| [1] |
Bray F, Laversanne M, Sung H, et al. Global cancer statistics 2022: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries[J]. CA Cancer J Clin, 2024, 74(3): 229-263.
|
| [2] |
Han J, Zhang B, Zhang Y, et al. Gut microbiome: decision-makers in the microenvironment of colorectal cancer[J]. Front Cell Infect Microbiol, 2023, 13: 1299977.
|
| [3] |
Toure M, Crews CM. Small-molecule PROTACS: new approaches to protein degradation[J]. Angew Chem Int Ed Engl, 2016, 55(6): 1966-1973.
|
| [4] |
Hu Z, Crews CM. Recent developments in PROTAC-mediated protein degradation: from bench to clinic[J]. Chembiochem, 2022, 23(2): e202100270.
|
| [5] |
Sakamoto KM, Kim KB, Kumagai A, et al. Protacs: chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation[J]. Proc Natl Acad Sci USA, 2001, 98(15): 8554-8559.
|
| [6] |
Békés M, Langley DR, Crews CM. PROTAC targeted protein degraders: the past is prologue[J]. Nat Rev Drug Discov, 2022, 21(3): 181-200.
|
| [7] |
Zhao LP, Zheng RR, Rao XN, et al. Chemotherapy-enabled colorectal cancer immunotherapy of self-delivery nano-PROTACs by inhibiting tumor glycolysis and avoiding adaptive immune resistance[J]. Adv Sci (Weinh), 2024, 11(15): e2309204.
|
| [8] |
Bannoura SF, Khan HY, Azmi AS. KRAS G12D targeted therapies for pancreatic cancer: has the fortress been conquered?[J]. Front Oncol, 2022, 12: 1013902.
|
| [9] |
Dong P, Ni J, Zheng X, et al. Small molecules for Kirsten rat sarcoma viral oncogene homolog mutant cancers: past, present, and future[J]. Eur J Pharmacol, 2025, 996: 177428.
|
| [10] |
Watterson A, Coelho MA. Cancer immune evasion through KRAS and PD-L1 and potential therapeutic interventions[J]. Cell Commun Signal, 2023, 21(1): 45.
|
| [11] |
Yin Y, Liu B, Cao Y, et al. Colorectal cancer-derived small extracellular vesicles promote tumor immune evasion by upregulating PD-L1 expression in tumor-associated macrophages[J]. Adv Sci (Weinh), 2022, 9(9): 2102620.
|
| [12] |
Dias Carvalho P, Guimarães CF, Cardoso AP, et al. KRAS oncogenic signaling extends beyond cancer cells to orchestrate the microenvironment[J]. Cancer Res, 2018, 78(1): 7-14.
|
| [13] |
Lal N, White BS, Goussous G, et al. KRAS mutation and consensus molecular subtypes 2 and 3 are independently associated with reduced immune infiltration and reactivity in colorectal cancer[J]. Clin Cancer Res, 2018, 24(1): 224-233.
|
| [14] |
Lv Y, Yang Z, Chen Y, et al. A potent SOS1 PROTAC degrader with synergistic efficacy in combination with KRASG12C inhibitor[J]. J Med Chem, 2024, 67(4): 2487-2511.
|
| [15] |
Khan S, Wiegand J, Zhang P, et al. BCL-XL PROTAC degrader DT2216 synergizes with sotorasib in preclinical models of KRASG12C-mutated cancers[J]. J Hematol Oncol, 2022, 15(1): 23.
|
| [16] |
Bian Y, Alem D, Beato F, et al. Development of SOS1 inhibitor-based degraders to target KRAS-mutant colorectal cancer[J]. J Med Chem, 2022, 65(24): 16432-16450.
|
| [17] |
Cheng J, Li Y, Wang X, et al. Discovery of novel PDEδ degraders for the treatment of KRAS mutant colorectal cancer[J]. J Med Chem, 2020, 63(14): 7892-7905.
|
| [18] |
Hogg SJ, Beavis PA, Dawson MA, et al. Targeting the epigenetic regulation of antitumour immunity[J]. Nat Rev Drug Discov, 2020, 19(11): 776-800.
|
| [19] |
Liu Z, Zhang Y, Xiang Y, et al. Small-molecule PROTACs for cancer immunotherapy[J]. Molecules, 2022, 27(17): 5439.
|
| [20] |
Tong J, Tan X, Risnik D, et al. BET protein degradation triggers DR5-mediated immunogenic cell death to suppress colorectal cancer and potentiate immune checkpoint blockade[J]. Oncogene, 2021, 40(48): 6566-6578.
