A multicentre, double blind, placebo controlled, safety and efficacy trial of whey growth factor extract (WGFEA) for oral mucositis in lymphoma patients undergoing carmustine, etoposide, cytosine arabinoside and melphalan (BEAM) chemotherapy and autologous stem cell transplantation

开始日期2006-06-01

申办/合作机构

TGR BioSciences Pty Ltd.

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项与 TGR BioSciences Pty Ltd. 相关的文献（医药）

2010-06-01·Current opinion in molecular therapeutics

An emerging role for kinase screening in GPCR drug discovery.

Review

作者: Dupriez, Vincent J ; Crouch, Michael F ; Osmond, Ronald I W

GPCRs are a large class of cell-surface receptors that are involved in a diverse array of biological processes, including many that are critical to diseases. As a result, GPCRs are a major focus for drug discovery research, and have been highly amenable to therapeutic intervention. However, the successes to date may represent the 'low-hanging fruit' (ie, outcomes that have been easiest to achieve). The signaling of many GPCRs is now recognized to be substantially more complex than initially thought. Thus, the traditional analysis of single GPCR-mediated secondary messengers for early-stage drug discovery, such as the measurement of Ca2+ or the formation of cAMP, may not provide all of the relevant signaling information on a target receptor or information on all of the effects of potential drugs. Given this complexity, the determination of other signaling events, such as the GPCR-mediated activation of major kinase pathways, including PI3K and MAPK, is likely to become increasingly important in the identification of indicators of GPCR function. Furthermore, the advent of highly efficient assays for detecting the GPCR-mediated activation of protein kinase targets allows this target class to be readily amenable to cell-based high-throughput screening programs.

2008-06-01·Combinatorial chemistry & high throughput screening4区 · 医学

New Strategies in Drug Discovery for GPCRs: High Throughput Detection of Cellular ERK Phosphorylation

4区 · 医学

Article

作者: Crouch, Michael F. ; Osmond, Ron I. W.

G-protein coupled receptors (GPCRs) are a large family of receptors for a wide range of stimulants, including hormones, neurotransmitters, and taste and olfactory chemicals. Due to their broad involvement in cellular responses, GPCRs affect many important body functions both in health and disease. Compared to other receptor families, the GPCRs have been a rich source of extracellularly-acting pharmaceuticals, due largely to the fact that many GPCR ligands are small molecules when compared with ligands for other receptors, such as the tyrosine kinase receptor family. This has allowed the development of small molecule modulators of receptor function that act on specific GPCRs, such as those involved in cardiovascular regulation. However, at several levels, current screening technologies of drug development for GPCRs are lacking. Firstly, responses from many GPCRs, such as the Gi-coupled GPCRs, are not easily measured in large screening programs by current techniques. Secondly, there are few options for detecting agonists of orphan GPCRs. Thirdly, it is now clear that the signaling from GPCRs is more complex than once thought, and the measurement of Ca(2+) and cAMP can account for only a fraction of the biological information emanating from an activated GPCR. Studies of the discrete and sometimes separable activation of the Ras/Raf/Mek/ERK cascade by many GPCRs is likely to offer development of new agonists and antagonists, contribute to new pharmacologies from receptors, and raise the potential for novel drug candidates in this important area of biology. Downstream activation of the ERK pathway, with or without transactivation of growth factor receptors, has not been measurable by high throughput methodologies. This article presents recent advances and associated applications for screening of GPCRs and other receptor species through the rapid measurement of protein phosphorylation events, such as ERK phosphorylation, as new readouts for drug discovery.

2005-10-01·Journal of biomolecular screening

GPCR Screening via ERK 1/2: A Novel Platform for Screening G Protein–Coupled Receptors

Article

作者: Sheehan, Antony ; Harvey, Georgina ; Brown, Andrea ; Crouch, Michael F. ; Borowicz, Romana ; Turner, Cheryl ; Dyer, Anthony R. ; Barnett, Emma ; Osmond, Ronald I. W.

Discovery of novel agonists and antagonists for G protein-coupled receptors (GPCRs) relies heavily on cell-based assays because determination of functional consequences of receptor engagement is often desirable. Currently, there are several key parameters measured to achieve this, including mobilization of intracellular Ca2+ and formation of cyclic adenosine monophosphate or inositol triphosphate. However, no single assay platform is suitable for all situations, and all of the assays have limitations. The authors have developed a new high-throughput homogeneous assay platform for GPCR discovery as an alternative to current assays, which employs detection of phosphorylation of the key signaling molecule p42/44 MAP kinase (ERK 1/2). The authors show that ERK 1/2 is consistently activated in cells stimulated by Gq-coupled GPCRs and provides a new high-throughput platform for screening GPCR drug candidates. The activation of ERK 1/2 in Gq-coupled GPCR systems generates comparable pharmacological data for receptor agonist and antagonist data obtained by other GPCR activation measurement techniques.

项与 TGR BioSciences Pty Ltd. 相关的新闻（医药）

2021-06-03

·GlobeNewswire

SHAREHOLDER ALERT: WeissLaw LLP Investigates TGR Financial, Inc.

NEW YORK, June 03, 2021 (GLOBE NEWSWIRE) -- WeissLaw LLP is investigating possible breaches of fiduciary duty and other violations of law by the board of directors of TGR Financial, Inc. (“TGR Financial” or the “Company”) (OTC: TGRF) in connection with the Company’s proposed acquisition by First Foundation Inc. (“First Foundation”) (NASDAQ: FFWM). Under the terms of the merger agreement, TGR Financial’s shareholders will receive 0.6068 of a share of First Foundation for each TGR Financial share they own or TGR Financial Series A non-voting convertible preferred stock, representing implied per-share merger consideration of approximately $15.24 based upon TGR Financial’s June 2, 2021 closing price of $25.12. Following consummation of the all-stock transaction, existing TGR Financial shareholders will own approximately 20.2% of the outstanding shares of First Foundation’s common stock. If you own TGR Financial shares and wish to discuss this investigation or have any questions concerning this notice or your rights or interests, visit our website: Or please contact:Joshua Rubin, Esq.WeissLaw LLP1500 Broadway, 16th FloorNew York, NY 10036(212) 682-3025(888) 593-4771stockinfo@weisslawllp.com WeissLaw LLP is investigating whether TGR Financial’s board acted in the best interest of TGR Financial’s public shareholders in agreeing to the proposed transaction, whether the per-share merger consideration adequately compensates TGR Financial’s shareholders, and whether all information regarding the process undertaken by the board and the valuation of the transaction will be fully and fairly disclosed to TGR Financial’s public shareholders. WeissLaw LLP has litigated hundreds of stockholder class and derivative actions for violations of corporate and fiduciary duties. We have recovered over a billion dollars for defrauded clients and obtained important corporate governance relief in many of these cases. If you have information or would like legal advice concerning possible corporate wrongdoing (including insider trading, waste of corporate assets, accounting fraud, or materially misleading information), consumer fraud (including false advertising, defective products, or other deceptive business practices), or anti-trust violations, please email us at stockinfo@weisslawllp.com

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