ON6 Targeted Therapies

Descripción

(Oncology) PHCY320 Test sobre ON6 Targeted Therapies, creado por Mer Scott el 06/10/2019.
Mer Scott
Test por Mer Scott, actualizado hace más de 1 año
Mer Scott
Creado por Mer Scott hace alrededor de 5 años
3
0

Resumen del Recurso

Pregunta 1

Pregunta
Targeted cancer therapies are products of [blank_start]rational[blank_end] drug design, act on [blank_start]specific[blank_end] molecular targets, and are generally [blank_start]cytostatic[blank_end]. They interfere with specific molecules involved in cancer cell [blank_start]growth and survival[blank_end]. Can be: 1. [blank_start]Small molecule[blank_end] drugs, easily enter tumour cell or 2. [blank_start]Moncolonal antibodies[blank_end], bind to specific targets on cell surface
Respuesta
  • rational
  • specific
  • cytostatic
  • growth and survival
  • Small molecule
  • Moncolonal antibodies

Pregunta 2

Pregunta
Tumour associated antigens (TIAs) are optimal blocking targets.
Respuesta
  • True
  • False

Pregunta 3

Pregunta
Products of activated oncogenes include cell surface receptors that [blank_start]activate[blank_end] tyrosine kinases. Tyrosine kinase [blank_start]autophosphorylates[blank_end] the receptors in the cell to make: [blank_start]vascular endothelium[blank_end] derived growth factor receptors, human [blank_start]epidermal[blank_end] growth factor, and [blank_start]platelet[blank_end]-derived growth factor receptors. These stimulate [blank_start]proliferation[blank_end] and block [blank_start]apoptosis[blank_end]. Chromosomal abnormalities are in cancer cells but not normal cells. [blank_start]Thee[blank_end] fusion gene which causes the abnormality makes fusion proteins that[blank_start]. drive[blank_end] cancer development. We can identify cancerous proteins and [blank_start]block[blank_end] their production. Example: Chronic [blank_start]myeloid leukaemia[blank_end] often have the Philadelphia chromosome, which creates a [blank_start]BCR-ABL[blank_end] fusion protein. In cancer it causes constitutively active [blank_start]tyrosine kinase[blank_end] activity.
Respuesta
  • activate
  • autophosphorylates
  • vascular endothelium
  • epidermal
  • platelet
  • proliferation
  • apoptosis
  • The
  • drive
  • block
  • myeloid leukaemia
  • BCR-ABL
  • tyrosine kinase

Pregunta 4

Pregunta
Imatinib: First NIB approved by FDA. The suffix "nib" indicates a small-molecule [blank_start]inhibitor[blank_end] ("nib" is verbal shorthand for "inhibit") of kinase enzymes. - A small molecule [blank_start]intracellular[blank_end] inhibitor of tyrosine kinase - Treats chronic myeloid leukaemia; as it is selective for [blank_start]BCR-ABL[blank_end] TK fusion protein and competes with [blank_start]ATP[blank_end] for binding siten inhibiting phosphorylation (and [blank_start]proliferation[blank_end]). Other NIBs in clinical use: gefitinib, erlotinib, sorafenib, sunitinib, and dasatinib. - Share [blank_start]same[blank_end] mechanism of action (competitive ATP inhibition at catalytic binding site of TK) BUT difference is the [blank_start]spectrum[blank_end] of targeted kinases e.g. [blank_start]sunitinib[blank_end] inhibits signals from several Rs including VEGF and PDGRF families. NIBs are well tolerated but frequently cause [blank_start]myelosupression, rash, GI upset, fatigue[blank_end], arthralgia, & myalgia. Rarely cumulative cardiotoxicity: [blank_start]monitoring[blank_end] needed.
Respuesta
  • inhibitor
  • intracellular
  • BCR-ABL
  • proliferation
  • ATP
  • same
  • spectrum
  • sunitinib
  • myelosupression, rash, GI upset, fatigue
  • monitoring

