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Poly-ADP ribose polymerase (PARP) proteins are critical mediators of DNA repair. Many traditional anti-cancer chemotherapy agents overwhelm a cell’s ability to repair DNA damage in order to kill proliferating malignant cells. Recent evidence suggests that cancers within and across tissue types have specific defects in DNA repair pathways, and that these defects may predispose for sensitivity and resistance to various classes of cytotoxic agents. Breast, ovarian and other cancers develop in the setting of inherited DNA repair deficiency, and these cancers may be more sensitive to cytotoxic agents that induce DNA strand breaks, as well as to inhibitors of PARP activity. A series of recent clinical trials has tested whether PARP inhibitors can achieve synthetic lethality in hereditary DNA repair-deficient tumors. At the current time, mutation of BRCA serves as a potential, but not comprehensive, biomarker to predict response to PARP inhibitor therapy. Mechanisms of resistance to PARP inhibitors are only recently being uncovered. Future studies seek to identify sporadic cancers that harbor genomic instability rendering susceptibility to PARP inhibitors that compound lethal DNA damage.

DNA reapir --- PARP inhibitor --- Homologous Recombination --- combination therapy --- DNA Damage --- Cancer

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Medical centers are widely recognized as vital components of the healthcare system. However, academic medical centers are differentiated from their community counterparts by their mission, which typically focuses on clinical care, education, and research. Nonetheless, community clinics/hospitals fill a critical need and play a complementary role serving as the primary sites for health care in most communities. Furthermore, it is now increasingly recognized that in addition to physicians, physician-scientists, and other healthcare-related professionals, basic research scientists also contribute significantly to the emerging inter- and cross-disciplinary, team-oriented culture of translational science. Therefore, approaches that combine the knowledge, skills, experience, expertise, and visions of clinicians in academic medical centers and their affiliated community centers and hospitals, together with basic research scientists, are critical in shaping the emerging culture of translational research so that patients from the urban as well as suburban settings can avail the benefits of the latest developments in science and medicine. ‘Integrating Clinical and Translational Research Networks—Building Team Medicine’ is an embodiment of this ethos at the City of Hope National Medical Center in Duarte, California. It includes a series of papers authored by teams of leading clinicians, basic research scientists, and translational researchers. The authors discuss how engaging and collaborating with community-based practices, where the majority of older patients with cancer receive their care, can ensure that these patients receive the highest-quality, evidence-based care. Based on our collective experience at City of Hope, we would like to stress that the success of academic-community collaborative programs not only depends on the goodwill and vision of the participants but also on the medical administration, academic leadership, and policymakers who define the principles and rules by which cooperation within the health care industry occurs. We trust that our experience embodied in this singular compendium will serve as a ‘Rosetta Stone’ for other institutions and practitioners.

Medicine --- renal cell carcinoma --- team medicine --- translational research --- community practice --- clinical trials --- geriatric oncology --- older adults --- cancer clinical trials --- recruitment --- community --- team science --- bladder cancer --- urothelial carcinoma --- COVID-19 --- team-based medicine --- colorectal cancer --- precisian medicine --- academic and community oncology --- cancer center --- lung cancer --- lung cancer screening --- low-dose CT scans --- cancer prevention --- smoking cessation --- tobacco control --- national guidelines for screening and prevention --- pharmaceutical aids to smoking cessation --- non-small cell lung cancer --- driver mutations --- testing rates --- receptor tyrosine kinases --- actionable mutations --- next-generation sequencing --- fast-and-frugal trees --- personalized medicine --- minorities --- ethnicity --- race --- breast cancer --- research --- HER2-directed therapy --- community oncology --- academic cancer center --- precision medicine --- cancer genetics --- cancer genomics --- small cell lung cancer --- immunotherapy --- epithelial ovarian cancer --- frontline treatment --- surgical debulking --- adjuvant chemotherapy --- maintenance therapy --- PARP inhibitor --- genetics counseling --- clinical research --- oropharyngeal cancer --- concurrent chemoradiation therapy --- human papillomavirus --- feeding tube dependency --- value-based care --- value-based cancer care --- oncology pathways --- Early Recovery After Surgery (ERAS) --- team-based care --- oncology medical home --- integrated cancer care --- supportive care pathways --- surgical pathways --- cancer care plans --- renal cell carcinoma --- team medicine --- translational research --- community practice --- clinical trials --- geriatric oncology --- older adults --- cancer clinical trials --- recruitment --- community --- team science --- bladder cancer --- urothelial carcinoma --- COVID-19 --- team-based medicine --- colorectal cancer --- precisian medicine --- academic and community oncology --- cancer center --- lung cancer --- lung cancer screening --- low-dose CT scans --- cancer prevention --- smoking cessation --- tobacco control --- national guidelines for screening and prevention --- pharmaceutical aids to smoking cessation --- non-small cell lung cancer --- driver mutations --- testing rates --- receptor tyrosine kinases --- actionable mutations --- next-generation sequencing --- fast-and-frugal trees --- personalized medicine --- minorities --- ethnicity --- race --- breast cancer --- research --- HER2-directed therapy --- community oncology --- academic cancer center --- precision medicine --- cancer genetics --- cancer genomics --- small cell lung cancer --- immunotherapy --- epithelial ovarian cancer --- frontline treatment --- surgical debulking --- adjuvant chemotherapy --- maintenance therapy --- PARP inhibitor --- genetics counseling --- clinical research --- oropharyngeal cancer --- concurrent chemoradiation therapy --- human papillomavirus --- feeding tube dependency --- value-based care --- value-based cancer care --- oncology pathways --- Early Recovery After Surgery (ERAS) --- team-based care --- oncology medical home --- integrated cancer care --- supportive care pathways --- surgical pathways --- cancer care plans

