Single-cell transcriptional changes associated with drug tolerance and response to combination therapies in cancer

Tags
Single-cell modleing
Affiliation
University of Illinois at Chicago
Article type
Research
Date
2023/12/16
Journal
Nature Comm.
Published Year
2021
keywords
Drug response prediction
Access to data: GSE149383
Novelty
Drug dose를 고려한 time-series single-cell RNA-seq 데이터 생산
LINCS 데이터를 활용한 drug combination identification pipeline 제안
Statistical test 기반
Hypothesis : Drug tolerance는 co-existence of heterogenous subpopulation 때문이다
Research question :다양한 subpopulation을 동시에 억제할 수 있는 drug combination을 찾는 다면 효과적인 치료가 되지 않을까?
keywords : cancer cell subpopulation, drug tolerant vs sensitive cells, Markers for drug tolerant cell populations

Background

EGFR mutation-positive Non-small-cell lung carcinoma (NSCLC)
NSCLC cell line: PC9 cell line (Exon 19 deletion in EGFR gene)
Targets
Epidermal growth factor receptor (EGFR)
T790M “gatekeeper” mutation in EGFR, which reportedly pre-exists or develops after several months of continuous treatment
Drugs (표적 치료제)
Erlotinib : targets and inhibits EGFR
Osimertinib : targets and inhibits EGFR
Significant variability in drug response at the level of individual cells
Drug-resistant colonies derived from a single cell were deficient in many known erlotinib-resistance mechanisms and was quite surprising and suggested that different surviving cells employ distinct mechanisms.
As genotyping and drug- sensitivity testing required high cell numbers, which usually could only be achieved after 12–16 weeks of expanding rare tolerant cells in culture, there was gap in analysis of genetic and epigenetic heterogeneity during the initial robust response to targeted therapy. → Exclusion of information regarding the earlier sequence of events

Goal

Inspection of cell-level drug response on earlier stage (~Day 19) after treatment
1.
Distinguishing drug-tolerant states
2.
Discovering unique cell subpopulations, likely reflecting functional heterogeneity of drug-tolerant cells
3.
Suggest drug combination with LINCS analysis (proposed by the authors)

Results

Diversity of drug-tolerant states

Resuming treatment after drug holiday restores tolerant cell populations and their markers

Common biological processes can be identified in tolerant subpopulations of distinct cell lines emerging from different treatments

Drug tolerant cells are highly heterogenous

Identify effective drug combinations

Efficacy of suggested drug combinations: Crizotinib + erlotinib

Cancer cell populations and potential drug sensitivity in patient tumors