☆ 4.7 Review

Properties of FDA-approved small molecule protein kinase inhibitors: A 2023 update

PHARMACOLOGICAL RESEARCH (2023)

Related references

Note: Only part of the references are listed.

Review Oncology

The cure of leukemia through the optimist's prism

Hagop M. Kantarjian et al.

Summary: Treatment of leukemia is advancing rapidly, with the potential for cure in many types and improved survival rates overall. The use of new therapies and drugs tailored to different types of leukemia, along with optimized treatment regimens, is having a positive impact on patient survival rates.

CANCER (2022)

Add to Collection

Article Pharmacology & Pharmacy

Asciminib: First Approval

Emma D. Deeks

Summary: Asciminib is a drug developed by Novartis for the treatment of Ph+ CML. It targets BCR-ABL1 tyrosine kinase and is effective against resistant mutations. It has received accelerated and full approvals, and further research is being conducted on its potential in CML treatment.

DRUGS (2022)

Add to Collection

Article Chemistry, Medicinal

Small Molecule Kinase Inhibitor Drugs (1995-2021): Medical Indication, Pharmacology, and Synthesis

Cecilia C. Ayala-Aguilera et al.

Summary: Kinase inhibitors play a central role in the treatment of progressive disorders, with FDA approving 73 small molecule kinase inhibitor drugs by September 2021. This review summarizes the therapeutic and pharmacological properties of approved kinase inhibitors, as well as their synthesis routes, with an update on drugs approved in 2021.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Add to Collection

Article Biochemistry & Molecular Biology

Kincore: a web resource for structural classification of protein kinases and their inhibitors

Vivek Modi et al.

Summary: The study clustered kinase structures and provided an accessible resource Kincore, allowing users to query the database for conformational states and inhibitor types. This will aid in understanding the conformational dynamics of proteins and guide the development of inhibitors targeting specific states.

NUCLEIC ACIDS RESEARCH (2022)

Add to Collection

Review Pharmacology & Pharmacy

Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update

Robert Roskoski

Summary: Due to the dysregulation of protein kinase activity, this enzyme family has become one of the most important drug targets in the 21st century. There are 68 FDA-approved therapeutic agents that target protein kinases, with six new drugs approved in 2021. These drugs are mainly used in the treatment of neoplasms and inflammatory diseases, with 58 drugs prescribed for tumor treatment. In addition, 18 drugs are used for the treatment of multiple diseases. This review summarizes the physicochemical properties of all FDA-approved small molecule protein kinase inhibitors.

PHARMACOLOGICAL RESEARCH (2022)

Add to Collection

Article Hematology

Treatment-free remission in patients with chronic myeloid leukemia following the discontinuation of tyrosine kinase inhibitors

Fadi G. Haddad et al.

Summary: This study evaluated the outcome of TKI discontinuation in CML patients and identified factors associated with success rates of treatment-free remission (TFR). The study found that TFR is safe and feasible in patients with Ph-positive CML on TKI therapy. Achieving MR4 or MR4.5 for at least 5 years was correlated with a better outcome.

AMERICAN JOURNAL OF HEMATOLOGY (2022)

Add to Collection

Article Pharmacology & Pharmacy

Pacritinib: First Approval

Yvette N. Lamb

Summary: Pacritinib is an orally administered kinase inhibitor developed for the treatment of myelofibrosis and graft-versus-host disease. It has received accelerated approval in the USA for the treatment of specific types of myelofibrosis based on clinical trial results.

DRUGS (2022)

Add to Collection

Review Pharmacology & Pharmacy

Targeting BCR-Abl in the treatment of Philadelphia-chromosome positive chronic myelogenous leukemia

Robert Roskoski

Summary: Chronic myelogenous leukemia is a slow-growing malignant hematologic disease caused by the formation of the Philadelphia chromosome, resulting in the abnormal proliferation of white blood cells with the BCR-Abl fusion protein. Drugs like imatinib revolutionized the treatment of this disease, while Asciminib is a type IV inhibitor that blocks BCR-Abl activity by interacting with the myristate-binding site of Abl kinase.

PHARMACOLOGICAL RESEARCH (2022)

Add to Collection

Article Oncology

Futibatinib, an Irreversible FGFR1-4 Inhibitor, in Patients with Advanced Solid Tumors Harboring FGF/FGFR Aberrations: A Phase I Dose-Expansion Study

Funda Meric-Bernstam et al.

