close menu
Bookswagon-24x7 online bookstore
close menu
My Account
Home > Mathematics and Science Textbooks > Chemistry > Structure Based Design of Potent and Specific Phosphatidyl-Inositol-3-Kinase and Braf Inhibitors: (English)
Structure Based Design of Potent and Specific Phosphatidyl-Inositol-3-Kinase and Braf Inhibitors: (English)

Structure Based Design of Potent and Specific Phosphatidyl-Inositol-3-Kinase and Braf Inhibitors: (English)

          
5
4
3
2
1

Out of Stock


Premium quality
Premium quality
Bookswagon upholds the quality by delivering untarnished books. Quality, services and satisfaction are everything for us!
Easy Return
Easy return
Not satisfied with this product! Keep it in original condition and packaging to avail easy return policy.
Certified product
Certified product
First impression is the last impression! Address the book’s certification page, ISBN, publisher’s name, copyright page and print quality.
Secure Checkout
Secure checkout
Security at its finest! Login, browse, purchase and pay, every step is safe and secured.
Money back guarantee
Money-back guarantee:
It’s all about customers! For any kind of bad experience with the product, get your actual amount back after returning the product.
On time delivery
On-time delivery
At your doorstep on time! Get this book delivered without any delay.
Notify me when this book is in stock
Add to Wishlist

About the Book

Mutations that constitutively activate the PI3K and PI3K signaling pathway are found in a variety of human cancers, implicating the PI3K lipid kinase as an attractive target for the development of therapeutic agents to treat cancer and other related diseases. In this thesis, I present studies on the combination of a novel organometallic kinase inhibitor scaffold with structure-based design to develop a PI3K inhibitor, called E5E2, with an IC50 potency in the mid-low-nanomolar range and selectivity against a panel of protein kinases. E5E2 inhibits phospho-AKT in human melanoma cells and leads to growth inhibition. Consistent with a role for the PI3K pathway in tumor cell invasion, E5E2 treatment also inhibits the migration of melanoma cells in a 3D spheroid assay. The structure of the PI3Kgamma/E5E2 complex reveals the molecular features that give rise to this potency and selectivity towards lipid kinases with implications for the design of a subsequent generation of PI3K-isoform specific organometallic inhibitors. BRAF mutations were found in about 67% of human malignant melanoma and a hyper-activating V600E mutation in the kinase domain accounts for more than 90% of these cancer mutations. Thus, BRAF has been proven to be an ideal target for developing small molecule inhibitors for therapeutic purpose. The molecular basis for BRAF regulation and V600E oncogenic activation are also captivating subject of research. In the chapter 3 and chapter 4 of this thesis, I present the identification and subsequent optimizations of novel and potent BRAF organometallic and organic inhibitors using structure-based inhibitor design, high throughput screening and high throughput virtual in silico screening. The structural evidence from the co-crystal structures of BRAF kinase with these inhibitors demonstrates that they inhibit BRAF in an active conformation and further suggests the potential mechanism for phosphor-regulation and BRAFV600E oncogene induced activation. The structural information about an active conformation of BRAF kinase is also informative in designing the next generation of potent BRAFV600E oncogene specific inhibitors for therapeutic application.


Best Seller

| | See All


Product Details
  • ISBN-13: 9781243536488
  • Publisher: Proquest, Umi Dissertation Publishing
  • Publisher Imprint: Proquest, Umi Dissertation Publishing
  • Height: 246 mm
  • No of Pages: 252
  • Series Title: English
  • Weight: 458 gr
  • ISBN-10: 1243536489
  • Publisher Date: 01 Sep 2011
  • Binding: Paperback
  • Language: English
  • Returnable: N
  • Spine Width: 13 mm
  • Width: 189 mm


Similar Products

How would you rate your experience shopping for books on Bookswagon?

