PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry, and Emerging Pharmacology

RJ Grams, WL Santos, IR Scorei, A Abad-García… - Chemical …, 2024 - ACS Publications
Boron-containing compounds (BCC) have emerged as important pharmacophores. To date,
five BCC drugs (including boronic acids and boroles) have been approved by the FDA for …

The state of the art in azaborine chemistry: new synthetic methods and applications

ZX Giustra, SY Liu - Journal of the American Chemical Society, 2018 - ACS Publications
Boron–nitrogen heteroarenes hold great promise for practical application in many areas of
chemistry. Enduring interest in realizing this potential has in turn driven perennial innovation …

Discovery of entrectinib: a new 3-aminoindazole as a potent anaplastic lymphoma kinase (ALK), c-ros oncogene 1 kinase (ROS1), and pan-tropomyosin receptor …

M Menichincheri, E Ardini, P Magnaghi… - Journal of medicinal …, 2016 - ACS Publications
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase responsible for the
development of different tumor types. Despite the remarkable clinical activity of crizotinib …

Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)

CM Robb, JI Contreras, S Kour, MA Taylor… - Chemical …, 2017 - pubs.rsc.org
Cyclin-dependent kinase 9 (CDK9), a member of the cyclin-dependent protein kinase (CDK)
family, is involved in transcriptional elongation of several target genes. CDK9 is ubiquitously …

The importance of plasma protein binding in drug discovery

GL Trainor - Expert opinion on drug discovery, 2007 - Taylor & Francis
Plasma protein binding of drugs is a well-recognised phenomena, but it is only recently that
the implications for drug action in vivo have been fully appreciated. Plasma proteins, by …

Identification of antitumor activity of pyrazole oxime ethers

HJ Park, K Lee, SJ Park, B Ahn, JC Lee, HY Cho… - Bioorganic & medicinal …, 2005 - Elsevier
Identification of antitumor activity of pyrazole oxime ethers - ScienceDirect Skip to main
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Cyclin-dependent kinase-2 as a target for cancer therapy: progress in the development of CDK2 inhibitors as anti-cancer agents

TA Chohan, H Qian, Y Pan… - Current medicinal …, 2015 - ingentaconnect.com
Cyclin-dependent kinase-2 (CDK2) is a member of protein kinase family. It plays an
important role in regulating various events of eukaryotic cell division cycle. Accumulated …

Molecular mechanical study of halogen bonding in drug discovery

MAA Ibrahim - Journal of computational chemistry, 2011 - Wiley Online Library
A halogen bond is a noncovalent bond between a halogen atom (X) and a Lewis base (Y).
This type of bond is attributed to the anisotropic distribution of the charge density on the …

Cyclin dependent kinase 9 inhibitors for cancer therapy: miniperspective

YA Sonawane, MA Taylor, JV Napoleon… - Journal of medicinal …, 2016 - ACS Publications
Cyclin dependent kinase (CDK) inhibitors have been the topic of intense research for nearly
2 decades due to their widely varied and critical functions within the cell. Recently CDK9 has …