Summary: Futibatinib, a selective FGFR1-4 inhibitor, showed clinical activity in various solid tumors, particularly in FGFR2 fusion/rearrangement-positive intrahepatic cholangiocarcinoma. It also demonstrated efficacy in patients who developed resistance to prior FGFR inhibitors. These findings provide a basis for further clinical trials and highlight the importance of genomic profiling in identifying patients who may benefit from targeted therapy.

CANCER DISCOVERY (2022)

Add to Collection

Review Pharmacology & Pharmacy

A Comprehensive Overview of Globally Approved JAK Inhibitors

Ahmed M. Shawky et al.

Summary: This review discusses eleven JAK inhibitors that have been approved for clinical use, including their chemical and pharmacological data, inhibitory activities, pharmacological uses, crystal structures, and metabolic pathways and metabolites. This information can contribute to the design of new JAK inhibitors for the treatment of inflammatory and autoimmune diseases.

PHARMACEUTICS (2022)

Add to Collection

Review Biochemistry & Molecular Biology

Structural features of the protein kinase domain and targeted binding by small-molecule inhibitors

Chris Arter et al.

Summary: Protein kinases play a crucial role in cellular signaling pathways, and their regulation is diverse. They are important targets for drug discovery, and kinase inhibitors have shown significant therapeutic effects in specific patient groups. The selectivity of inhibitors depends on the differences between amino acids. Recently, researchers have been targeting allosteric pockets outside the ATP site to improve selectivity and overcome drug resistance.

JOURNAL OF BIOLOGICAL CHEMISTRY (2022)

Add to Collection

Review Pharmacology & Pharmacy

Janus kinase (JAK) inhibitors in the treatment of neoplastic and inflammatory disorders

Robert Roskoski

Summary: Janus kinase (JAK) family is a group of nonreceptor protein-tyrosine kinases that regulate mammalian cell signaling. They participate in multiple biological processes including inflammation, hematopoiesis, and immunity, together with various cytokines. Abnormal activation of JAKs is associated with inflammatory disorders and the development of different malignancies. Several JAK inhibitors have been developed and approved for the treatment of related diseases.

PHARMACOLOGICAL RESEARCH (2022)

Add to Collection

Article Hematology

Pacritinib for the treatment of patients with myelofibrosis and thrombocytopenia

John Mascarenhas

Summary: Myelofibrosis (MF) is a rare myeloproliferative neoplasm characterized by a complex symptom profile, cytopenias, splenomegaly, and potential for leukemic progression. Pacritinib, a potent Janus kinase (JAK) 2/interleukin-1 receptor-associated kinase 1 (IRAK1) inhibitor, has demonstrated significant reduction in splenomegaly, improved symptom control, and a manageable safety profile in patients with MF regardless of the severity of thrombocytopenia. Pacritinib offers MF patients with severe thrombocytopenia a new treatment option.

EXPERT REVIEW OF HEMATOLOGY (2022)

Add to Collection

Review Biochemistry & Molecular Biology

Molecular targeted therapy for anticancer treatment

Hye-Young Min et al.

Summary: Molecular targeted therapy has become a fundamental approach in precision medicine for cancer treatment, offering efficient anticancer effects with fewer side effects. However, drug resistance remains a major drawback that needs to be overcome to improve therapeutic efficacy.

EXPERIMENTAL AND MOLECULAR MEDICINE (2022)

Add to Collection

Article Biochemistry & Molecular Biology

The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification

Carrow I. Wells et al.

Summary: The chemogenomic set of protein kinase inhibitors described in this study is a valuable open science resource for studying kinase biology, consisting of 187 inhibitors that target 215 human kinases. It is highly annotated and selective, making it a useful tool for researchers in cell-based screens.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

Add to Collection

Article Pharmacology & Pharmacy

Abrocitinib: First Approval

Emma D. Deeks et al.

Summary: Abrocitinib is an oral small-molecule inhibitor of JAK1 developed by Pfizer for moderate-to-severe atopic dermatitis, approved in the UK, Japan, and the EU, with regulatory applications under review in other countries. This marks the first approval for treating moderate-to-severe AD with this medication.

DRUGS (2021)

Add to Collection

Article Chemistry, Medicinal

Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases

Zhouling Xie et al.

