased CLL cell death, presumably by increasing cellular cAMP levels. I characterized the GPCR profile of bone marrow NKtert cells and found that cAMP-mediated effects reduce NKtert cell viability and proliferation by modulation of protein kinase A (PKA) and the Exchange Protein activated by cAMP -1 (Epac-1), respectively. I determined that PDAC cells express 73 GPCRs whose expression was shared on three patient tumors, and 55 GPCRs shared between two patient-derived cell lines and two PDAC cell lines. Of these GPCRs, the Class C orphan GPRC5A was found to be the most highly expressed and up-regulated in PDAC cells relative to a normal pancreatic ductal epithelial cell line (HPDE6) and in CAFs compared to pre-fibroblast precursor cells (pancreatic stellate cells, PSC). Transfection of HPDE6 cells with GPRC5A enhanced DNA synthesis in the cells, indicating that GPRC5A may contribute to the malignant phenotype of PDAC and may be a novel therapeutic target for pancreatic cancer. Thus, I was able to characterize the expression of GPCRs in two types of cancer, in both the cancer cells themselves and in cells of their associated microenvironment. The findings provide new insights regarding GPCR expression in cancer and suggest new ways in which cancer cells interact with their surrounding microenvironment.

GPCR Signaling in Cancer

GPCR Signaling in Cancer PDF

Author:

Publisher: Academic Press

Published: 2020-02-21

Total Pages: 0

ISBN-13: 9780128202302

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GPCR Signaling in Cancer, Volume 145, the latest release in the Advances in Cancer Research series, highlights recent developments in the area of GPCRs and cancer biology. Chapters included in this volume cover several GPCRs and their downstream effectors as case examples to highlight their fundamental understanding and therapeutic potential. Specific chapters address the Role of GRKs and beta-arrestins in cancer, Atypical GPCRs in cancer, the Role of a chemokine receptor (CCR) 5 in cancer, Targeting G protein-coupled receptors for therapeutics in cancer, Emerging GPCR signaling pathways in cancer, and more. G protein-coupled receptors (GPCRs) constitute a large family of cell surface receptors which are involved in nearly every cellular and physiological event. These receptors can recognize a broad array of ligands and they are targeted by nearly one third of the currently prescribed drugs including anti-cancer therapeutics.

The Role of CXCR4 and Arrestins in Breast Cancer Signaling and Apoptosis

The Role of CXCR4 and Arrestins in Breast Cancer Signaling and Apoptosis PDF

Author:

Publisher:

Published: 2005

Total Pages: 7

ISBN-13:

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G protein--coupled receptors (GPCR) are a family of receptors that are involved in all physiologic and many pathologic processes. Recently, they have been described as playing a critical role in breast cancer metastasis. As all GPCRs interact with arresting, we have sought to better understand the role of arrestin interaction with GPCRs particularly in the process of apoptosis. Previously published data has described the initiation of apoptosis when GPCRs are stimulated in the absence of arrestins. It is therefore our goal to better understand this process and therefore better understand potential roles for GPCRs and arrestins in breast cancer development. From this work, we hypothesize that arrestin can be used as a novel chemotherapeutic target. If arrestins are inhibited, stimulation of GPCRs found on metastatic breast cancer cells may undergo apoptosis therefore providing a new treatment to eradicate breast cancer.

G Protein-Coupled Receptor Signaling

G Protein-Coupled Receptor Signaling PDF

Author: Mario Tiberi

Publisher: Humana Press

Published: 2019-03-01

Total Pages: 406

ISBN-13: 9781493991204

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This detailed volume assembles comprehensive protocols to assist with the study of structural, molecular, cell biological, and in vivo facets of GPCRs, and to enable the development of experimental tools for screening novel GPCR drugs. Sections explore the tweaking of ligands, bioluminescence and FRET approaches, specific GPCR signaling properties, as well as visualization of subcellular compartmentalization. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, G Protein-Coupled Receptor Signaling: Methods and Protocols serves as an ideal reference for life scientists working in a variety of research fields including molecular pharmacology, cell and developmental biology, brain behavior and physiology, drug development and screening. Chapter 4 is available open access under a CC BY 4.0 license via link.springer.com.

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