|
| [21] |
Deng Z, Catlett J, Lee Y, et al. Harnessing the SPOP E3 ubiquitin ligase via a bridged proteolysis targeting chimera (PROTAC) strategy for targeted protein degradation[J]. J Med Chem, 2025, 68(8): 8634-8647.
|
| [22] |
Sharma BR, Karki R, Sundaram B, et al. The transcription factor IRF9 promotes colorectal cancer via modulating the IL-6/STAT3 signaling axis[J]. Cancers (Basel), 2022, 14(4): 919.
|
| [23] |
Jin J, Wu Y, Zhao Z, et al. Small-molecule PROTAC mediates targeted protein degradation to treat STAT3-dependent epithelial cancer[J]. JCI Insight, 2022, 7(22): e160606.
|
| [24] |
Kapoor S, Gustafson T, Zhang M, et al. Deacetylase Plus Bromodomain Inhibition Downregulates ERCC2 and Suppresses the Growth of Metastatic Colon Cancer Cells[J]. Cancers (Basel), 2021, 13(6): 1438.
|
| [25] |
Wu M, Jiang Y, Zhang D, et al. Discovery of a potent PARP1 PROTAC as a chemosensitizer for the treatment of colorectal cancer[J]. Eur J Med Chem, 2025, 282: 117062.
|
| [26] |
Whittaker SR, Mallinger A, Workman P, et al. Inhibitors of cyclin-dependent kinases as cancer therapeutics[J]. Pharmacol Ther, 2017, 173: 83-105.
|
| [27] |
Nieto-Jiménez C, Morafraile EC, Alonso-Moreno C, et al. Clinical considerations for the design of PROTACs in cancer[J]. Mol Cancer, 2022, 21(1): 67.
|
| [28] |
Huang Z, Zhang K, Jiang Y, et al. Molecular glue triggers degradation of PHGDH by enhancing the interaction between DDB1 and PHGDH[J]. Acta Pharm Sin B, 2024, 14(9): 4001-4013.
|
| [29] |
Huang M, Huang Y, Guo J, et al. Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors[J]. Eur J Med Chem, 2021, 211: 113023.
|
| [30] |
Lu J, Huang Y, Huang J, et al. Discovery of the first examples of threonine tyrosine kinase PROTAC degraders[J]. J Med Chem, 2022, 65(3): 2313-2328.
|
| [31] |
Zheng D, Li J, Yan H, et al. Emerging roles of aurora-a kinase in cancer therapy resistance[J]. Acta Pharm Sin B, 2023, 13(7): 2826-2843.
|
| [32] |
Wang Q, Lu Q, Jia S, et al. Gut immune microenvironment and autoimmunity[J]. Int Immunopharmacol, 2023, 124(Pt A): 110842.
|
| [33] |
Zhao H, Ming T, Tang S, et al. Wnt signaling in colorectal cancer: pathogenic role and therapeutic target[J]. Mol Cancer, 2022, 21(1): 144.
|
| [34] |
Hu X, Li J, Fu M, et al. The JAK/STAT signaling pathway: from bench to clinic[J]. Signal Transduct Target Ther, 2021, 6(1): 402.
|
| [35] |
Guryanova SV, Maksimova TV, Azova MM. Transcription factors and methods for the pharmacological correction of their activity[J]. Int J Mol Sci, 2025, 26(13): 6394.
|
| [36] |
Liao H, Li X, Zhao L, et al. A PROTAC peptide induces durable β-catenin degradation and suppresses Wnt-dependent intestinal cancer[J]. Cell Discov, 2020, 6: 35.
|
| [37] |
Hirano T, Hirayama D, Wagatsuma K, et al. Immunological mechanisms in inflammation-associated colon carcinogenesis[J]. Int J Mol Sci, 2020, 21(9): 3062.
|
| [38] |
Gargalionis AN, Papavassiliou KA, Papavassiliou AG. Targeting STAT3 signaling pathway in colorectal cancer[J]. Biomedicines, 2021, 9(8): 1016.
|
| [39] |
Zhou H, Bai L, Xu R, et al. Structure-based discovery of SD-36 as a potent, selective, and efficacious PROTAC degrader of STAT3 protein[J]. J Med Chem, 2019, 62(24): 11280-11300.
|
| [40] |
Gadd MS, Testa A, Lucas X, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation[J]. Nat Chem Biol, 2017, 13(5): 514-521.
|
| [41] |
Nafie MS, Diab MK, Yassen ASA, et al. Next-generation proteolysis-targeting chimeras in precision oncology: multifunctional designs, emerging modalities, and translational prospects in targeted protein degradation[J]. Drug Dev Res, 2025, 86(8): e70192.