Summary: Kinase inhibitors have been successful in treating various diseases beyond cancer, including autoimmune diseases and inflammatory diseases. Several non-oncologic small-molecule kinase inhibitors have been approved, with more in development for different applications.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Add to Collection

Review Pharmacology & Pharmacy

Properties of FDA-approved small molecule protein kinase inhibitors: A 2021 update

Robert Roskoski

Summary: This article discusses the importance of protein kinase inhibitors in drug therapy, covering the therapeutic targets, types, and indications of 62 FDA-approved drugs. It summarizes the physicochemical properties of these drugs, emphasizing their wide applications in the treatment of diseases such as tumors and inflammatory conditions.

PHARMACOLOGICAL RESEARCH (2021)

Add to Collection

Review Pharmacology & Pharmacy

Orally effective FDA-approved protein kinase targeted covalent inhibitors (TCIs)

Robert Roskoski

Summary: This article discusses the important role of protein kinase inhibitors in treating human diseases such as cancer, introducing some successful examples and the mechanism of covalent inhibitors.

PHARMACOLOGICAL RESEARCH (2021)

Add to Collection

Review Pharmacology & Pharmacy

Posttranslational modifications as therapeutic targets for intestinal disorders

Jieun Choo et al.

Summary: Posttranslational modifications regulate biological processes and play crucial roles in intestinal diseases research, serving as potential novel biomarkers and therapeutic targets.

PHARMACOLOGICAL RESEARCH (2021)

Add to Collection

Review Pharmacology & Pharmacy

Blockade of mutant RAS oncogenic signaling with a special emphasis on KRAS

Robert Roskoski

Summary: RAS proteins play crucial roles in physiological signal transduction processes related to cell growth, division, and survival. RAS mutations, especially KRAS mutations, are common in various cancers, with potential implications for targeted therapy. Covalent modification of the KRAS C12 led to the discovery of a new pocket, facilitating the development of second-line treatment for KRAS(G12C)-mutant non-small cell lung cancer. Efforts are also being made to develop inhibitors targeting MAP kinase and PI3-kinase pathways as indirect RAS antagonists.

PHARMACOLOGICAL RESEARCH (2021)

Add to Collection

Review Biochemistry & Molecular Biology

From structure to the dynamic regulation of a molecular switch: A journey over 3 decades

Susan S. Taylor et al.

Summary: The Protein Data Bank has played a crucial role in the signaling community for over 30 years, facilitating information sharing between academics and industry. Through the study of protein kinases, particularly cAMP-dependent protein kinase, researchers have made significant discoveries including the importance of crystal packing in biological processes and disease relevance. Integrating crystallography with other techniques is opening up new possibilities for understanding intrinsically disordered regions and dynamic biological processes.

JOURNAL OF BIOLOGICAL CHEMISTRY (2021)

Add to Collection

Article Chemistry, Medicinal

Target-Based Evaluation of Drug-Like Properties and Ligand Efficiencies

Paul D. Leeson et al.

Summary: The study compares the physicochemical properties of drugs approved between 2010-2020 with compounds reported to bind to their efficacious target. It finds that drugs differ from their target comparators in terms of potency, ligand efficiency, and other descriptors. Furthermore, 96% of drugs have values of LE or LLE greater than the median values of their target comparator compounds.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Add to Collection

Review Biotechnology & Applied Microbiology

Kinase drug discovery 20 years after imatinib: progress and future directions

Philip Cohen et al.

Summary: Advances in improving the potency and specificity of small-molecule protein kinase inhibitors over the past 20 years have had a significant impact on the treatment of cancers and non-cancerous conditions. Efforts are being made to address the challenge of drug resistance to kinase inhibitors, and future directions in kinase drug discovery are being discussed.

NATURE REVIEWS DRUG DISCOVERY (2021)

Add to Collection

Review Medicine, General & Internal

Chronic myeloid leukaemia

Jorge Cortes et al.

Summary: Tyrosine-kinase inhibitors have significantly altered the natural course of chronic myeloid leukaemia, allowing some patients to approach a near-normal life expectancy. Successful treatment requires understanding the patient's treatment goals, monitoring optimal response hallmarks, timely interventions, recognition of adverse events, and management of comorbidities.

LANCET (2021)

Add to Collection

Review Biotechnology & Applied Microbiology

Trends in kinase drug discovery: targets, indications and inhibitor design

Misty M. Attwood et al.