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Medical centers are widely recognized as vital components of the healthcare system. However, academic medical centers are differentiated from their community counterparts by their mission, which typically focuses on clinical care, education, and research. Nonetheless, community clinics/hospitals fill a critical need and play a complementary role serving as the primary sites for health care in most communities. Furthermore, it is now increasingly recognized that in addition to physicians, physician-scientists, and other healthcare-related professionals, basic research scientists also contribute significantly to the emerging inter- and cross-disciplinary, team-oriented culture of translational science. Therefore, approaches that combine the knowledge, skills, experience, expertise, and visions of clinicians in academic medical centers and their affiliated community centers and hospitals, together with basic research scientists, are critical in shaping the emerging culture of translational research so that patients from the urban as well as suburban settings can avail the benefits of the latest developments in science and medicine. ‘Integrating Clinical and Translational Research Networks—Building Team Medicine’ is an embodiment of this ethos at the City of Hope National Medical Center in Duarte, California. It includes a series of papers authored by teams of leading clinicians, basic research scientists, and translational researchers. The authors discuss how engaging and collaborating with community-based practices, where the majority of older patients with cancer receive their care, can ensure that these patients receive the highest-quality, evidence-based care. Based on our collective experience at City of Hope, we would like to stress that the success of academic-community collaborative programs not only depends on the goodwill and vision of the participants but also on the medical administration, academic leadership, and policymakers who define the principles and rules by which cooperation within the health care industry occurs. We trust that our experience embodied in this singular compendium will serve as a ‘Rosetta Stone’ for other institutions and practitioners.

renal cell carcinoma --- team medicine --- translational research --- community practice --- clinical trials --- geriatric oncology --- older adults --- cancer clinical trials --- recruitment --- community --- team science --- bladder cancer --- urothelial carcinoma --- COVID-19 --- team-based medicine --- colorectal cancer --- precisian medicine --- academic and community oncology --- cancer center --- lung cancer --- lung cancer screening --- low-dose CT scans --- cancer prevention --- smoking cessation --- tobacco control --- national guidelines for screening and prevention --- pharmaceutical aids to smoking cessation --- non-small cell lung cancer --- driver mutations --- testing rates --- receptor tyrosine kinases --- actionable mutations --- next-generation sequencing --- fast-and-frugal trees --- personalized medicine --- minorities --- ethnicity --- race --- breast cancer --- research --- HER2-directed therapy --- community oncology --- academic cancer center --- precision medicine --- cancer genetics --- cancer genomics --- small cell lung cancer --- immunotherapy --- epithelial ovarian cancer --- frontline treatment --- surgical debulking --- adjuvant chemotherapy --- maintenance therapy --- PARP inhibitor --- genetics counseling --- clinical research --- n/a --- oropharyngeal cancer --- concurrent chemoradiation therapy --- human papillomavirus --- feeding tube dependency --- value-based care --- value-based cancer care --- oncology pathways --- Early Recovery After Surgery (ERAS) --- team-based care --- oncology medical home --- integrated cancer care --- supportive care pathways --- surgical pathways --- cancer care plans

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This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.

