L1 SAQ - Intro

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Name two major developments in the pharmaceutical industry related to cancer therapy.

Antibody based therapy and cell therapies.

What are the hallmarks of cancer?

Telomeres and cellular immortality, mechanisms of metastasis, angiogenesis and tumor formation, tumor associated inflammation, tumor as an organ.

What are the basic processes of the cell cycle?

DNA replication and cell division.

What is the major protein of erythrocytes?

Hemoglobin Signup and view all the answers

What is sickle cell anemia?

A genetic disorder of erythrocytes that affects the shape of red blood cells and causes symptoms like anemia, fatigue, pain, and swelling Signup and view all the answers

What did Linus Pauling discover about sickle cell anemia hemoglobin?

He found that sickle-cell anemia hemoglobin is molecularly distinct from normal hemoglobin and has an altered charge Signup and view all the answers

What is the role of Cdc7 kinase in DNA replication?

Cdc7 kinase plays a role in DNA replication by phosphorylating proteins involved in the initiation of DNA replication, such as Cdc6 and Mcm proteins. Signup and view all the answers

How do Cdc7 inhibitors work in cancer therapy?

Cdc7 inhibitors have potent antitumor activity by inhibiting the activity of Cdc7 kinase, which is essential for DNA replication in cancer cells. Signup and view all the answers

What is molecular medicine?

Molecular medicine is a branch of medicine that seeks to understand the causes and mechanisms of diseases at the molecular level, and applies this knowledge to the prevention, diagnosis, and treatment of diseases and disorders. Signup and view all the answers

What are the general concepts of cancers?

Types of tumors, Darwinian evolution of cancers, Signaling pathways and gatekeepers in cancer, DNA damage responses Signup and view all the answers

Which disease besides cancer has small-molecule kinase inhibitors been approved for?

Rheumatoid arthritis Signup and view all the answers

How many small-molecule kinase inhibitors (SMKIs) are currently approved by the FDA?

71 Signup and view all the answers

Approximately what percentage of the human kinome is represented by the targets of approved kinase inhibitors and the novel kinases being explored?

30% Signup and view all the answers

What are some trends in kinase inhibitor design mentioned in the article?

Development of allosteric and covalent inhibitors Signup and view all the answers

Which regulatory agency has approved the highest number of small-molecule kinase inhibitors (SMKIs)?

FDA Signup and view all the answers

Which kinase inhibitor has been approved for a non-oncology indication?

Baricitinib Signup and view all the answers

Which kinase family was the first to have an agent targeting it approved?

EGFR/HER Signup and view all the answers

Which regulatory agency has approved the highest number of monoclonal antibodies?

FDA Signup and view all the answers

Which major group of protein kinases do atypical protein kinases belong to?

Lipid kinases Signup and view all the answers

Which natural compound was pursued as a potential kinase inhibitor despite having poor selectivity?

Staurosporine Signup and view all the answers

What was the first kinase inhibitor to reach the market in the United States?

Sirolimus Signup and view all the answers

Which kinase inhibitor is perceived as a pivotal landmark in the development of kinase inhibitors?

Imatinib Signup and view all the answers

What is the main purpose of using CenterWatch as a resource for obtaining information on new kinase inhibitors entering clinical trials?

To provide weekly updates on drugs entering clinical trials Signup and view all the answers

Which of the following is NOT mentioned as a resource for obtaining information on the molecular targets of new kinase inhibitors entering clinical trials?

ClinicalTrials.gov Signup and view all the answers

What is the advantage of the methods used to create the dataset of kinase inhibitors in clinical trials?

It collates agents from different sources to obtain an exhaustive list Signup and view all the answers

What is the proportion of FDA-approved kinase inhibitors that are small molecule kinase inhibitors (SMKIs)?

Approximately 15% Signup and view all the answers

Which gene families are targeted by tirbanibulin?

NTRK, ABL, ALK, BTK, FLT3, KIT, MET Signup and view all the answers

Which mutations are considered sensitizing mutations associated with EGFR kinase domain?

Exon 21 and exon 19 deletions Signup and view all the answers

Which kinase inhibitors are approved by the FDA for the treatment of NSCLC?

All of the above Signup and view all the answers

Which gene rearrangement is identified in approximately 5% of NSCLC cases?

ALK rearrangement Signup and view all the answers

Which compound was discovered through a phenotypic screen using BCR-ABL-transformed cell lines?

GNF-2 Signup and view all the answers

What is the function of the myr pocket in the ABL kinase domain?

It binds to myristate and leads to an auto-inhibited conformation Signup and view all the answers

Which compound can induce an auto-inhibited conformation of the ABL-T315I mutant?

Asciminib Signup and view all the answers

What is the primary end point of the phase III trial involving asciminib?

Higher rate of major molecular responses than bosutinib Signup and view all the answers

Which compound is expected to have a regulatory submission in 2021?

Asciminib Signup and view all the answers

Which compound is among the most potent and specific ABL kinase inhibitors known to date?

ABL001 Signup and view all the answers

Which group of protein kinases are primarily targeted by the FDA-approved small-molecule kinase inhibitors (SMKIs)?

TK Signup and view all the answers

Which family of receptor tyrosine kinases (RTKs) is the most targeted by FDA-approved SMKIs?

HER Signup and view all the answers

How many FDA-approved SMKIs primarily target proteins within the TK group?

49 Signup and view all the answers

What is the most common indication for FDA-approved SMKIs and monoclonal antibodies (mAbs) that target kinases?

Oncology Signup and view all the answers

Which group of kinases is the most targeted by FDA-approved SMKIs?

TKL Signup and view all the answers

Which family of RTKs has the most FDA-approved SMKIs and mAbs targeting them?