Summary: The article analyzes the landscape of approved and investigational therapies that target kinases, highlighting the increasing importance of kinase inhibitors in oncology and beyond. It discusses trends in kinase inhibitor design and points out that there are still substantial unexplored opportunities for this drug class.

NATURE REVIEWS DRUG DISCOVERY (2021)

Add to Collection

Review Pharmacology & Pharmacy

Properties of FDA-approved small molecule phosphatidylinositol 3-kinase inhibitors prescribed for the treatment of malignancies

Robert Roskoski

Summary: The discovery of the phosphatidylinositol 3-kinase (PI 3-kinase) pathway has provided a major advance in understanding eukaryotic signal transduction, leading to the development of drugs targeting oncogenic mutants. PI 3-kinases are divided into three classes, with Class I PI 3-kinases being the main subject, catalyzing the phosphorylation of phosphatidylinositol-4,5-bisphosphate (PI-4,5-P2) to generate phosphatidylinositol-3,4,5-trisphosphate (PIP3). These kinases interact with various receptor and regulatory subunits to affect cell growth and survival.

PHARMACOLOGICAL RESEARCH (2021)

Add to Collection

Review Pharmacology & Pharmacy

Hydrophobic and polar interactions of FDA-approved small molecule protein kinase inhibitors with their target enzymes

Robert Roskoski

Summary: Dysregulation and mutations of protein kinases are involved in various diseases, making targeted inhibitors increasingly important for treatments. FDA-approved drugs mainly interact with kinase residues in the small lobe and hinge-linker region, with type IIA inhibitors having the most hydrophobic interactions with their targets. Further studies on protein kinase signaling pathways hold promise for biomedical breakthroughs.

PHARMACOLOGICAL RESEARCH (2021)

Add to Collection

Article Multidisciplinary Sciences

Crowdsourced mapping of unexplored target space of kinase inhibitors

Anna Cichonska et al.

Summary: By benchmarking predictive algorithms on unpublished bioactivity data, it was found that ensemble models based on various approaches can improve prediction accuracy and accelerate experimental mapping of unexplored compound-kinase interactions.

NATURE COMMUNICATIONS (2021)

Add to Collection

Article Biochemistry & Molecular Biology

KinaseMD: kinase mutations and drug response database

Ruifeng Hu et al.

Summary: Mutations in kinases play a critical role in studying signaling pathways and regulatory roles in human diseases, especially cancer. The newly constructed database KinaseMD provides structural and functional annotations for kinase mutations, including information on drug response and resistance. This database serves as a centralized resource for researchers to access the most up-to-date information on kinase mutations and drug response.

NUCLEIC ACIDS RESEARCH (2021)

Add to Collection

Review Chemistry, Multidisciplinary

New Promise and Opportunities for Allosteric Kinase Inhibitors

Xiaoyun Lu et al.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2020)

Add to Collection

Review Pharmacology & Pharmacy

The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2020)

Add to Collection

Review Pharmacology & Pharmacy

Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2020)

Add to Collection

Review Pharmacology & Pharmacy

The role of small molecule Flt3 receptor protein-tyrosine kinase inhibitors in the treatment of Flt3-positive acute myelogenous leukemias

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2020)

Add to Collection

Review Oncology

The specificity of asciminib, a potential treatment for chronic myeloid leukemia, as a myristate-pocket binding ABL inhibitor and analysis of its interactions with mutant forms of BCR-ABL1 kinase

Paul W. Manley et al.

LEUKEMIA RESEARCH (2020)

Add to Collection

Review Oncology

Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001-2020)

Liling Huang et al.

JOURNAL OF HEMATOLOGY & ONCOLOGY (2020)

Add to Collection

Review Pharmacology & Pharmacy

Properties of FDA-approved small molecule protein kinase inhibitors

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2019)

Add to Collection

Article Multidisciplinary Sciences

Defining a new nomenclature for the structures of active and inactive kinases

Vivek Modi et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2019)

Add to Collection

Review Pharmacology & Pharmacy

Targeting ERK1/2 protein-serine/threonine kinases in human cancers

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2019)

Add to Collection

Article Oncology

TAS-120 Overcomes Resistance to ATP-Compartitive FGFR Inhibitors in Patients with FGFR2 Fusion-Positive Intrahepatic Cholanjiocarcinoma

Lipika Goyal et al.