Medicine --- benzofurans --- chemical synthesis --- cytotoxic properties --- HeLa --- MOLT-4 --- K562 --- anticancer --- anti-neuroinflammation --- coumarin --- dihydroartemisinin --- flavonoids --- allene --- E-stereoselective --- regioselective --- anti-cancer activity --- cyanopyridone --- substituted pyridine --- pyridotriazine --- pyrazolopyridine --- thioxotriazopyridine --- anticancer activity --- HepG2 --- antitumor activity --- computational docking --- MDM2-p53 interaction --- xanthones --- yeast-based assays --- estrone derivatives --- hydrazine --- N-substituted pyrazoline --- anti-ovarian cancer --- topoisomerase II inhibitor --- kinase inhibitor --- antiproliferative agent --- urea --- synthesis --- antiproliferative activity --- apoptosis --- indoleamine 2,3-dioxygenase --- inhibitor --- anti-tumor --- immune modulation --- tryptophan metabolism --- taxoids --- βIII-tubulin --- P-glycoprotein --- drug resistance --- thiopene --- thienopyrimidinone --- thiazolidinone --- breast cancer --- benzofuran–pyrazole --- nanoparticles --- cytotoxic activity --- PARP-1 inhibition --- 3,6-dibromocarbazole --- 5-bromoindole --- carbazole --- actin --- migration --- Thienopyrimidine --- Pyrazole --- PI3Kα inhibitor --- quinazolin-4(3H)-one --- quinazolin-4(3H)-thione --- Schiff base --- antioxidant activity --- DFT study --- ortho-quinones --- beta-lapachone --- tanshione IIA --- PI3Ks --- PI3Kδ inhibitors --- 2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide --- anticancer agents --- protein–protein interactions --- virtual screening --- mimetics --- drug discovery --- bivalency --- polyvalency --- antitumor --- cell cycle --- ovarian cancer --- P-MAPA --- IL-12 --- TLR signaling --- inflammation --- chemoresistance --- 4-(pyridin-4-yloxy)benzamide --- 1,2,3-triazole --- c-Met --- natural product --- anticancer agent --- zampanolide --- Talazoparib --- PARP inhibitor --- prodrug --- o-nitro-benzyl --- photoactivatable protecting groups --- salinomycin --- overcoming drug resistance --- tumor specificity --- synergy --- 5-fluorouracil --- gemcitabine --- amides/esters --- colchicine analogs --- thiocolchicine --- colchiceine --- antimitotic agents --- hydrates --- dihydropyranoindole --- HDAC inhibitors --- neuroblastoma --- aromatase --- MCF-7 --- NIH3T3 --- benzimidazole --- triazolothiadiazine --- docking --- ADME --- organosilicon compounds --- SILA-409 (Alis-409) --- SILA-421 (Alis-421) --- multidrug resistance (MDR) reversal --- ABCB1 (P-glycoprotein) --- colon cancer --- colchicine amide --- colchicine sulfonamide --- tubulin inhibitors --- docking studies --- crystal structure --- PROTACs --- protein degradation --- IGF-1R --- Src --- protein kinase --- phenylpyrazolopyrimidine --- enzyme inhibition --- molecular simulation --- androgen receptor --- prostate cancer --- enzalutamide --- apalutamide --- darolutamide --- triple-negative breast cancer --- cytotoxicity --- chrysin analogues --- flavonoid --- anticancer compounds --- benzofurans --- chemical synthesis --- cytotoxic properties --- HeLa --- MOLT-4 --- K562 --- anticancer --- anti-neuroinflammation --- coumarin --- dihydroartemisinin --- flavonoids --- allene --- E-stereoselective --- regioselective --- anti-cancer activity --- cyanopyridone --- substituted pyridine --- pyridotriazine --- pyrazolopyridine --- thioxotriazopyridine --- anticancer activity --- HepG2 --- antitumor activity --- computational docking --- MDM2-p53 interaction --- xanthones --- yeast-based assays --- estrone derivatives --- hydrazine --- N-substituted pyrazoline --- anti-ovarian cancer --- topoisomerase II inhibitor --- kinase inhibitor --- antiproliferative agent --- urea --- synthesis --- antiproliferative activity --- apoptosis --- indoleamine 2,3-dioxygenase --- inhibitor --- anti-tumor --- immune modulation --- tryptophan metabolism --- taxoids --- βIII-tubulin --- P-glycoprotein --- drug resistance --- thiopene --- thienopyrimidinone --- thiazolidinone --- breast cancer --- benzofuran–pyrazole --- nanoparticles --- cytotoxic activity --- PARP-1 inhibition --- 3,6-dibromocarbazole --- 5-bromoindole --- carbazole --- actin --- migration --- Thienopyrimidine --- Pyrazole --- PI3Kα inhibitor --- quinazolin-4(3H)-one --- quinazolin-4(3H)-thione --- Schiff base --- antioxidant activity --- DFT study --- ortho-quinones --- beta-lapachone --- tanshione IIA --- PI3Ks --- PI3Kδ inhibitors --- 2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide --- anticancer agents --- protein–protein interactions --- virtual screening --- mimetics --- drug discovery --- bivalency --- polyvalency --- antitumor --- cell cycle --- ovarian cancer --- P-MAPA --- IL-12 --- TLR signaling --- inflammation --- chemoresistance --- 4-(pyridin-4-yloxy)benzamide --- 1,2,3-triazole --- c-Met --- natural product --- anticancer agent --- zampanolide --- Talazoparib --- PARP inhibitor --- prodrug --- o-nitro-benzyl --- photoactivatable protecting groups --- salinomycin --- overcoming drug resistance --- tumor specificity --- synergy --- 5-fluorouracil --- gemcitabine --- amides/esters --- colchicine analogs --- thiocolchicine --- colchiceine --- antimitotic agents --- hydrates --- dihydropyranoindole --- HDAC inhibitors --- neuroblastoma --- aromatase --- MCF-7 --- NIH3T3 --- benzimidazole --- triazolothiadiazine --- docking --- ADME --- organosilicon compounds --- SILA-409 (Alis-409) --- SILA-421 (Alis-421) --- multidrug resistance (MDR) reversal --- ABCB1 (P-glycoprotein) --- colon cancer --- colchicine amide --- colchicine sulfonamide --- tubulin inhibitors --- docking studies --- crystal structure --- PROTACs --- protein degradation --- IGF-1R --- Src --- protein kinase --- phenylpyrazolopyrimidine --- enzyme inhibition --- molecular simulation --- androgen receptor --- prostate cancer --- enzalutamide --- apalutamide --- darolutamide --- triple-negative breast cancer --- cytotoxicity --- chrysin analogues --- flavonoid --- anticancer compounds