Add Photo
Add Photo

Customer Reviews

REVIEWS           
Click Here To Be The First to Review this Product
Structure Based Design of Potent and Specific Phosphatidyl-Inositol-3-Kinase and Braf Inhibitors: (English)
Proquest, Umi Dissertation Publishing -
Structure Based Design of Potent and Specific Phosphatidyl-Inositol-3-Kinase and Braf Inhibitors: (English)
Writing guidlines
We want to publish your review, so please:
  • keep your review on the product. Review's that defame author's character will be rejected.
  • Keep your review focused on the product.
  • Avoid writing about customer service. contact us instead if you have issue requiring immediate attention.
  • Refrain from mentioning competitors or the specific price you paid for the product.
  • Do not include any personally identifiable information, such as full names.

Structure Based Design of Potent and Specific Phosphatidyl-Inositol-3-Kinase and Braf Inhibitors: (English)

Required fields are marked with *

Review Title*
Review
    Add Photo Add up to 6 photos
    Would you recommend this product to a friend?
    Tag this Book
    Read more
    Does your review contain spoilers?
    What type of reader best describes you?
    I agree to the terms & conditions
    You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.

    CUSTOMER RATINGS AND REVIEWS AND QUESTIONS AND ANSWERS TERMS OF USE

    These Terms of Use govern your conduct associated with the Customer Ratings and Reviews and/or Questions and Answers service offered by Bookswagon (the "CRR Service").


    By submitting any content to Bookswagon, you guarantee that:
    • You are the sole author and owner of the intellectual property rights in the content;
    • All "moral rights" that you may have in such content have been voluntarily waived by you;
    • All content that you post is accurate;
    • You are at least 13 years old;
    • Use of the content you supply does not violate these Terms of Use and will not cause injury to any person or entity.
    You further agree that you may not submit any content:
    • That is known by you to be false, inaccurate or misleading;
    • That infringes any third party's copyright, patent, trademark, trade secret or other proprietary rights or rights of publicity or privacy;
    • That violates any law, statute, ordinance or regulation (including, but not limited to, those governing, consumer protection, unfair competition, anti-discrimination or false advertising);
    • That is, or may reasonably be considered to be, defamatory, libelous, hateful, racially or religiously biased or offensive, unlawfully threatening or unlawfully harassing to any individual, partnership or corporation;
    • For which you were compensated or granted any consideration by any unapproved third party;
    • That includes any information that references other websites, addresses, email addresses, contact information or phone numbers;
    • That contains any computer viruses, worms or other potentially damaging computer programs or files.
    You agree to indemnify and hold Bookswagon (and its officers, directors, agents, subsidiaries, joint ventures, employees and third-party service providers, including but not limited to Bazaarvoice, Inc.), harmless from all claims, demands, and damages (actual and consequential) of every kind and nature, known and unknown including reasonable attorneys' fees, arising out of a breach of your representations and warranties set forth above, or your violation of any law or the rights of a third party.


    For any content that you submit, you grant Bookswagon a perpetual, irrevocable, royalty-free, transferable right and license to use, copy, modify, delete in its entirety, adapt, publish, translate, create derivative works from and/or sell, transfer, and/or distribute such content and/or incorporate such content into any form, medium or technology throughout the world without compensation to you. Additionally,  Bookswagon may transfer or share any personal information that you submit with its third-party service providers, including but not limited to Bazaarvoice, Inc. in accordance with  Privacy Policy


    All content that you submit may be used at Bookswagon's sole discretion. Bookswagon reserves the right to change, condense, withhold publication, remove or delete any content on Bookswagon's website that Bookswagon deems, in its sole discretion, to violate the content guidelines or any other provision of these Terms of Use.  Bookswagon does not guarantee that you will have any recourse through Bookswagon to edit or delete any content you have submitted. Ratings and written comments are generally posted within two to four business days. However, Bookswagon reserves the right to remove or to refuse to post any submission to the extent authorized by law. You acknowledge that you, not Bookswagon, are responsible for the contents of your submission. None of the content that you submit shall be subject to any obligation of confidence on the part of Bookswagon, its agents, subsidiaries, affiliates, partners or third party service providers (including but not limited to Bazaarvoice, Inc.)and their respective directors, officers and employees.

    Accept

    New Arrivals

    | | See All


    Inspired by your browsing history


    Your review has been submitted!

    You've already reviewed this product!
    ASK VIDYA