化学·生活·社会 
																		 
									
										
		  							 
          							
		  			
    
	|
 
	
	
	
	  
        						 
      						
      					 
  					 
					
    					 
   					 
   										
    					肿瘤PET示踪剂核素标记中的基础化学  
  					 
  					  										
						杨雪梅1 , 乔雨宸2 , 郝亚萌1 , 王志鹏3,4* , 任鹏1*  
					 
															
						1.哈尔滨工业大学(深圳)理学院 广东深圳 518055;  2.华大研究院生物智能技术研究所广东深圳 518103;  3.Division of Genetics,Department of Medicine,Brigham and Women’s Hospital,Boston,Massachusetts 02115,United States;Department of Biological Chemistry and Molecular Pharmacology,Harvard Medical School,Boston,Massachusetts 02115,United States;  4.Desai Sethi Urology Institute,Sylvester Comprehensive Cancer Center,University of Miami Miller School of Medicine,Miami,FL 33136,United States 
					 
					  					
    					 
   					 
   					
   										
    					Basic Chemistry in Radionuclide Labeling of Tumor PET Tracers  
  					 
  					  					  					
						YANG Xue-Mei1 , QIAO Yu-Chen2 , HAO Ya-Meng1 , WANG Zhipeng A3,4* , REN Peng1*  
					 
															
						1. School of Science,Harbin Institute of Technology(Shenzhen),Shenzhen 518055,China;  2. BGI-Shenzhen,Shenzhen 518103,China;  3. Division of Genetics,Department of Medicine,Brigham and Women’s Hospital,Boston,Massachusetts 02115,United States;Department of Biological Chemistry and Molecular Pharmacology,Harvard Medical School,Boston, Massachusetts 02115,United States;  4. Desai Sethi Urology Institute,Sylvester Comprehensive Cancer Center, University of Miami Miller School of Medicine,Miami,FL 33136,United States 
					   
									
				
				
					
						
							
								
									
										
											
                        					 
												
													
													    
													    	
									 
								 
								
																										
													    
													    		                            																		 
  														 
		                            																	    摘要: 癌症作为全球主要的致死原因之一,对公共卫生构成了巨大的挑战。癌症的防控策略不仅需要治疗技术的进步,也同样需要诊断技术的发展。肿瘤的发生和发展伴随着细胞结构和功能的多种变化,以及肿瘤微环境的显著改变。在这些变化过程中,特定分子的表达水平会出现异常,这些异常表达的分子可以作为肿瘤诊断的生物标志物。近年来,正电子发射断层扫描(Positron Emission Tomography,简称PET)作为一种重要的分子成像技术,已被广泛应用于检测肿瘤的结构和功能变化。PET技术的核心在于放射性示踪剂的开发与应用,这些示踪剂的设计和合成一般基于化学原理的深入理解和创新应用。本文旨在综述PET中几种典型的放射性示踪剂,并探讨核素标记过程中涉及的化学原理,增进对PET在肿瘤诊断中应用的理解,并提升对化学在生物医学领域中作用的认识。此外,PET放射性示踪剂的设计和合成过程是化学教育的宝贵资源,对化学在生命科学相关学科的教学具有重要意义。
																										     
													    
													    	
															 
														 
												  		 
												         
												        														
															关键词:  癌症 , 
																																肿瘤诊断 , 
																																正电子发射断层 , 
																																放射性示踪剂 , 
																																化学应用  
																																  
															 
														 
																												
														
															
															    																	收稿日期:  2024-06-19
															    															        
															    															 
														 
														 																											    														
															
															通讯作者: 
																*王志鹏,E-mail:wzpchem1991@gmail.com;任鹏,E-mail:repeng@hit.edu.cu   
																													     		 
													     	 
														 
																																									
													
														
															引用本文:     
														 
														
															
																杨雪梅, 乔雨宸, 郝亚萌, 王志鹏, 任鹏. 肿瘤PET示踪剂核素标记中的基础化学[J]. 化学教育(中英文), 2025, 46(6):                         	1-10
                             
															 
														 
														 
														
														
													
												 
												
												
													
																																													
																	[1] 
																	 
														     			王志鹏,申镇,蒋振雄,等.化学教育(中英文),2021,42(16):1-10
														     																	     
																	 
																  
																															
																	[2] 
																	 
														     			王志鹏,程农壹,马新雨,等.化学教育(中英文),2019,40(10):12-18
														     																	     
																	 
																  
																															
																	[3] 
																	 
														     			张淑贤,乔晋萍,李崧,等.化学教育,2015,36(14):1-5
														     																	     
																	 
																  
																															
																	[4] 
																	 
														     			姚新月,张利芳,曹建花,等.化学教育(中英文),2017,38(2):24-29
														     																	     
																	 
																  
																															
																	[5] 
																	 
