Výsledky vyhledávání - "Steve Wenglowsky"

Abstract P6-10-07: CDK2 inhibition with BLU-222 in combination with ribociclib demonstrates robust antitumor activity in pre-clinical models of CDK4/6 inhibitor-naïve and -resistant HR+/HER2- breast cancer

Autor: Victoria Brown, Nealia House, Phil Ramsden, Karen Ho, Hsin-Jung Wu, Erik Wilker, Jian Guo, Maxine Chen, Douglas Wilson, Neil Bifulco, Steve Wenglowsky, Yoon Jong Choi, Kerrie Faia

Publikováno v: Cancer Research. 83:P6-10

Cyclin-dependent kinase 4/6 (CDK4/6) inhibitors are standard of care in combination with endocrine therapy in advanced hormone receptor-positive (HR+), human epidermal growth factor receptor 2 negative (HER2-) breast cancer. Despite improved progress

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fc6d20bceceb1cc735d1a8f803dbcaf5
https://doi.org/10.1158/1538-7445.sabcs22-p6-10-07

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Abstract 2306: BLU-222, an investigational, potent, and selective CDK2 inhibitor, demonstrated robust antitumor activity in CCNE1-amplified ovarian cancer models

Autor: Victoria Brown, Phil Ramsden, Nealia House, Richard Vargas, Jian Guo, Ruduan Wang, Riadh Lobbardi, Maxine Chen, Douglas Wilson, Joseph Kim, Neil Bifulco, Michelle Maynard, Emanuele Perola, Dean Zhang, Steve Wenglowsky, Yoon Jong Choi

Publikováno v: Cancer Research. 82:2306-2306

Background: Cyclin-dependent kinases (CDK) are a class of enzymes that, along with their regulatory cyclin binding partners, drive cell cycle progression. Cell cycle dysregulation is a hallmark of cancer and targeting its genetic drivers can confer t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8d89d4c271e2dff423ca97010d6af0af
https://doi.org/10.1158/1538-7445.am2022-2306

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Abstract 1279: Development of a selective CDK2-E inhibitor in CCNE driven cancers

Publikováno v: Cancer Research. 81:1279-1279

Background: Cyclin dependent kinases (CDK) comprise a family of proteins which are activated upon cyclin binding to promote cell cycle progression. Historically, CDK family inhibitors have had limited utility in the clinic due to 1) toxicities associ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a09f8cd954d28465a9103a79c7a17d6d
https://doi.org/10.1158/1538-7445.am2021-1279

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Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-RafV600E kinase

Autor: Victoria Dinkel, Jonas Grina, David A. Moreno, Simon Mathieu, Joshua D. Hansen, Kevin Rasor, Gregg Hastings, Walter C. Voegtli, Guy Vigers, Sumeet Rana, Joachim Rudolph, Susan L. Gloor, Ellen R. Laird, Li Ren, Steve Wenglowsky, Brandon S. Willis, Hillary L. Sturgis

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 24:1923-1927

Herein we describe the design of a novel series of ATP competitive B-Raf inhibitors via structure-based methods. These 3-N-methylquinazoline-4(3H)-one based inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimizati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b7cdfcadee638970486cfd5239d3478
https://doi.org/10.1016/j.bmcl.2014.03.007

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Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase

Autor: Alexandre J. Buckmelter, Kateri A. Ahrendt, Susan L. Gloor, Ellen R. Laird, Steve Wenglowsky, Nathalie Klopfenstein, Bainian Feng, Xianfeng Li, Jonas Grina, Li Ren, Brad Newhouse, Zhaoyang Wen, Walter C. Voegtli, Joachim Rudolph

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:5896-5899

This Letter details the synthesis and evaluation of imidazo[4,5-b]pyridines as inhibitors of B-Raf kinase. These compounds bind in a DFG-in, αC-helix out conformation of B-Raf, which is a binding mode associated with significant kinase selectivity.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0ac7a3d9b7f5f24125f9fe3a150e5ef
https://doi.org/10.1016/j.bmcl.2013.08.086

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Systemic in vitro and in vivo evaluation for determining the feasibility of making an amorphous solid dispersion of a B-Raf (rapidly accelerated fibrosarcoma) inhibitor

Autor: Joachim Rudolph, Jason Boggs, Yingqing Ran, Po-Chang Chiang, Edna F. Choo, Jonas Grina, Yong Cui, Steve Wenglowsky

Publikováno v: International Journal of Pharmaceutics. 454:241-248

It is well acknowledged that oral bioavailability of a drug candidate is often influenced by factors such as the permeability, physico-chemical properties, and metabolism of the drug. Among the physico-chemical properties, solubility and dissolution

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59f062c01ee7a1e40ec9e00923734e7c
https://doi.org/10.1016/j.ijpharm.2013.06.064

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Pyrazolo[3,4-b]pyridine kinase inhibitors: a patent review (2008 – present)

Autor: Steve Wenglowsky

Publikováno v: Expert Opinion on Therapeutic Patents. 23:281-298

Numerous heterocycles occur as recurring motifs in the design of kinase inhibitors. Pyrazolo[3,4-b]pyridine has proved particularly versatile due to its ability to interact with kinases via multiple binding modes. As such, this scaffold has been clai

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b6be5547968a22dc93c6537230e5a506
https://doi.org/10.1517/13543776.2013.749861

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