Pregunta 5

Pregunta
Targeted therapy with monoclonal antibodies: Target is angiogenesis, specifically the key targets [blank_start]VEGF-A and VEGFR2[blank_end]. Bevacizumab (brand name Avastin): [blank_start]recombinant humanized[blank_end] monoclonal v VEGF-A, given by [blank_start]intravenous[blank_end] infusion, first line for [blank_start]colorectal, lung, renal[blank_end] cancer. Mode of action: Prevents VEGF-A [blank_start]binding[blank_end] and so prevents tumour vascularisation and growth. Serious unwanted effects:, [blank_start]Hyper[blank_end]tension • Infections (from [blank_start]neutropaenia[blank_end]), impaired [blank_start]would[blank_end] healing, bleeding, GI perforation, haemorrhage. [blank_start]DVT, PE[blank_end] in the elderly.
Respuesta
  • VEGF-A and VEGFR2
  • recombinant humanized
  • intravenous
  • colorectal, lung, & renal
  • binding
  • Hyper
  • neutropaenia
  • wound
  • DVT, PE

Pregunta 6

Pregunta
Target: Human epidermal growth factor 2 (HER-2) Receptor coupled [blank_start]enzyme[blank_end], binds to EGF. • Normally promotes growth and [blank_start]differentiation[blank_end] • Integral [blank_start]tyrosine kinase[blank_end] activity inhibits p27 (cyclin dependent cell cycle [blank_start]regulator[blank_end]) • Stimulates [blank_start]proliferation[blank_end] • HER2 is found in 20-30% of breast tumours.
Respuesta
  • enzyme
  • differentiation
  • tyrosine kinase
  • regulator
  • proliferation

Pregunta 7

Pregunta
Trastuzumab (Herceptin): [blank_start]Humanised mouse[blank_end] monoclonal of HER2, for [blank_start]metastatic[blank_end] breast cancer. Mode of action: G1 [blank_start]arrest[blank_end] - less proliferation(no change in HER2 expression). Downregulates [blank_start]kinase[blank_end] activation, causing less [blank_start]PI3K, Akt[blank_end], which activates [blank_start]p27[blank_end] and halts cell cycle. Pertuzumab: inhibits HER2 [blank_start]dimerisation[blank_end].
Respuesta
  • Humanised mouse
  • metastatic
  • arrest
  • kinase
  • PI3K, Akt
  • p27
  • dimerisation

Pregunta 8

Pregunta
Unwanted effects of monoclonal ABs: Mechanism dependent. Common: • [blank_start]Infusion[blank_end] related SEs ([blank_start]cytokine[blank_end] release syndrome), 1st infusion • [blank_start]Fever, chills,[blank_end] nausea and vomiting, hypersensitivity More Serious • [blank_start]Tumour Lysis Syndrome[blank_end] - release of cellular contents: high K+, P, uric acid, N, low Ca2+ = kidney [blank_start]failure[blank_end], seizures, [blank_start]cardiac[blank_end] arrhythmias, death. • Increased [blank_start]infection[blank_end] risk (HepB/reactivation) • Caution: autoimmune disease, HIV
Respuesta
  • Infusion
  • cytokine
  • Fever, chills,
  • Tumour Lysis Syndrome
  • failure
  • cardiac
  • infection

Pregunta 9

Pregunta
Target: Cell surface glycoproteins. [blank_start]CD20[blank_end] antigen found on the surface of normal and malignant B lymphocytes, function unknown. Can activate [blank_start]B[blank_end] cells. Drug: Rituxumab. Mediates B cell [blank_start]lysis[blank_end]. - [blank_start]Complement[blank_end] dependent cytotoxicity (CDCC) - [blank_start]Antibody[blank_end] dependent cell-mediated cytotoxicity (ADCC) - Apotosis • [blank_start]Increases[blank_end] NK cell success from 40-80% Unwanted effects, most serious: • Cardiomyopathy • [blank_start]Infusion[blank_end] related SEs • Hypersensitivity ([blank_start]first[blank_end] infusion) • Myelosupression
Respuesta
  • CD20
  • B
  • lysis
  • Complement
  • Antibody
  • Increases
  • Infusion
  • first
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