CANCER DISCOVERY (2019)

Add to Collection

Review Pharmacology & Pharmacy

The new entries in the therapeutic armamentarium: The small molecule JAK inhibitors

Katie Bechman et al.

PHARMACOLOGICAL RESEARCH (2019)

Add to Collection

Article Biochemistry & Molecular Biology

Surprising Non-Additivity of Methyl Groups in Drug Kinase Interaction

Barbara Wienen-Schmidt et al.

ACS CHEMICAL BIOLOGY (2019)

Add to Collection

Review Pharmacology & Pharmacy

The Landscape of Atypical and Eukaryotic Protein Kinases

Georgi K. Kanev et al.

TRENDS IN PHARMACOLOGICAL SCIENCES (2019)

Add to Collection

Article Chemistry, Medicinal

TAS-120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure

Maria Kalyukina et al.

CHEMMEDCHEM (2019)

Add to Collection

Review Pharmacology & Pharmacy

Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2019)

Add to Collection

Review Pharmacology & Pharmacy

Cyclin-dependent protein serine/threonine kinase inhibitors as anticancer drugs

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2019)

Add to Collection

Article Chemistry, Medicinal

Identification of N-{cis-3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)aminolcyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases

Michael L. Vazquez et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Add to Collection

Article Biochemistry & Molecular Biology

PKIDB: A Curated, Annotated and Updated Database of Protein Kinase Inhibitors in Clinical Trials

Fabrice Carles et al.

MOLECULES (2018)

Add to Collection

Correction Biotechnology & Applied Microbiology

Unexplored therapeutic opportunities in the human genome (vol 17, pg 317, 2018)

Tudor I. Oprea et al.

NATURE REVIEWS DRUG DISCOVERY (2018)

Add to Collection

Review Pharmacology & Pharmacy

Role of RET protein-tyrosine kinase inhibitors in the treatment RET-driven thyroid and lung cancers

Robert Roskoski et al.

PHARMACOLOGICAL RESEARCH (2018)

Add to Collection

Review Pharmacology & Pharmacy

The role of small molecule Kit protein-tyrosine kinase inhibitors in the treatment of neoplastic disorders

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2018)

Add to Collection

Review Pharmacology & Pharmacy

The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2018)

Add to Collection

Article Chemistry, Medicinal

Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1

Joseph Schoepfer et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Add to Collection

Review Pharmacology & Pharmacy

Targeting oncogenic Raf protein-serine/threonine kinases in human cancers

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2018)

Add to Collection

Article Biochemistry & Molecular Biology

Redefining the Protein Kinase Conformational Space with Machine Learning

Peter Man-Un Ung et al.

CELL CHEMICAL BIOLOGY (2018)

Add to Collection

Article Chemistry, Medicinal

Approved and Experimental Small-Molecule Oncology Kinase Inhibitor Drugs: A Mid-2016 Overview

Peter M. Fischer

MEDICINAL RESEARCH REVIEWS (2017)

Add to Collection

Review Pharmacology & Pharmacy

Anaplastic lymphoma kinase (ALK) inhibitors in the treatment of ALK-driven lung cancers

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2017)

Add to Collection

Review Pharmacology & Pharmacy

ROS1 protein-tyrosine kinase inhibitors in the treatment of ROS1 fusion protein-driven non-small cell lung cancers

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2017)

Add to Collection

Review Pharmacology & Pharmacy

Vascular endothelial growth factor (VEGF) and VEGF receptor inhibitors in the treatment of renal cell carcinomas

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2017)

Add to Collection

Review Pharmacology & Pharmacy

Allosteric MEK1/2 inhibitors including cobimetanib and trametinib in the treatment of cutaneous melanomas

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2017)

Add to Collection

Review Chemistry, Medicinal

Structure-based Virtual Screening Approaches in Kinase-directed Drug Discovery

David Bajusz et al.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2017)

Add to Collection

Article Chemistry, Medicinal

AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective

Samuel H. Myers et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

Add to Collection

Article Biochemistry & Molecular Biology

KLIFS: a structural kinase-ligand interaction database

Albert J. Kooistra et al.

NUCLEIC ACIDS RESEARCH (2016)

Add to Collection

Article Chemistry, Multidisciplinary

Thermodynamic Proxies to Compensate for Biases in Drug Discovery Methods

Sean Ekins et al.