														     			Bray F,Laversanne M,Weiderpass E,et al.Cancer,2021,127(16):3029-3030
														     																	     
																	 
																  
																															
																	[6] 
																	 
														     			Ferlay J,Colombet M,Soerjomataram I,et al.International Journal of Cancer,2021,149(4):778-789
														     																	     
																	 
																  
																															
																	[7] 
																	 
														     			Marusyk A,Polyak K.Biochimica et Biophysica Acta,2010,1805(1):105-117
														     																	     
																	 
																  
																															
																	[8] 
																	 
														     			Hanahan D,Weinberg R A.Cell,2011,144(5):646-674
														     																	     
																	 
																  
																															
																	[9] 
																	 
														     			Swain S M,Shastry M,Hamilton E.Nature Reviews:Drug Discovery,2023,22(2):101-126
														     																	     
																	 
																  
																															
																	[10] 
																	 
														     			Paquette M,Lavallée É,Phoenix S,et al.Journal of Nuclear Medicine,2018,59(2):197-203
														     																	     
																	 
																  
																															
																	[11] 
																	 
														     			Ristau B T,O′keefe D S,Bacich D J.Urologic Oncology,2014,32(3):272-279
														     																	     
																	 
																  
																															
																	[12] 
																	 
														     			Junttila M R,De Sauvage F J.Nature,2013,501(7467):346-354
														     																	     
																	 
																  
																															
																	[13] 
																	 
														     			Fan P,Zhang N,Candi E,et al.Oncogene,2023,42(49):3591-3604
														     																	     
																	 
																  
																															
																	[14] 
																	 
														     			Guelfi S,Hodivala-Dilke K,Bergers G.Nature Reviews Cancer,2024,24(10):655-675
														     																	     
																	 
																  
																															
																	[15] 
																	 
														     			Voron T,Colussi O,Marcheteau E,et al.Journal of Experimental Medicine,2015,212(2):139-148
														     																	     
																	 
																  
																															
																	[16] 
																	 
														     			Robert C.Nature Communications,2020,11(1):3801
														     																	     
																	 
																  
																															
																	[17] 
																	 
														     			Sharma P,Goswami S,Raychaudhuri D,et al.Cell,2023,186(8):1652-1669
														     																	     
																	 
																  
																															
																	[18] 
																	 
														     			Dall’olio F G,Marabelle A,Caramella C,et al.Nature Reviews Clinical Oncology,2022,19(2):75-90
														     																	     
																	 
																  
																															
																	[19] 
																	 
														     			Lewis D Y,Soloviev D,Brindle K M.Cancer Journal,2015,21(2):129-136
														     																	     
																	 
																  
																															
																	[20] 
																	 
														     			Schwenck J,Sonanini D,Cotton J M,et al.Nature Reviews Cancer,2023,23(7):474-490
														     																	     
																	 
																  
																															
																	[21] 
																	 
														     			Phelps M E.Proceedings of the National Academy of Sciences of the United States of America,2000,97(16):9226-9233
														     																	     
																	 
																  
																															
																	[22] 
																	 
														     			Beyer T,Townsend D W,Brun T,et al.Journal of Nuclear Medicine,2000,41(8):1369-1379
														     																	     
																	 
																  
																															
																	[23] 
																	 
														     			Al-Nabhani K Z,Syed R,Michopoulou S,et al.Journal of Nuclear Medicine,2014,55(1):88-94
														     																	     
																	 
																  
																															
																	[24] 
																	 
														     			Schöder H,Erdi Y E,Larson S M,et al.European Journal of Nuclear Medicine and Molecular Imaging,2003,30(10):1419-1437
														     																	     
																	 
																  
																															
																	[25] 
																	 
														     			Vāvere A L,Scott P J H.Seminars in Nuclear Medicine,2017,47(5):429-453
														     																	     
																	 
																  
																															
																	[26] 
																	 
														     			Pichler V,Berroterán-Infante N,Philippe C,et al.Journal of Nuclear Medicine,2018,59(9):1350-1354
														     																	     
																	 
																  
																															
																	[27] 
																	 
														     			Brasse D,Nonat A.Dalton Transactions,2015,44(11):4845-4858
														     																	     
																	 
																  
																															
																	[28] 
																	 
														     			Rösch F.Recent Results in Cancer Research,2013,194:3-16
														     																	     
																	 
																  
																															
																	[29] 
																	 
														     			Abrantes A M,Pires A S,Monteiro L,et al.Biochim Biophys Acta Mol Basis Dis,2020,1866(6):165717
														     																	     
																	 
																  
																															
																	[30] 
																	 
														     			Nayak T K,Brechbiel M W.Bioconjugate Chemistry,2009,20(5):825-841
														     																	     
																	 
																  
																															
																	[31] 
																	 