|
| [42] |
Kroemer G, Galassi C, Zitvogel L, et al. Immunogenic cell stress and death[J]. Nat Immunol, 2022, 23(4): 487-500.
|
| [43] |
Yan H, Wang Z, Teng D, et al. Hexokinase 2 senses fructose in tumor-associated macrophages to promote colorectal cancer growth[J]. Cell Metab, 2024, 36(11): 2449-2467.e2446.
|
| [44] |
Lin TY, Gu SY, Lin YH, et al. Paclitaxel-resistance facilitates glycolytic metabolism via Hexokinase-2-regulated ABC and SLC transporter genes in ovarian clear cell carcinoma[J]. Biomed Pharmacother, 2024, 180: 117452.
|
| [45] |
Fischer K, Hoffmann P, Voelkl S, et al. Inhibitory effect of tumor cell-derived lactic acid on human T cells[J]. Blood, 2007, 109(9): 3812-3819.
|
| [46] |
Colegio OR, Chu NQ, Szabo AL, et al. Functional polarization of tumour-associated macrophages by tumour-derived lactic acid[J]. Nature, 2014, 513(7519): 559-563.
|
| [47] |
Sang R, Fan R, Deng A, et al. Degradation of hexokinase 2 blocks glycolysis and induces gsdme-dependent pyroptosis to amplify immunogenic cell death for breast cancer therapy[J]. J Med Chem, 2023, 66(13): 8464-8483.
|
| [48] |
Mashima T, Seimiya H, Tsuruo T. De novo fatty-acid synthesis and related pathways as molecular targets for cancer therapy[J]. Br J Cancer, 2009, 100(9): 1369-1372.
|
| [49] |
Burslem GM, Smith BE, Lai AC, et al. The advantages of targeted protein degradation over inhibition: an rtk case study[J]. Cell Chem Biol, 2018, 25(1): 67-77.e63.
|
| [50] |
Li Q, Guo Q, Wang S, et al. Design and synthesis of proteolysis targeting chimeras (PROTACs) as an EGFR degrader based on CO-1686[J]. Eur J Med Chem, 2022, 238: 114455.
|
| [51] |
Yang L, Yang Y, Zhang J, et al. Sequential responsive nano-PROTACs for precise intracellular delivery and enhanced degradation efficacy in colorectal cancer therapy[J]. Signal Transduct Target Ther, 2024, 9(1): 275.
|
| [52] |
Li Z, Ren G, Wang X, et al. Tumor microenvironment responsive nano-PROTAC for BRD4 degradation enhanced cancer photo-immunotherapy[J]. Biomaterials, 2025, 322: 123387.
|
| [53] |
Gao J, Hou B, Zhu Q, et al. Engineered bioorthogonal POLY-PROTAC nanoparticles for tumour-specific protein degradation and precise cancer therapy[J]. Nat Commun, 2022, 13(1): 4318.
|
| [54] |
Zhang C, Xu M, He S, et al. Checkpoint nano-PROTACs for activatable cancer photo-immunotherapy[J]. Adv Mater, 2023, 35(6): e2208553.
|
| [55] |
Choi J, Park B, Park JY, et al. Light-triggered PROTAC nanoassemblies for photodynamic ido proteolysis in cancer immunotherapy[J]. Adv Mater, 2024, 36(38): e2405475.
|
| [56] |
He Y, Ju Y, Hu Y, et al. Brd4 proteolysis-targeting chimera nanoparticles sensitized colorectal cancer chemotherapy[J]. J Control Release, 2023, 354: 155-166.
|
| [57] |
Wang X, Yan J, Zhao Y, et al. Targeted degradation of EGFR mutations via self-delivery nano-PROTACs for boosting tumor synergistic immunotherapy[J]. ACS Appl Mater Interfaces, 2025, 17(14): 20943-20956.
|
| [58] |
Zimmermann M, Zimmermann-Kogadeeva M, Wegmann R, et al. Mapping human microbiome drug metabolism by gut bacteria and their genes[J]. Nature, 2019, 570(7762): 462-467.
|
| [59] |
Dale B, Cheng M, Park K S, et al. Advancing targeted protein degradation for cancer therapy[J]. Nat Rev Cancer, 2021, 21(10): 638-654.
|
| [60] |
Moreau K, Coen M, Zhang AX, et al. Proteolysis-targeting chimeras in drug development: a safety perspective[J]. Br J Pharmacol, 2020, 177(8): 1709-1718.
|