PHARMACEUTICAL RESEARCH (2016)

Add to Collection

Review Pharmacology & Pharmacy

Molecular inflation, attrition and the rule of five

Paul D. Leeson

ADVANCED DRUG DELIVERY REVIEWS (2016)

Add to Collection

Review Pharmacology & Pharmacy

Quality guidelines for oral drug candidates: dose, solubility and lipophilicity

Martin K. Bayliss et al.

DRUG DISCOVERY TODAY (2016)

Add to Collection

Review Pharmacology & Pharmacy

Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2016)

Add to Collection

Review Pharmacology & Pharmacy

Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2016)

Add to Collection

Article Pharmacology & Pharmacy

Ibrutinib inhibition of Bruton protein-tyrosine kinase (BTK) in the treatment of B cell neoplasms

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2016)

Add to Collection

Review Pharmacology & Pharmacy

Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2016)

Add to Collection

Review Oncology

Use of Second- and Third-Generation Tyrosine Kinase Inhibitors in the Treatment of Chronic Myeloid Leukemia: An Evolving Treatment Paradigm

Elias Jabbour et al.

CLINICAL LYMPHOMA MYELOMA & LEUKEMIA (2015)

Add to Collection

Review Pharmacology & Pharmacy

A historical overview of protein kinases and their targeted small molecule inhibitors

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2015)

Add to Collection

Review Pharmacology & Pharmacy

Src protein-tyrosine kinase structure, mechanism, and small molecule inhibitors

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2015)

Add to Collection

Review Biochemistry & Molecular Biology

Dynamics-Driven Allostery in Protein Kinases

Alexandr P. Kornev et al.

TRENDS IN BIOCHEMICAL SCIENCES (2015)

Add to Collection

Review Pharmacology & Pharmacy

FDA-approved small-molecule kinase inhibitors

Peng Wu et al.

TRENDS IN PHARMACOLOGICAL SCIENCES (2015)

Add to Collection

Article Hematology

Relative survival in patients with chronic-phase chronic myeloid leukaemia in the tyrosine-kinase inhibitor era: analysis of patient data from six prospective clinical trials

Koji Sasaki et al.

LANCET HAEMATOLOGY (2015)

Add to Collection

Article Chemistry, Medicinal

KLIFS: A Knowledge-Based Structural Database To Navigate Kinase-Ligand Interaction Space

Oscar P. J. van Linden et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Add to Collection

Article Chemistry, Medicinal

Physicochemical Descriptors of Aromatic Character and Their Use in Drug Discovery

Timothy J. Ritchie et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Add to Collection

Article Biotechnology & Applied Microbiology

The role of ligand efficiency metrics in drug discovery

Andrew L. Hopkins et al.

NATURE REVIEWS DRUG DISCOVERY (2014)

Add to Collection

Review Pharmacology & Pharmacy

ErbB/HER protein-tyrosine kinases: Structures and small molecule inhibitors

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2014)

Add to Collection

Review Pharmacology & Pharmacy

The ErbB/HER family of protein-tyrosine kinases and cancer

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2014)

Add to Collection

Review Pharmacology & Pharmacy

The preclinical profile of crizotinib for the treatment of non-small-cell lung cancer and other neoplastic disorders

Robert Roskoski

EXPERT OPINION ON DRUG DISCOVERY (2013)

Add to Collection

Review Biochemistry & Molecular Biology

Polyproline-II Helix in Proteins: Structure and Function

Alexei A. Adzhubei et al.

JOURNAL OF MOLECULAR BIOLOGY (2013)

Add to Collection

Review Pharmacology & Pharmacy

Anaplastic lymphoma kinase (ALK): Structure, oncogenic activation, and pharmacological inhibition

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2013)

Add to Collection

Review Biochemistry & Molecular Biology

Approaches to discover non-ATP site kinase inhibitors

Lori Krim Gavrin et al.

MEDCHEMCOMM (2013)

Add to Collection

Article Biochemistry & Molecular Biology

Deciphering the Structural Basis of Eukaryotic Protein Kinase Regulation

Hiruy S. Meharena et al.

PLOS BIOLOGY (2013)

Add to Collection

Review Biochemistry & Molecular Biology

MEK1/2 dual-specificity protein kinases: Structure and regulation

Robert Roskoski

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2012)

Add to Collection

Review Pharmacology & Pharmacy

New Directions in Targeting Protein Kinases: Focusing Upon True Allosteric and Bivalent Inhibitors

Vandana Lamba et al.