														     			De Feo M S,Pontico M,Frantellizzi V,et al.Clinical and Translational Imaging,2022,10(1):23-36
														     																	     
																	 
																  
																															
																	[32] 
																	 
														     			Rong J,Haider A,Jeppesen T E,et al.Nature Communications,2023,14(1):3257
														     																	     
																	 
																  
																															
																	[33] 
																	 
														     			Goud N S,Joshi R K,Bharath R D,et al.European Journal of Medical Chemistry,2020,187:111979
														     																	     
																	 
																  
																															
																	[34] 
																	 
														     			Preshlock S,Tredwell M,Gouverneur V.Chemical Reviews,2016,116(2):719-766
														     																	     
																	 
																  
																															
																	[35] 
																	 
														     			Velikyan I.Theranostics,2013,4(1):47-80
														     																	     
																	 
																  
																															
																	[36] 
																	 
														     			Buck A K,Reske S N.Journal of Nuclear Medicine,2004,45(3):461-463
														     																	     
																	 
																  
																															
																	[37] 
																	 
														     			Fletcher J W,Djulbegovic B,Soares H P,et al.Journal of Nuclear Medicine,2008,49(3):480-508
														     																	     
																	 
																  
																															
																	[38] 
																	 
														     			Yu S.Biomedical Imaging and Intervention Journal,2006,2(4):e57
														     																	     
																	 
																  
																															
																	[39] 
																	 
														     			Peck M,Pollack H A,Friesen A,et al.Quarterly Journal of Nuclear Medicine and Molecular Imaging,2015,59(1):95-104
														     																	     
																	 
																  
																															
																	[40] 
																	 
														     			Bodapati S,Abraham P,Chen A,et al.Tomography,2022,8(2):1060-1065
														     																	     
																	 
																  
																															
																	[41] 
																	 
														     			Michaud L,Touijer K A,Mauguen A,et al.Journal of Nuclear Medicine,2020,61(6):827-833
														     																	     
																	 
																  
																															
																	[42] 
																	 
														     			Szydło M,Jadwiński M,Chmura A,et al.Contemp Oncol(Pozn),2016,20(3):229-236
														     																	     
																	 
																  
																															
																	[43] 
																	 
														     			Comar D,Cartron J,Maziere M,et al.European Journal of Nuclear Medicine,1976,1(1):11-14
														     																	     
																	 
																  
																															
																	[44] 
																	 
														     			Soloviev D,Tamburella C.Applied Radiation and Isotopes,2006,64(9):995-1000
														     																	     
																	 
																  
																															
																	[45] 
																	 
														     			杨雪梅,王志鹏,张永臻,等.化学教育(中英文),2024,45(6):99-107
														     																	     
																	 
																  
																															
																	[46] 
																	 
														     			Ajish Kumar K S,Mathur A.European Journal of Medicinal Chemistry Reports,2021,3:100014
														     																	     
																	 
																  
																															
																	[47] 
																	 
														     			Chatterjee S,Lesniak W G,Miller M S,et al.Biochemical and Biophysical Research Communications,2017,483(1):258-263
														     																	     
																	 
																  
																															
																	[48] 
																	 
														     			Meyer J P,Adumeau P,Lewis J S,et al.Bioconjugate Chemistry,2016,27(12):2791-2807
														     																	     
																	 
																  
																															
																	[49] 
																	 
														     			Dammes N,Peer D.Theranostics,2020,10(2):938-955
														     																	     
																	 
																  
																															
																	[50] 
																	 
														     			De Silva R A,Kumar D,Lisok A,et al.Molecular Pharmaceutics,2018,15(9):3946-3952
														     																	     
																	 
																  
																															
																	[51] 
																	 
														     			Chomet M,Schreurs M,Bolijn M J,et al.European Journal of Nuclear Medicine and Molecular Imaging,2021,48(3):694-707
														     																	     
																	 
																  
																															
																	[52] 
																	 
														     			Lesniak W G,Chatterjee S,Gabrielson M,et al.Bioconjugate Chemistry,2016,27(9):2103-2110
														     																	     
																	 
																  
																															
																	[53] 
																	 
														     			Mossine A V,Tanzey S S,Brooks A F,et al.Nature Protocols,2020,15(5):1742-1759
														     																	     
																	 
																  
																															
																	[54] 
																	 
														     			Doi H.J. Labelled Comp. Radiopharm.,2015,58(3):73-85
														     																	     
																	 
																  
																															
																	[55] 
																	 
														     			Lanzenberger R R,Mitterhauser M,Spindelegger C,et al.Biological Psychiatry,2007,61(9):1081-1089
														     																	     
																	 
																  
																															
																	[56] 
																	 
														     			Dahl K,Schou M,Amini N,et al.European Journal of Organic Chemistry,2013,2013(7):1228-1231