Evidence map›Paper›PMID 39569642›Full record

ReviewFuture medicinal chemistry2024

Insights into direct KRAS inhibition strategies for cancer treatment.

Tong Li, Chenglei Gu, Chen Zhou, Chunqin Mao, Kan Yang, Jinyi Xu, Tulin Lu, Jichao Chen

Abstract readReview
PubMed Full text at PMC Publisher
In one paragraph

Review in Future medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors.

Tong LiSchool of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
Chenglei GuSchool of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
Chen ZhouDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL 32610, United States.
Chunqin MaoSchool of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
Kan YangKey Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, 071002, China.
Jinyi XuState Key Laboratory of Natural Medicines & Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing, 210009, China.ORCID 0000-0002-1961-0402
Tulin LuSchool of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.
Jichao ChenSchool of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China.ORCID 0009-0001-8656-045X

Funding

Jiangsu Specially-Appointed Professors program No. 013038023001Nanjing Science and Technology Innovation Project for Overseas Talents No. 013062001012National Natural Science Foundation of China Nos. 82304285, 82003597Research Foundation of Nanjing University of Chinese Medicine No. 013038023001P
6 · The paper itself

Abstract

KRAS is the most commonly mutated isoform in RAS-driven cancers. In the early stage, KRAS was deemed as an "undruggable" cancer target due to the lack of suitable binding pockets. With the development of KRAS inhibitors in recent years, strategies that directly suppress oncogenic KRAS have achieved significant breakthroughs. In this review, we summarize recent advances in direct small-molecule KRAS inhibitors used for cancer therapy, highlighting their medicinal chemistry optimization processes. Moreover, new PROTACs targeting the KRAS mutation are also presented. Additionally, we put forward the challenges and prospects for the development of future KRAS inhibitors.

Indexed as

Antineoplastic AgentsNeoplasmsProto-Oncogene Proteins p21(ras)AnimalsHumansMutationSmall Molecule LibrariesAntineoplastic AgentsKRAS protein, humanProto-Oncogene Proteins p21(ras)Small Molecule LibrariesCancer treatmentKRAS mutationPROTACsSmall-molecule inhibitorStructural optimization

Identifiers

PMID39569642
PMCPMC11622815

What OpenQuestion holds

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.