CURRENT PHARMACEUTICAL DESIGN (2012)

Add to Collection

Review Biochemistry & Molecular Biology

The language of SH2 domain interactions defines phosphotyrosine-mediated signal transduction

Bernard A. Liu et al.

FEBS LETTERS (2012)

Add to Collection

Article Chemistry, Medicinal

Discovery of a Novel Class of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (c-MET) Protein Kinase Inhibitors and Identification of the Clinical Candidate 2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the Treatment of Cancer

J. Jean Cui et al.

JOURNAL OF MEDICINAL CHEMISTRY (2012)

Add to Collection

Review Pharmacology & Pharmacy

ERK1/2 MAP kinases: Structure, function, and regulation

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2012)

Add to Collection

Review Biochemistry & Molecular Biology

The Evolution of Protein Kinase Inhibitors from Antagonists to Agonists of Cellular Signaling

Arvin C. Dar et al.

ANNUAL REVIEW OF BIOCHEMISTRY, VOL 80 (2011)

Add to Collection

Review Biochemistry & Molecular Biology

Protein kinase biochemistry and drug discovery

Phillip A. Schwartz et al.

BIOORGANIC CHEMISTRY (2011)

Add to Collection

Article Biochemistry & Molecular Biology

Discovery and Characterization of a Cell-Permeable, Small-Molecule c-Abl Kinase Activator that Binds to the Myristoyl Binding Site

Jingsong Yang et al.

CHEMISTRY & BIOLOGY (2011)

Add to Collection

Review Biochemistry & Molecular Biology

RAF protein-serine/threonine kinases: Structure and regulation

Robert Roskoski

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2010)

Add to Collection

Article Biochemistry & Molecular Biology

Defining the conserved internal architecture of a protein kinase

Alexandr P. Kornev et al.

BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS (2010)

Add to Collection

Article Chemistry, Medicinal

Through the Gatekeeper Door: Exploiting the Active Kinase Conformation

Fabio Zuccotto et al.

JOURNAL OF MEDICINAL CHEMISTRY (2010)

Add to Collection

Article Biochemistry & Molecular Biology

cAMP-dependent protein kinase: Crystallographic insights into substrate recognition and phosphotransfer

Madhusudan et al.

PROTEIN SCIENCE (2010)

Add to Collection

Article Multidisciplinary Sciences

A helix scaffold for the assembly of active protein kinases

Alexandr P. Kornev et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2008)

Add to Collection

Article Biotechnology & Applied Microbiology

The influence of drug-like concepts on decision-making in medicinal chemistry

Paul D. Leeson et al.

NATURE REVIEWS DRUG DISCOVERY (2007)

Add to Collection

Review Chemistry, Medicinal

Molecular recognition of protein kinase binding pockets for design of potent and selective kinase inhibitors

Jeffrey Jie-Lou Liao

JOURNAL OF MEDICINAL CHEMISTRY (2007)

Add to Collection

Article Multidisciplinary Sciences

Surface comparison of active and inactive protein kinases identifies a conserved activation mechanism

Alexandr P. Kornev et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2006)

Add to Collection

Article Biotechnology & Applied Microbiology

Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia

BL Roth et al.

NATURE REVIEWS DRUG DISCOVERY (2004)

Add to Collection

Review Cell Biology

Regulation of the C-Abl and Bcr-Abl tyrosine kinases

O Hantschel et al.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2004)

Add to Collection

Article Biochemistry & Molecular Biology

A myristoyl/phosphotyrosine switch regulates c-Abl

O Hantschel et al.

CELL (2003)

Add to Collection

Article Multidisciplinary Sciences

The protein kinase complement of the human genome

G Manning et al.

SCIENCE (2002)

Add to Collection

Article Chemistry, Medicinal

Molecular properties that influence the oral bioavailability of drug candidates

DF Veber et al.

JOURNAL OF MEDICINAL CHEMISTRY (2002)

Add to Collection

Article Biotechnology & Applied Microbiology

Protein kinases - the major drug targets of the twenty-first century?

P Cohen

NATURE REVIEWS DRUG DISCOVERY (2002)

Add to Collection

© Peeref 2019-2024. All rights reserved.