Choose an application

• Reference Manager
• EndNote
• RefWorks (Direct export to RefWorks)

This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.

benzofurans --- chemical synthesis --- cytotoxic properties --- HeLa --- MOLT-4 --- K562 --- anticancer --- anti-neuroinflammation --- coumarin --- dihydroartemisinin --- flavonoids --- allene --- E-stereoselective --- regioselective --- anti-cancer activity --- cyanopyridone --- substituted pyridine --- pyridotriazine --- pyrazolopyridine --- thioxotriazopyridine --- anticancer activity --- HepG2 --- antitumor activity --- computational docking --- MDM2-p53 interaction --- xanthones --- yeast-based assays --- estrone derivatives --- hydrazine --- N-substituted pyrazoline --- anti-ovarian cancer --- topoisomerase II inhibitor --- kinase inhibitor --- antiproliferative agent --- urea --- synthesis --- antiproliferative activity --- apoptosis --- indoleamine 2,3-dioxygenase --- inhibitor --- anti-tumor --- immune modulation --- tryptophan metabolism --- taxoids --- βIII-tubulin --- P-glycoprotein --- drug resistance --- thiopene --- thienopyrimidinone --- thiazolidinone --- breast cancer --- benzofuran–pyrazole --- nanoparticles --- cytotoxic activity --- PARP-1 inhibition --- 3,6-dibromocarbazole --- 5-bromoindole --- carbazole --- actin --- migration --- Thienopyrimidine --- Pyrazole --- PI3Kα inhibitor --- quinazolin-4(3H)-one --- quinazolin-4(3H)-thione --- Schiff base --- antioxidant activity --- DFT study --- ortho-quinones --- beta-lapachone --- tanshione IIA --- PI3Ks --- PI3Kδ inhibitors --- 2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide --- anticancer agents --- protein–protein interactions --- virtual screening --- mimetics --- drug discovery --- bivalency --- polyvalency --- antitumor --- cell cycle --- ovarian cancer --- P-MAPA --- IL-12 --- TLR signaling --- inflammation --- chemoresistance --- 4-(pyridin-4-yloxy)benzamide --- 1,2,3-triazole --- c-Met --- natural product --- anticancer agent --- zampanolide --- Talazoparib --- PARP inhibitor --- prodrug --- o-nitro-benzyl --- photoactivatable protecting groups --- salinomycin --- overcoming drug resistance --- tumor specificity --- synergy --- 5-fluorouracil --- gemcitabine --- amides/esters --- colchicine analogs --- thiocolchicine --- colchiceine --- antimitotic agents --- hydrates --- dihydropyranoindole --- HDAC inhibitors --- neuroblastoma --- aromatase --- MCF-7 --- NIH3T3 --- benzimidazole --- triazolothiadiazine --- docking --- ADME --- organosilicon compounds --- SILA-409 (Alis-409) --- SILA-421 (Alis-421) --- multidrug resistance (MDR) reversal --- ABCB1 (P-glycoprotein) --- colon cancer --- colchicine amide --- colchicine sulfonamide --- tubulin inhibitors --- docking studies --- crystal structure --- PROTACs --- protein degradation --- IGF-1R --- Src --- protein kinase --- phenylpyrazolopyrimidine --- enzyme inhibition --- molecular simulation --- androgen receptor --- prostate cancer --- enzalutamide --- apalutamide --- darolutamide --- triple-negative breast cancer --- cytotoxicity --- chrysin analogues --- flavonoid --- anticancer compounds